!Source	"The Drug Repurposing Hub, Broad Institute"				
!URL	http://www.broadinstitute.org/repurposing				
!File_date	3/24/2020				
!Table_name	drug information				
!API_available	We suggest using the available data API and/or custom web export function for additional annotation fields and database source information.				
!Disclaimer	For research use only. Do not use the Repurposing Hub to make clinical treatment decisions. BROAD DOES NOT GUARANTEE OR WARRANT THE ACCURACY OF THE DATA WITHIN THE REPURPOSING HUB.  RELIANCE ON THE REPURPOSING HUB IS AT THE USER'S SOLE RISK.				
!Restrictions	The Drug Repurposing Hub data is provided for non-commercial use only.				
!Citation	"Please cite usage as: Corsello SM, et al. Nature Medicine. 2017 Apr 7;23(4):405-408. doi: 10.1038/nm.4306."				
!Contact	repurposing@broadinstitute.org				
pert_iname	clinical_phase	moa	target	disease_area	indication
(R)-(-)-apomorphine	Launched	dopamine receptor agonist	ADRA2A|ADRA2B|ADRA2C|CALY|DRD1|DRD2|DRD3|DRD4|DRD5|HTR1A|HTR1B|HTR1D|HTR2A|HTR2B|HTR2C|HTR5A	neurology/psychiatry	Parkinson's Disease
(R)-(-)-rolipram	Phase 1	phosphodiesterase inhibitor	PDE4A|PDE4B|PDE4C|PDE4D|PDE5A		
(R)-baclofen	Phase 3	benzodiazepine receptor agonist	GABBR1|GABBR2		
(S)-(+)-rolipram	Phase 1	phosphodiesterase inhibitor	PDE4B|PDE4D		
"[sar9,met(o2)11]-substance-p"	Preclinical	tachykinin antagonist	TACR1		
A-1070722	Preclinical	glycogen synthase kinase inhibitor	GSK3A|GSK3B		
A-1120	Preclinical	retinoid receptor ligand	RBP4		
A-317491	Preclinical	purinergic receptor antagonist	P2RX3		
A-33903	Phase 2				
A-366	Preclinical	histone lysine methyltransferase inhibitor	EHMT1|EHMT2		
A-381393	Preclinical	dopamine receptor antagonist			
A-412997	Preclinical	dopamine receptor agonist	DRD4		
A-438079	Preclinical	purinergic receptor antagonist	P2RX7		
A-485	Preclinical	histone acetyltransferase inhibitor			
A-582941	Preclinical	nicotinic receptor agonist	CHRNA7		
A-61603	Preclinical	adrenergic receptor agonist	ADRA1A|ADRA1B|ADRA1D		
A-674563	Preclinical	AKT inhibitor	AKT1|PKIA|PRKACA		
A-7	Preclinical	calmodulin antagonist			
A-769662	Preclinical	AMPK activator			
A-784168	Preclinical	transient receptor potential channel antagonist	TRPV1		
A-803467	Preclinical	sodium channel blocker	SCN10A		
A-804598	Preclinical	purinergic receptor antagonist	P2RX7		
A-839977	Preclinical	purinergic receptor antagonist	P2RX7		
A-867744	Preclinical	acetylcholine receptor allosteric modulator	CHRNA3|CHRNA4|CHRNA7		
A-887826	Preclinical	sodium channel blocker	SCN10A		
A-922500	Preclinical	diacylglycerol O acyltransferase inhibitor	DGAT1		
A-939572	Preclinical	stearoyl-CoA desaturase inhibitor	SCD		
A-967079	Preclinical	transient receptor potential channel antagonist	TRPA1		
A-987306	Preclinical	histamine receptor antagonist	ADORA1|AVPR1A|CCR1|CHRM1|CHRM2|CHRM3|CHRM4|DRD3|HTR1A|HTR1B|HTR2A|HTR2B|HTR3A|TACR2		
AA-29504	Preclinical	GABA receptor positive allosteric modulator	GABRA1|GABRA4|GABRB3		
AAI101	Phase 3	lactamase inhibitor			
AB-423	Preclinical	HBV capsid assembly inhibitor			
abacavir	Launched	nucleoside reverse transcriptase inhibitor		infectious disease	human immunodeficiency virus (HIV-1)
abafungin	Phase 3	sterol methyltransferase inhibitor			
abamectin	Launched	benzodiazepine receptor agonist	GABBR1|GABBR2	infectious disease	gastrointestinal parasites
abametapir	Phase 3	metalloproteinase inhibitor	MMP9		
abarelix	Phase 3	gonadotropin releasing factor hormone receptor antagonist	GNRHR		
ABBV-744	Phase 1	bromodomain inhibitor			
ABC-294640	Phase 2	sphingosine kinase inhibitor	SPHK2		
abemaciclib	Launched	CDK inhibitor	CDK4|CDK6	oncology	breast cancer
abiraterone	Launched	androgen biosynthesis inhibitor	CYP11B1|CYP17A1	oncology	prostate cancer
abiraterone-acetate	Launched	androgen biosynthesis inhibitor	CYP17A1	oncology	prostate cancer
ABT-072	Phase 2	RNA polymerase inhibitor			
ABT-202	Phase 1	acetylcholine receptor agonist			
ABT-239	Phase 1	histamine receptor antagonist	HRH1|HRH2|HRH3		
ABT-491	Phase 1	platelet activating factor receptor antagonist	PTAFR		
ABT-639	Phase 2	calcium channel blocker	CACNA1G|CACNA1H|CACNA1I		
ABT-702	Preclinical	adenosine kinase inhibitor	ADK		
ABT-724	Phase 2	dopamine receptor agonist	DRD4		
ABT-737	Phase 1/Phase 2	BCL inhibitor	BCL2|BCL2L1|BCL2L2		
ABT-751	Phase 2	tubulin polymerization inhibitor	TUBB		
ABX-1431	Phase 2	monoacylglycerol lipase inhibitor			
ABX464	Phase 2	antiviral			
AC-186	Preclinical	estrogen receptor agonist	ESR2		
AC-261066	Preclinical	retinoid receptor agonist	RARB		
AC-264613	Preclinical	PAR agonist	F2RL1		
AC-55541	Preclinical	PARP inhibitor	PARP2		
AC-55649	Preclinical	retinoid receptor agonist	RARA|RARB		
AC-710	Preclinical	PDGFR tyrosine kinase receptor inhibitor	CSF1R|FLT3|KIT|PDGFRA|PDGFRB		
AC-7954-(+/-)	Preclinical	urotensin receptor agonist	UTS2R		
acadesine	Phase 3	AMPK activator			
acalabrutinib	Launched	Bruton's tyrosine kinase (BTK) inhibitor	BTK	hematologic malignancy	mantle cell lymphoma (MCL)
acalisib	Phase 1	PI3K inhibitor	PIK3CB|PIK3CD		
acamprosate	Launched	glutamate receptor antagonist	GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ|GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|GRIN3A|GRIN3B|GRM5	neurology/psychiatry	abstinence from alcohol
acarbose	Launched	glucosidase inhibitor	AMY2A|MGAM	endocrinology	diabetes mellitus
ACDPP	Preclinical	glutamate receptor antagonist	GRM5		
acebilustat	Phase 2	leukotriene inhibitor			
acebutolol	Launched	adrenergic receptor antagonist	ADRB1	cardiology	hypertension|ventricular arrhythmias
acecainide	Phase 3	polarization inhibitor	SCN5A		
aceclidine	Launched	acetylcholine receptor agonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5	ophthalmology	glaucoma
aceclofenac	Launched	prostanoid receptor antagonist	PTGS2	rheumatology	rheumatoid arthritis|ankylosing spondylitis|osteoarthritis|periarthritis|lumbago|ischiadynia
acedapsone	Launched			infectious disease	leprosy
acedoben	Phase 2				
acefylline	Launched	adenosine receptor agonist	ADORA1	pulmonary	asthma
aceglutamide	Launched			gastroenterology	peptic ulcer disease (PUD)
acelarin	Phase 2/Phase 3	anticancer agent			
acemetacin	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	rheumatology	osteoarthritis
aceneuramic-acid	Phase 3		CES1|SELE|SELP		
acenocoumarol	Launched	vitamin K antagonist	VKORC1	hematology	deep vein thrombosis (DVT)
acepromazine	Launched	dopamine receptor antagonist	ADRA1A|ADRA1B|DRD1|DRD2|HTR1A|HTR2A	neurology/psychiatry	sedative
acesulfame-potassium	Phase 3				
acetanilide	Preclinical	hydrogen peroxide decomposition inhibitor			
acetarsol	Launched			gastroenterology	diarrhea
acetazolamide	Launched	carbonic anhydrase inhibitor	AQP1|CA1|CA12|CA14|CA2|CA3|CA4|CA7	ophthalmology	glaucoma
acetohexamide	Launched	ATP channel blocker	ABCC8|KCNJ1|KCNJ10|KCNJ11	endocrinology	diabetes mellitus
acetohydroxamic-acid	Launched	urease inhibitor	MMP12	infectious disease	urinary tract infections
acetophenazine	Launched	dopamine receptor antagonist	DRD1|DRD2	neurology/psychiatry	psychosis
acetriazoic-acid	Preclinical				
acetyl-farnesyl-cysteine	Launched	methyltransferase inhibitor	PPARG	dermatology	acne vulgaris (AV)
acetyl-l-leucine	Launched			neurology/psychiatry	vertigo
acetyl-11-keto-beta-boswellic-acid	Phase 2	lipoxygenase inhibitor	HSD11B1|HSD11B2		
acetylcholine	Launched	acetylcholine receptor agonist	ACHE|CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|CHRNA2	neurology/psychiatry|gastroenterology|pulmonary	drowsiness|fatigue|headache|indigestion|chest congestion
acetylcysteine	Launched	mucolytic agent	ACY1|CHUK|GRIN1|GRIN2A|GRIN2B|GRIN2D|GRIN3A|GSS|IKBKB|RELA|SLC7A11	gastroenterology	acetaminophen overdose|hepatic injury
acetylsalicylsalicylic-acid	Preclinical	cyclooxygenase inhibitor			
acetylspiramycin	Preclinical	other antibiotic			
acexamic-acid	Launched	5 alpha reductase inhibitor	GAST	dermatology	wound healing
acifran	Phase 3	cholesterol inhibitor	HCAR2|HCAR3		
acipimox	Launched	cholesterol inhibitor	HCAR2	endocrinology	hyperlipidemia
acitazanolast	Launched	mediator release inhibitor		allergy	allergic rhinitis
acitretin	Launched	retinoid receptor agonist	RARA|RARB|RARG|RBP1|RXRA|RXRB|RXRG|STAT3	dermatology	psoriasis
acivicin	Phase 2	gamma glutamyltransferase inhibitor	CTPS1		
aclarubicin	Launched	topoisomerase inhibitor	TOP1|TOP2A	hematologic malignancy	acute myeloid leukemia (AML)
aclidinium	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5	pulmonary	bronchitis|emphysema|chronic obstructive pulmonary disease (COPD)
acolbifene	Phase 3	estrogen receptor antagonist			
acoziborole	Preclinical	antitrypanosomal			
ACPC	Phase 1	glutamate receptor antagonist			
acriflavine	Launched	hypoxia inducible factor inhibitor	HIF1A	infectious disease	fungal infection
acriflavinium	Launched	hypoxia inducible factor inhibitor	HIF1A	infectious disease	fungal infection
acrisorcin	Launched	other antifungal		infectious disease	fungal infection
acrivastine	Launched	histamine receptor antagonist	HRH1	allergy	allergic rhinitis
acrylate	Phase 3	mucus protecting agent			
ACT-132577	Launched	endothelin receptor antagonist	EDNRA|EDNRB	pulmonary	pulmonary arterial hypertension (PAH)
ACT-462206	Phase 1	orexin receptor antagonist	HCRTR1|HCRTR2		
actarit	Launched	interleukin receptor agonist		rheumatology	rheumatoid arthritis
ACTB-1003	Phase 1	FGFR inhibitor|VEGFR inhibitor	KDR|TEK		
actinomycin-d	Launched	RNA polymerase inhibitor		oncology	Wilm's tumor|Ewing's sarcoma|rhabdomyosarcoma|testicular carcinoma
actinoquinol	Preclinical				
acumapimod	Phase 1	p38 MAPK inhibitor			
ACY-1215	Phase 1/Phase 2	HDAC inhibitor	HDAC1|HDAC2|HDAC3|HDAC6|HDAC8		
acyclovir	Launched	DNA polymerase inhibitor	PNP	infectious disease	genitial herpes|shingles|chicken pox
AC1NDSS5	Phase 1				
AC260584	Preclinical	cholinergic receptor agonist			
AD-5467	Phase 2	aldose reductase inhibitor	AKR1B1		
adapalene	Launched	retinoid receptor agonist	RARA|RARB|RARG|RXRA|RXRB|RXRG	dermatology	acne vulgaris (AV)
adaprev	Phase 3	TGF beta receptor inhibitor	AKR1B1|GPI|HK1|M6PR|PYGM		
adaptavir	Phase 2	CC chemokine receptor antagonist	CCR5		
adarotene	Phase 1	retinoid receptor agonist	RARB|RARG		
adatanserin	Phase 2	serotonin receptor agonist|serotonin receptor antagonist	HTR1A|HTR2A		
adavivint	Phase 1	WNT pathway inhibitor			
ADD-233089	Phase 1	benzodiazepine receptor agonist			
adefovir	Launched	DNA polymerase inhibitor		infectious disease	hepatitis B
adefovir-dipivoxil	Launched	DNA polymerase inhibitor		infectious disease	hepatitis B
adelmidrol	Launched	anti-inflammatory agent		dermatology	dermatitis
ademetionine	Launched	methyltransferase stimulant|phosphodiesterase inhibitor		neurology/psychiatry	depression|attention-deficit/hyperactivity disorder (ADHD)
adenine	Preclinical	protein synthesis stimulant	ACACB|ACP1|APRT|MTAP|PECR|SRPK2		
adenosine	Launched	adenosine receptor agonist	ADORA1|ADORA2A|ADORA2B|ADORA3|PI4K2A|PI4K2B|TRPM4	cardiology	Wolff-Parkinson-White Syndrome (WPW)
adenosine-phosphate	Launched	adenosine receptor agonist	ACSL1|ACSS1|ACSS2|ADCY1|ADK|CREB1|FBP1|HINT1|PDE4B|PDE4D|PIM1|PRKAA1|PRKAB1|PRKAB2|PYGL|TRPM4		
adenosine-triphosphate	Phase 2	adenosine receptor agonist	ABCA1|ABCB1|ABCB11|ABCC2|ABCC8|ABCC9|ABCG1|ABL1|ABL2|ACSL1|ACSS1|ACSS2|ACVR1|ACVR1B|ACVRL1|ADCY1|ADRBK1|ADRBK2|AFG3L2|AKT1|ALK|AMHR2|APAF1|ARAF|ASNA1|ASNS|ASS1|CDK15|GPR17|ITPR1|NAE1|NT5C2|P2RY1|P2RY11|P2RY13|P2RY2|P2RY4|PRKAA1|RYR1|RYR2|RYR3|SLC25A4|TNK2|TRPM4|TRPM7		
adiphenine	Launched	acetylcholine receptor antagonist	CHRNA1	neurology/psychiatry	spasms
adipic-acid	Preclinical	solute carrier family member inhibitor	SLC22A6		
adiporon	Preclinical	adiponectin receptor agonist	ADIPOR1|ADIPOR2		
ADL5859	Phase 2	opioid receptor agonist	OPRD1		
adomeglivant	Preclinical	glucagon receptor antagonist			
adoprazine	Phase 2	dopamine receptor antagonist|serotonin receptor agonist	DRD2|HTR1A		
adrafinil	Launched	adrenergic receptor agonist		neurology/psychiatry	fatigue
adrenalone	Launched	adrenergic receptor agonist	ADRA1A	hematology	hemorrhage
adrenosterone	Preclinical	11-beta hydroxysteroid dehydrogenase inhibitor	HSD11B1|HSD11B2		
ADX-10059	Phase 2	glutamate receptor negative allosteric modulator	GRM5		
ADX-47273	Preclinical	glutamate receptor modulator	GRM5		
AEE788	Phase 1/Phase 2	EGFR inhibitor|VEGFR inhibitor	EGFR|ERBB2|ERBB4|FGFR2|FGFR3|KDR		
AEG3482	Preclinical	HSP inducer			
afalanine	Phase 3	dopamine receptor agonist	DRD2		
afamelanotide	Launched	melanocyte-stimulating hormone mimetic			
afatinib	Launched	EGFR inhibitor	EGFR|ERBB2|ERBB4	oncology	non-small cell lung cancer (NSCLC)
afimoxifene	Phase 2	estrogen receptor antagonist	ESR1|ESR2|ESRRG|PLD1|PRKCD|PRKCE|PRKCQ|PRKCZ		
afloqualone	Launched	acetylcholine receptor antagonist		neurology/psychiatry	sedative
AFN-1252	Phase 2	FABI inhibitor			
afobazole	Launched	anxiolytic		neurology/psychiatry	anxiety
AF38469	Preclinical	sortilin inhibitor	SORT1		
AG-1024	Preclinical	insulin growth factor receptor inhibitor	IGF1R		
AG-14361	Preclinical	PARP inhibitor	PARP1		
AG-490	Preclinical	EGFR inhibitor|JAK inhibitor	EGFR|JAK2|JAK3		
AG-555	Preclinical	tyrosine kinase inhibitor	CDK2		
AG-556	Preclinical	tyrosine kinase inhibitor			
AGI-5198	Preclinical	isocitrate dehydrogenase inhibitor	IDH1		
AGI-6780	Preclinical	isocitrate dehydrogenase inhibitor	IDH2		
AGM-1470	Phase 2	cell cycle inhibitor	METAP2		
agmatine	Phase 3	nitric oxide synthase inhibitor	ADRA2C|ASIC3|CACNA1B|CHRNA1|GRIN1|KCNJ1|NISCH		
AGN-192403	Preclinical	imidazoline receptor ligand	NISCH		
AGN-194310	Phase 3	retinoid receptor antagonist	RXRA|RXRB|RXRG		
AGN-195183	Phase 1/Phase 2	retinoid receptor agonist	RARA		
agomelatine	Launched	melatonin receptor agonist|serotonin receptor antagonist	HTR2A|HTR2B|HTR2C|MTNR1A|MTNR1B	neurology/psychiatry	depression
AGP-103	Launched	membrane permeability inhibitor			
AH-7614	Preclinical	free fatty acid receptor antagonist	FFAR4		
AH11110	Preclinical	adrenergic receptor ligand	ADRA1B		
AH6809	Preclinical	prostanoid receptor antagonist	PTGDR|PTGER1|PTGER2|PTGER3		
AI-10-49	Preclinical	core binding factor inhibitor	CBFB		
AIM-100	Preclinical	tyrosine kinase inhibitor	TNK2		
ajmaline	Launched	sodium channel blocker		cardiology	Wolff-Parkinson-White Syndrome (WPW)
AJ76-(+)	Preclinical	dopamine receptor antagonist	DRD2|DRD3|DRD4		
AK-7	Preclinical	SIRT inhibitor	SIRT2		
AKBA	Phase 3	lipoxygenase inhibitor	ALOX5		
aklomide	Launched			infectious disease	coccidiosis
AL-8697	Preclinical	p38 MAPK inhibitor	MAPK14		
alacepril	Launched	angiotensin converting enzyme inhibitor	ACE	cardiology	hypertension
alafosfalin	Phase 1	bacterial cell wall synthesis inhibitor			
alagebrium	Phase 2/Phase 3	glycosylation inhibitor			
alanine	Launched				
alanosine	Phase 2	antimetabolite			
alantolactone	Preclinical	apoptosis stimulant|STAT inhibitor	STAT3		
alaproclate	Phase 2	serotonin receptor antagonist	SLC6A4		
alarelin	Launched	gonadotropin releasing factor hormone receptor antagonist	GNRH1		
albendazole	Launched	tubulin polymerization inhibitor	TUBA1A|TUBB|TUBB4B	infectious disease	cystic hydatid disease|parenchymal neurocysticercosis
albendazole-oxide	Launched	anthelmintic agent		infectious disease	cystic hydatid disease|parenchymal neurocysticercosis
albuterol	Launched	adrenergic receptor agonist	ADRB2	pulmonary	asthma
alcaftadine	Launched	histamine receptor antagonist	HRH1	allergy	allergic conjunctivitis
alclofenac	Launched	cyclooxygenase inhibitor	PTGS1	rheumatology	rheumatoid arthritis
alclometasone-dipropionate	Launched	glucocorticoid receptor agonist	CYP3A4|NR3C1|SERPINA6	dermatology	corticosteroid-responsive dermatoses
alcuronium	Launched	muscle relaxant	CHRM1|CHRM2|CHRM3|CHRM4|CHRNA7	neurology/psychiatry	muscle relaxant
alda-1	Preclinical	aldehyde dehydrogenase activator	ALDH2		
aldoxorubicin	Phase 3	topoisomerase inhibitor	TOP2A		
alectinib	Launched	ALK tyrosine kinase receptor inhibitor	ALK|MET	oncology	non-small cell lung cancer (NSCLC)
alendronate	Launched	bone resorption inhibitor	ATP6V1A|FDPS|PTPN4|PTPRE|PTPRS	orthopedics	osteoporosis
alexidine	Preclinical	phosphatidylglycerophosphatase inhibitor	PTPMT1		
alfacalcidol	Launched	vitamin D receptor agonist	CYP27B1|VDR	endocrinology	vitamin D deficiency
alfadolone-acetate	Phase 2	benzodiazepine receptor agonist			
alfuzosin	Launched	adrenergic receptor antagonist	ADRA1A|ADRA1B|ADRA1D|SCN10A|SCN11A|SCN1A|SCN2A|SCN3A|SCN4A|SCN5A|SCN7A|SCN8A|SCN9A	urology	benign prostatic hyperplasia (BPH)
algestone-acetophenide	Launched			endocrinology	contraceptive
alibendol	Launched	antispasmodic		gastroenterology	bile stimulation
alimemazine	Launched	histamine receptor agonist|histamine receptor antagonist	HRH1	neurology/psychiatry|allergy|pulmonary	sedative|urticaria|itching|cough suppressant
alinidine	Phase 3	bradycardic effect 			
alisertib	Phase 3	Aurora kinase inhibitor	AURKA		
aliskiren-hemifumarate	Launched	renin inhibitor	REN	cardiology	hypertension
alisporivir	Phase 3	cyclophilin inhibitor			
alizapride	Launched	dopamine receptor antagonist		gastroenterology	nausea
alizarin	Preclinical				
allantoin	Launched	cosmetic		dermatology	skin protectant
allicin	Phase 2	cytokine production inhibitor	TRPA1|TRPV1		
allopurinol	Launched	xanthine oxidase inhibitor	XDH	rheumatology|urology	gout|kidney stones
allopurinol-riboside	Phase 2	anti-leishmanial agent|phosphorylase inhibitor			
allylestrenol	Launched	steroidal progestin	ESR1|PGR|SLC6A9	obstetrics/gynecology	premature labor
allylisothiocyanate	Preclinical	TRPV agonist	TRPA1		
allylthiourea	Preclinical	nitrification inhibitor			
almitrine	Launched	neurotransmitter agonist	ATP1A1	pulmonary	chronic obstructive pulmonary disease (COPD)
almorexant	Phase 3	orexin receptor antagonist	HCRTR1|HCRTR2		
almotriptan	Launched	serotonin receptor agonist	HTR1B|HTR1D	neurology/psychiatry	migraine headache
aloe-emodin	Preclinical	anticancer agent	CASP8		
alogliptin	Launched	dipeptidyl peptidase inhibitor	DPP4	endocrinology	diabetes mellitus
aloin	Preclinical	angiogenesis inhibitor			
aloperine	Preclinical				
alosetron	Withdrawn	serotonin receptor antagonist	HTR3A		
alovudine	Phase 2	DNA synthesis marker			
aloxistatin	Phase 3	protease inhibitor	CTSG		
alpelisib	Launched	PI3K inhibitor	PIK3CA|PIK3CB|PIK3CD|PIK3CG	oncology	breast cancer
alpha-asarone	Preclinical	cytochrome P450 inhibitor|HMGCR inhibitor	HMGCR		
alpha-D-glucopyranose	Preclinical				
alpha-glucosyl-hesperidin	Preclinical	antioxidant			
alpha-linolenic-acid	Phase 3	omega 3 fatty acid stimulant	ELOVL4|FADS1|FADS2|FFAR1|FFAR4|PTGS2|SLC8A1|TRPV1		
alpha-methylhistamine-dihydrobromide-(R)-(-)	Preclinical	histamine receptor agonist	HRH3		
alpha-methylhistamine-dihydrobromide-(S)-(+)	Preclinical	histamine receptor agonist	HRH3		
alpha-methylserotonin	Preclinical	serotonin receptor agonist	HTR1D|HTR1E|HTR1F|HTR2A|HTR2B|HTR2C|HTR4		
alpha-tochopherol	Launched	antioxidant		endocrinology	vitamin E deficiency
alpha-tochopheryl-acetate	Launched	antioxidant		endocrinology	vitamin E deficiency
alpidem	Withdrawn	benzodiazepine receptor agonist	GABRA1		
alprenolol	Launched	adrenergic receptor antagonist	ADRB1|ADRB2	cardiology	angina pectoris
alprostadil	Launched	prostanoid receptor agonist	CATSPER1|CATSPER2|CATSPER3|CATSPER4|PTGDR|PTGER1|PTGER2|PTGER4|PTGIR	cardiology	congenital heart defects
alrestatin	Preclinical	aldose reductase inhibitor	AKR1B1		
ALS-8112	Phase 1				
ALS-8176	Phase 1	RNA polymerase inhibitor			
altanserin	Phase 2	serotonin receptor antagonist	HTR2A		
althiazide	Launched	diuretic		cardiology	hypertension
altinicline	Phase 2	nicotinic receptor agonist	CHRNA4|CHRNB2		
altiratinib	Phase 1	MET inhibitor|VEGFR inhibitor	KDR|MET|TEK		
altrenogest	Launched	progestogen hormone	PGR	endocrinology	estrus
altretamine	Launched	DNA synthesis inhibitor		oncology	ovarian cancer
alverine	Launched	muscle relaxant	HTR1A	gastroenterology	irritable bowel syndrome|diverticular disease
alvespimycin	Phase 2	HSP inhibitor	HSP90AA1		
alvimopan	Launched	opioid receptor antagonist	OPRD1|OPRK1|OPRM1	gastroenterology	postoperative ileus
alvocidib	Phase 2	CDK inhibitor	CDK1|CDK2|CDK4|CDK5|CDK6|CDK7|CDK8|CDK9|EGFR|PYGM		
ALX-40-4C	Preclinical	CC chemokine receptor antagonist			
ALX-5407	Phase 1	glycine transporter inhibitor	SLC6A9		
AM-1241	Preclinical	cannabinoid receptor agonist	CNR1|CNR2		
AM-24	Phase 2	lipoxygenase inhibitor	ALOX5		
AM-251	Preclinical	cannabinoid receptor antagonist	CNR1|GPR18|GPR55		
AM-281	Preclinical	cannabinoid receptor antagonist	CNR1|CNR2|GPR55		
AM-404	Preclinical	cyclooxygenase inhibitor|FAAH inhibitor|TRPV antagonist	CNR1|CNR2|FAAH|TRPV1		
AM-580	Preclinical	retinoid receptor agonist	RARA		
AM-630	Preclinical	cannabinoid receptor antagonist	CNR1|CNR2		
AM-92016	Preclinical	potassium channel blocker	GRIN1		
amantadine	Launched	glutamate receptor antagonist	DRD2|GRIN2A|GRIN2B|GRIN2C|GRIN2D|GRIN3A	infectious disease|neurology/psychiatry	influenza A virus infection|Parkinson's Disease
ambazone	Phase 1	DNA damage inducer			
ambenonium	Launched	cholinesterase inhibitor	ACHE	neurology/psychiatry	myasthenia gravis
ambrisentan	Launched	endothelin receptor antagonist	EDNRA|EDNRB	pulmonary	pulmonary arterial hypertension (PAH)
ambroxol	Launched	sodium channel blocker	CYP3A4	pulmonary	bronchitis
amcasertib	Phase 2	kinase inhibitor			
amcinonide	Launched	glucocorticoid receptor agonist	NR3C1	dermatology	corticosteroid-responsive dermatoses
AMD-3465	Preclinical	CC chemokine receptor antagonist	CXCR4		
amdinocillin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	urinary tract infections|gram-negative bacterial infections
AMD11070	Phase 3	CC chemokine receptor antagonist	CCR5|CXCR4		
ameltolide	Preclinical	anticonvulsant			
amenamevir	Phase 1	helicase primase inhibitor			
ametantrone	Preclinical	anticancer agent			
amezinium	Launched	adrenergic receptor agonist	ADRB2	cardiology	hypotension
amfenac	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	neurology/psychiatry	pain relief
amflutizole	Phase 2	xanthine oxidase inhibitor	XDH		
AMG-PERK-44	Preclinical	PERK inhibitor	EIF2AK4		
AMG-176	Phase 1	MCL1 inhibitor			
AMG-208	Phase 1	tyrosine kinase inhibitor	MET		
AMG-232	Phase 2	MDM inhibitor	MDM2		
AMG-319	Phase 2	PI3K inhibitor	PIK3CD		
AMG-337	Phase 2	MET inhibitor	MET		
AMG-487	Phase 2	CC chemokine receptor antagonist			
AMG-487-(+/-)	Phase 2	CC chemokine receptor antagonist	CXCR3		
AMG-510	Phase 1/Phase 2	K-Ras inhibitor			
AMG-517	Phase 1	TRPV antagonist	TRPV1		
AMG-548	Phase 1	MAP kinase inhibitor	MAPK11|MAPK12|MAPK13|MAPK14		
AMG-837	Phase 1	free fatty acid receptor agonist	FFAR1		
AMG-925	Phase 1	CDK inhibitor|FLT3 inhibitor	CDK4|CDK6|FLT3		
AMG-9810	Preclinical	TRPV antagonist	TRPV1		
AMG319	Phase 2	PI3K inhibitor	PIK3CD		
AMG458	Preclinical	MET inhibitor	MET		
AMG900	Phase 1	Aurora kinase inhibitor	AURKA|AURKB|AURKC		
AMI-1	Preclinical	protein arginine N-methyltransferase inhibitor	PRMT1		
amibegron	Phase 3	adrenergic receptor agonist	ADRB3		
amidopyrine	Launched	analgesic agent		dermatology	dermatitis herpetiformis (DH)
amifampridine	Launched	potassium channel blocker		neurology/psychiatry	Lambert-Eaton myasthenic syndrome (LEMS)
amiflamine	Phase 1	monoamine oxidase inhibitor	MAOA|SLC6A2		
amifostine	Launched	reducing agent	ALPPL2|ENPP1	nephrology	renal toxicity
amikacin	Launched	bacterial 30S ribosomal subunit inhibitor		infectious disease	gram-negative bacterial infections
amiloride	Launched	sodium channel blocker	AOC1|ASIC1|ASIC2|ASIC3|PKD2|PKD2L1|PLAU|SCNN1A|SCNN1B|SCNN1D|SCNN1G|SLC9A1|TRPC7|TRPV2	cardiology	hypertension|congestive heart failure
amineptine	Withdrawn	dopamine receptor agonist	SLC6A2|SLC6A4		
aminocaproic-acid	Launched	plasminogen activator inhibitor	LPA|PLAT|PLG	hematology	fibrinolytic bleeding
aminoglutethimide	Launched	glucocorticoid receptor antagonist	CYP11A1|CYP19A1	endocrinology|oncology	Cushing's syndrome|breast cancer
aminoguanidine	Phase 3	nitric oxide synthase inhibitor	AKR1B1|NOS2|TIMP3		
aminohydroxybutyric-acid	Launched			neurology/psychiatry	epilepsy
aminolevulinic-acid-benzyl-ester	Phase 1				
aminomethyltransferase	Preclinical	nitric oxide synthase inhibitor	NOS2		
aminopentamide	Launched	acetylcholine receptor antagonist	CHRM1	gastroenterology	acute abdominal visceral spasm|hypertrophic gastritis (GHG)|nausea
aminophylline	Launched	adenosine receptor antagonist	ADORA1|ADORA2A|ADORA2B|ADORA3|HDAC2|PDE3A|PDE3B|PDE4A|PDE4B|PDE4C|PDE4D|PDE5A	pulmonary	asthma|bronchitis|emphysema
aminopterin	Phase 3	dihydrofolate reductase inhibitor	DHFR|SLC46A1		
aminopurvalanol-a	Preclinical	CDK inhibitor|tyrosine kinase inhibitor	CDK1|CDK2|CDK5		
aminosalicylate	Launched	cyclooxygenase inhibitor	ALOX5|CHUK|PLA2G2E|PTGS1|PTGS2	gastroenterology	inflammatory bowel disease|ulcerative colitis
aminothiadiazole	Phase 2	inosine monophosphate dehydrogenase inhibitor	ADORA3|IMPDH1		
aminothiazole	Preclinical	cyclin D inhibitor	NOS2		
amiodarone	Launched	potassium channel blocker	ADRB1|CACNA1H|CACNA2D2|KCNA7|KCNH2	cardiology	ventricular arrhythmias
amiprilose	Phase 3	CD antagonist			
amiselimod	Phase 2	sphingosine 1-phosphate receptor modulator			
amisulpride	Launched	dopamine receptor antagonist	DRD2	neurology/psychiatry	psychosis|bipolar disorder|schizophrenia
amitifadine	Phase 3	serotonin transporter (SERT) inhibitor	SLC6A2|SLC6A3|SLC6A4		
amitraz	Launched	adrenergic receptor agonist	ADRA1A|ADRA2A	infectious disease	generalized demodicosis
amitriptyline	Launched	norepinephrine inhibitor|norepinephrine reuptake inhibitor|serotonin receptor antagonist|serotonin–norepinephrine reuptake inhibitor (SNRI)	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRB1|ADRB2|ADRB3|CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|HRH1|HRH2|HRH4|HTR1A|HTR1B|HTR1D|HTR2A|HTR2C|HTR6|HTR7|KCNA1|KCND2|KCND3|KCNQ2|KCNQ3|NTRK1|NTRK2|OPRD1|OPRK1|OPRM1|SIGMAR1|SLC6A2|SLC6A4	neurology/psychiatry	depression
amlexanox	Launched	histamine receptor modulator	FGF1|IL3|PDE4A|PDE4B|PDE4C|PDE4D|S100A12|S100A13	dental|pulmonary|ophthalmology|allergy	aphthous ulcers|asthma|conjunctivitis|allergic rhinitis
amlodipine	Launched	calcium channel blocker	CACNA1C|CACNA1D|CACNA1F|CACNA1S|CACNA2D1	cardiology	hypertension|chronic stable angina|vasospastic angina|coronary artery disease (CAD)
ammonium-glycyrrhizinate	Launched	thrombin inhibitor	HSD11B1|HSD11B2|SLCO1B1|SLCO1B3	dermatology	cosmetic
ammonium-lactate	Launched		HCAR1	dermatology	xerosis cutis|ichthyosis vulgaris
ammonium-perfluorocaprylate	Phase 1	Pim kinase inhibitor	PIM1		
AMN-082	Preclinical	glutamate receptor modulator	GRM7		
amodiaquine	Launched	histamine receptor agonist	HNMT	infectious disease	malaria
amonafide	Phase 3	topoisomerase inhibitor	TOP2A|TOP2B		
amorolfine	Launched	membrane integrity inhibitor		infectious disease	onychomycosis
amoxapine	Launched	norepinephrine reputake inhibitor	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|DRD1|DRD2|DRD3|DRD4|DRD5|GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ|HRH1|HRH4|HTR1A|HTR1B|HTR2A|HTR2B|HTR2C|HTR3A|HTR6|HTR7|SLC6A2|SLC6A3|SLC6A4	neurology/psychiatry	depression
amoxicillin	Launched	penicillin binding protein inhibitor	CYP2C19|SLC15A1|SLC15A2|SLC22A6	infectious disease|gastroenterology	skin infections|duodenal ulcer disease|gonorrhea|ear infections|throat infections|genitourinary tract infections|respiratory tract infections
AMPA-(RS)	Preclinical	glutamate receptor agonist	GRIN1		
AMPA-(S)	Preclinical	glutamate receptor agonist	GRIA2|GRIN1		
ampalex	Phase 2	glutamate receptor agonist	GRIA1|GRIA2|GRIA3|GRIA4		
amperozide	Launched	dopamine receptor antagonist	FAAH|HTR2A	neurology/psychiatry	psychosis
amphotericin-b	Launched	membrane permeability enhancer		infectious disease	fungal infection
ampicillin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	respiratory tract infections|meningitis|bacterial septicemia|endocarditis|urinary tract infections|gastrointestinal infections
ampiroxicam	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	neurology/psychiatry	pain relief
amprenavir	Launched	HIV protease inhibitor		infectious disease	human immunodeficiency virus (HIV-1)
amprolium	Launched	thiamine uptake blocker		infectious disease	coccidiosis
ampyrone	Preclinical	cyclooxygenase inhibitor			
amrinone	Launched	phosphodiesterase inhibitor	PDE3A|PDE3B|PDE4B|TNF	cardiology	congestive heart failure
amrubicin	Launched	topoisomerase inhibitor	TOP2A|TOP2B	oncology	small cell lung cancer
amsacrine	Launched	topoisomerase inhibitor	KCNH2|TOP2A	hematologic malignancy	acute lymphoblastic leukemia (ALL)
amthamine	Preclinical	histamine receptor agonist	HRH2		
amtolmetin-guacil	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	rheumatology	rheumatoid arthritis|osteoarthritis
amuvatinib	Phase 2	FLT3 inhibitor|KIT inhibitor|PDGFR tyrosine kinase receptor inhibitor|RAD51 inhibitor|RET tyrosine kinase inhibitor	KIT|MET		
amygdalin	Phase 2	caspase activator	CASP3		
amyl-nitrite	Preclinical	atrial natriuretic peptide receptor agonist			
amyleine	Preclinical	local anesthetic			
amylene-hydrate	Preclinical	local anesthetic			
AMZ30	Preclinical	protein phosphatase inhibitor			
AM095	Preclinical	lysophosphatidic acid receptor antagonist			
AM211	Preclinical	prostaglandin inhibitor			
AM679	Preclinical	cannabinoid receptor agonist|lipoxygenase inhibitor	ALOX5AP|CNR1|CNR2		
ANA-12	Preclinical	tropomyosin receptor kinase inhibitor	NTRK2		
anabasine	Preclinical	acetylcholine receptor agonist			
anacetrapib	Phase 3	cholesteryl ester transfer protein inhibitor	CETP		
anagliptin	Launched	dipeptidyl peptidase inhibitor	DPP4	endocrinology	diabetes mellitus
anagrelide	Launched	phosphodiesterase inhibitor	PDE3A	hematology|hematologic malignancy	thrombocythemia|myeloproliferative neoplasms
anamorelin	Phase 3	growth hormone secretagogue receptor agonist	GHSR		
anandamide	Phase 2	cannabinoid receptor agonist	CACNA1G|CACNA1H|CACNA1I|CNR1|CNR2|GLRA1|GPR18|GPR55|KCNA2|KCNK3|KCNK9|TRPM8|TRPV1		
anastrozole	Launched	aromatase inhibitor	CYP19A1	oncology	breast cancer
andarine	Phase 1	androgen receptor modulator	AR		
andrographolide	Phase 2	tumor necrosis factor production inhibitor	IL1B|IL6|NFKB1|NFKB2|TNF		
androstenone	Preclinical	steroid			
androsterone	Preclinical	androgen receptor agonist			
anecortave-acetate	Launched	angiogenesis inhibitor		ophthalmology	macular degeneration
anethole	Launched	glutathione transferase stimulant			
anethole-trithione	Launched	glutathione transferase stimulant		dental	xerostomia
anguidine	Phase 2	protein synthesis inhibitor	SLC5A1		
anidulafungin	Launched	"fungal 1,3-beta-D-glucan synthase inhibitor"		infectious disease	candidemia|fungal infection|esophageal candidiasis
aniracetam	Launched	glutamate receptor agonist	DRD2|GRIA1|GRIA2|GRIA3|GRIA4|HTR2A		
anisindione	Launched	vitamin K antagonist	GGCX	hematology	deep vein thrombosis (DVT)
anisodamine	Phase 3	lipid peroxidase inhibitor	ADRA1A		
anisomycin	Preclinical	DNA synthesis inhibitor	NHP2L1|RPL10L|RPL11|RPL13A|RPL15|RPL19|RPL23|RPL23A|RPL26L1|RPL3|RPL37|RPL8|RSL24D1		
anisotropine	Launched	acetylcholine receptor antagonist		gastroenterology	peptic ulcer disease (PUD)
anlotinib	Launched	PDGFR tyrosine kinase receptor inhibitor|VEGFR inhibitor	KDR|PDGFRB		
anpirtoline	Phase 1	serotonin receptor agonist	HTR1B		
ANR-94	Preclinical	adenosine receptor antagonist	ADORA2A		
ansamitocin-p-3	Preclinical	apoptosis stimulant			
antagonist-g	Phase 1	neuropeptide receptor antagonist	MAPK8		
antalarmin	Preclinical	corticotropin releasing factor receptor antagonist	CRHR1		
antazoline	Launched	antihistamine	HRH1	ophthalmology|otolaryngology	conjunctivitis|nasal congestion
anthralin	Launched	DNA synthesis inhibitor		dermatology	psoriasis
anthraquinone	Preclinical	CDC inhibitor	CDC25B		
antimony-potassium	Phase 2				
antimonyl	Phase 1				
antimycin-A	Preclinical	ATP synthase inhibitor	CYCS		
antioxine	Launched				
AN2718	Phase 1	leucyl-tRNA synthetase inhibitor			
AP-18	Preclinical	transient receptor potential channel antagonist	TRPA1		
apabetalone	Phase 3	apolipoprotein expression enhancer	BRD3		
apafant	Phase 3	platelet activating factor receptor antagonist	PTAFR		
apalutamide	Launched	androgen receptor antagonist		oncology	prostate cancer
apararenone	Preclinical	mineralocorticoid receptor antagonist			
apatinib	Phase 3	RET tyrosine kinase inhibitor	CSK|KDR|KIT|RET		
APC-100	Phase 1/Phase 2	androgen receptor antagonist|anti-inflammatory agent	AR		
APcK-110	Preclinical	KIT inhibitor	KIT|STAT3		
APD597	Phase 1	glucose dependent insulinotropic receptor agonist	GPR119		
APD668	Phase 1	glucose dependent insulinotropic receptor agonist	GPR119		
aphidicolin	Phase 1	RNA synthesis inhibitor			
API-001	Phase 2	sigma receptor antagonist	SIGMAR1		
API-1	Preclinical	AKT inhibitor	AKT1|AKT2|AKT3		
apigenin	Preclinical	casein kinase inhibitor|cell proliferation inhibitor	AKR1B1|AR|CDK6|CFTR|CYP19A1|CYP1B1|HSD17B1		
apixaban	Launched	coagulation factor inhibitor	F10	neurology/psychiatry|hematology|cardiology	stroke|systemic embolism|pulmonary embolism (PE)|atrial fibrillation (AF)|deep vein thrombosis (DVT)
apocynin	Phase 1	NADPH oxidase inhibitor	NOX4		
apoptosis-activator-II	Preclinical	carboxylesterase inhibitor	BCHE|CES1		
APR-246	Phase 3	p53 activator	TP53		
apraclonidine	Launched	adrenergic receptor agonist	ADRA1A|ADRA2A|ADRA2B|ADRA2C	ophthalmology	glaucoma|intraocular pressure
apramycin	Launched	bacterial 30S ribosomal subunit inhibitor		infectious disease	gram-negative bacterial infections
apratastat	Phase 2	matrix metalloprotease inhibitor|tumor necrosis factor production inhibitor	ADAM17|MMP1|MMP13|MMP9		
apremilast	Launched	phosphodiesterase inhibitor	PDE4A|PDE4B|PDE4C|PDE4D	dermatology|rheumatology	psoriasis|psoriatic arthritis
aprepitant	Launched	tachykinin antagonist	TACR1	gastroenterology	nausea|vomiting
apricitabine	Phase 3	nucleoside reverse transcriptase inhibitor			
aprindine	Launched	voltage-gated sodium channel blocker	CALM1|SCN5A	cardiology	cardiac arrythmia
apronal	Preclinical	cytochrome P450 modulator			
aptiganel	Phase 3	glutamate receptor antagonist	GRIN1		
APTO-253	Phase 1	krüppel-like factor expression enhancer	KLF4		
APY-29	Preclinical	serine/threonine kinase inhibitor	ERN1		
apyramide	Preclinical	cyclooxygenase inhibitor			
APY0201	Preclinical	phosphoinositide dependent kinase inhibitor	IL12A|IL12B|PIKFYVE		
AP1903	Phase 1/Phase 2		MTOR		
AP26113	Phase 2	ALK tyrosine kinase receptor inhibitor	ALK|EGFR		
AQ-RA741	Preclinical	acetylcholine receptor antagonist	CHRM2		
AQ-13	Phase 2	antimalarial agent			
AQW-051	Preclinical	nicotinic receptor agonist			
AR-A014418	Preclinical	glycogen synthase kinase inhibitor	GSK3B		
AR-C155858	Preclinical	monocarboxylate transporter inhibitor	SLC16A1|SLC16A7		
AR-12	Phase 1	phosphoinositide dependent kinase inhibitor	PDPK1		
AR-42	Phase 1	HDAC inhibitor	HDAC1		
arachidonic-acid	Phase 1	cytochrome P450 inhibitor	CLCN2|KCNJ4|KCNK10|KCNK18|KCNK2|PRKCZ|PTGS1|TRPC6|TRPM2		
aramchol	Phase 2/Phase 3	stearoyl-CoA desaturase inhibitor			
arbidol	Launched	cytochrome P450 inhibitor	CYP3A4	infectious disease	influenza A virus infection
arbutin	Phase 2/Phase 3	melanin inhibitor	TYR		
ARC-239	Preclinical	adrenergic receptor antagonist	ADRA2A|ADRA2B|ADRA2C		
arctigenin	Preclinical	MEK inhibitor	CHUK|MAP2K1		
arcyriaflavin-a	Preclinical	CDK inhibitor	CCND1|CDK4		
ardeparin	Withdrawn	thrombin inhibitor	SERPIND1		
arecaidine-but-2-ynyl-ester	Preclinical	acetylcholine receptor agonist	CHRM2		
arecaidine-propargyl-ester	Preclinical	acetylcholine receptor agonist	CHRM1|CHRM2|CHRM3|CHRM4		
arecoline	Phase 1	acetylcholine receptor agonist	CHRM1|CHRM2|CHRM3|CHRM4		
argatroban	Launched	thrombin inhibitor	F2	hematology	heparin-induced thrombocytopenia (HIT)
argireline	Phase 3	neurotransmitter release inhibitor			
arglabin	Launched	farnesyltransferase inhibitor	FNTA|NFKB1		
aripiprazole	Launched	serotonin receptor agonist|serotonin receptor antagonist	ADRA1A|ADRA1B|ADRA2A|ADRA2B|ADRA2C|CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|DRD1|DRD2|DRD3|DRD4|DRD5|HRH1|HTR1A|HTR1B|HTR1D|HTR1E|HTR2A|HTR2C|HTR3A|HTR6|HTR7	neurology/psychiatry	depression|schizophrenia|bipolar disorder
aripiprazole-lauroxil	Launched	serotonin receptor agonist		neurology/psychiatry	schizophrenia
arofylline	Phase 3	phosphodiesterase inhibitor	PDE4A		
arotinolol	Launched	adrenergic receptor antagonist	ADRB3	cardiology|neurology/psychiatry	hypertension|tremors
ARQ-092	Phase 1	AKT inhibitor	AKT2		
ARQ-621	Phase 1	kinesin-like spindle protein inhibitor	KIF11		
ARRY-334543	Phase 2/Phase 3	EGFR inhibitor	ERBB2		
arsanilic-acid	Phase 1		LYZ		
arsenic-trioxide	Launched	apoptosis stimulant	AKT1|CCND1|IKBKB|JUN|MAPK1|MAPK3|TXNRD1	gastroenterology	diarrhea
artemether	Launched	antimalarial agent	ATP1A1	infectious disease	malaria
artemisinin	Launched	DNA synthesis inhibitor	CYP2B6	infectious disease	malaria
artemotil	Launched			infectious disease	malaria
artesunate	Launched	DNA synthesis inhibitor		infectious disease	malaria
articaine	Launched	local anesthetic		neurology/psychiatry	local anesthetic
arundic-acid	Phase 2/Phase 3	astrocyte modulating agent	PTGS2|S100B		
ARV-825	Preclinical	bromodomain inhibitor	BRD4		
AS-1269574	Preclinical	glucose dependent insulinotropic receptor agonist	GPR119		
AS-1892802	Preclinical	rho associated kinase inhibitor	ROCK1		
AS-1949490	Preclinical	SHIP2 phosphatase inhibitor	INPP5D		
AS-2034178	Preclinical	free fatty acid receptor agonist	FFAR1		
AS-2444697	Preclinical	interleukin inhibitor	IRAK4		
AS-252424	Preclinical	PI3K inhibitor	PIK3CG		
AS-604850	Preclinical	PI3K inhibitor	PIK3CA|PIK3CG		
AS-703026	Phase 2	MEK inhibitor	MAP2K1|MAP2K2		
AS-77	Phase 1	potassium channel blocker	KCNA3|KCNA5|KCNN4		
ASA-404	Phase 3	angiogenesis inhibitor			
asapiprant	Preclinical	prostaglandin inhibitor			
asaraldehyde	Preclinical	cyclooxygenase inhibitor	PTGS2		
ASC-J9	Phase 2	androgen receptor enhancer	AR		
asciminib	Phase 2	Bcr-Abl kinase inhibitor			
ascomycin	Preclinical	calcineurin inhibitor	FKBP1A		
ascorbic-acid	Launched	antioxidant	SLC23A1|SLC23A2	endocrinology	scurvy
asenapine	Launched	dopamine receptor antagonist|serotonin receptor antagonist	DRD2|HRH1|HTR1A|HTR1B|HTR1D|HTR1E|HTR2A	neurology/psychiatry	schizophrenia|bipolar disorder
asiatic-acid	Preclinical	apoptosis stimulant	PYGM		
asimadoline	Phase 3	opioid receptor agonist	OPRK1		
asivatrep	Phase 3	transient receptor potential channel antagonist			
ASP-2535	Phase 1	glycine transporter inhibitor	SLC6A9		
ASP-6537	Preclinical	cyclooxygenase inhibitor			
ASP-9521	Preclinical	aldo-keto reductase inhibitor			
aspartame	Launched		TAS1R2|TRPV1		
aspirin	Launched	cyclooxygenase inhibitor	AKR1C1|ASIC3|EDNRA|HSPA5|IKBKB|NFKB1|NFKB2|NFKBIA|PRKAA1|PRKAA2|PRKAB1|PRKAB2|PRKAG1|PRKAG2|PRKAG3|PTGS1|PTGS2|RPS6KA3|TP53	neurology/psychiatry|endocrinology|dental	headache|fever|toothache|muscle pain
ASP3026	Phase 1	ALK tyrosine kinase receptor inhibitor	ALK		
AST-1306	Phase 1	EGFR inhibitor	EGFR|ERBB2		
astaxanthin	Launched	antioxidant			
astemizole	Withdrawn	histamine receptor antagonist	HRH1|KCNH1|KCNH2		
astilbin	Preclinical	nuclear factor erythroid derived|like (NRF2) activator			
astragaloside-a	Preclinical	anti-inflammatory agent			
ASTX660	Phase 1/Phase 2	apoptosis inhibitor			
asunaprevir	Phase 3	HCV inhibitor			
asymmetrical-dimethylarginine	Phase 1	nitric oxide synthase inhibitor	NOS2|NOS3		
AT-1015	Preclinical	serotonin receptor antagonist	HTR2A		
AT-406	Phase 1	IAP antagonist 			
AT-7519	Phase 2	CDK inhibitor	CDK1|CDK2|CDK4|CDK5|CDK6|CDK9		
AT-9283	Phase 2	Aurora kinase inhibitor|JAK inhibitor	AURKA|AURKB|JAK2|JAK3|RPS6KA6|STK17A		
ataluren	Launched	CFTR channel agonist|dystrophin stimulant	DMD	genetics|pulmonary	duchenne muscular dystrophy (DMD)|cystic fibrosis
atazanavir	Launched	HIV protease inhibitor		infectious disease	human immunodeficiency virus (HIV-1)
ATB-346	Phase 2	cyclooxygenase inhibitor	PTGER2		
atenolol-(+)	Preclinical	adrenergic receptor antagonist			
atenolol-(+/-)	Launched	adrenergic receptor antagonist	ADRB1|ADRB2|LTF|PLA2G2E	cardiology	hypertension|angina pectoris
atenolol-(-)	Launched	adrenergic receptor antagonist		cardiology	hypertension
atglistatin	Preclinical	adipose triglyceride lipase inhibitor			
aticaprant	Phase 2	opioid receptor antagonist			
atipamezole	Launched	adrenergic receptor antagonist		neurology/psychiatry	reverse sedative
atiprimod	Phase 2	JAK inhibitor|STAT inhibitor	JAK2|STAT3		
atizoram	Phase 2	phosphodiesterase inhibitor	PDE4A|PDE4B|PDE4C|PDE4D		
ATN-161	Phase 2	integrin antagonist	ITGA5|ITGAV|ITGB1|ITGB3		
atomoxetine	Launched	norepinephrine transporter inhibitor	GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|GRIN3A|GRIN3B|SLC6A2|SLC6A3|SLC6A4	neurology/psychiatry	attention-deficit/hyperactivity disorder (ADHD)
atorvastatin	Launched	HMGCR inhibitor	AHR|DPP4|HMGCR	neurology/psychiatry|cardiology	stroke|heart attack
atosiban	Launched	oxytocin receptor antagonist	AVPR1A|AVPR1B|AVPR2|OXTR	neurology/psychiatry|cardiology|endocrinology	stroke|angina pectoris|myocardial infarction|hyperlipidemia
atovaquone	Launched	mitochondrial electron transport inhibitor		infectious disease	pneumonia
ATPA	Preclinical	glutamate receptor agonist	GRIK1		
atractylenolide-i	Preclinical	JAK inhibitor			
atracurium	Launched	acetylcholine receptor antagonist		critical care|neurology/psychiatry	endotracheal intubation|muscle relaxant
atrasentan	Phase 3	endothelin receptor antagonist	EDNRA		
atropine	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3	ophthalmology	cycloplegia|mydriasis|amblyopia
atropine-oxide	Preclinical	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5		
atuveciclib	Phase 1	CDK9 inhibitor			
AT13148	Phase 1	protein kinase inhibitor	AKT1|AKT2|AKT3|ROCK1|ROCK2|SGK3		
AT13387	Phase 2	HSP inhibitor	HSP90AA1		
AT7867	Preclinical	AKT inhibitor	AKT2|GSK3B|PKIA|PRKACA		
auranofin	Launched	NFkB pathway inhibitor	IKBKB|PRDX5|TRPA1	rheumatology	rheumatoid arthritis
aurora-a-inhibitor-i	Preclinical	Aurora kinase inhibitor	AURKA		
aurothioglucose	Launched	PKC inhibitor	PRKCI	rheumatology	rheumatoid arthritis
AUT-1	Preclinical	potassium channel activator			
autotaxin-modulator-1	Preclinical	autotaxin inhibitor	ENPP2		
AV-412	Phase 1	protein tyrosine kinase inhibitor	EGFR|ERBB2		
AV-608	Phase 2	tachykinin antagonist	TACR1		
avacopan	Phase 2	complement inhibitor			
avadomide	Phase 2	antitumor agent			
avagacestat	Phase 2	gamma secretase inhibitor	PSEN1		
avanafil	Launched	phosphodiesterase inhibitor	PDE5A	urology	erectile dysfunction
avapritinib	Launched	KIT inhibitor			
avasimibe	Phase 3	ACAT inhibitor	CES1		
avatrombopag	Launched	thrombopoietin receptor agonist	MPL	hematology	thrombocytopenia
AVE-0991	Preclinical	angiotensin receptor agonist	MRGPRX1		
AVE-3085	Preclinical	nitric oxide synthase stimulant			
AVex-73	Preclinical	sigma receptor agonist			
avibactam	Launched	beta lactamase inhibitor		infectious disease	intra-abdominal infections|urinary tract infections|pyelonephritis
avitinib	Phase 2	EGFR inhibitor			
AVL-292	Phase 2	Bruton's tyrosine kinase (BTK) inhibitor	BTK|YES1		
AVN-492	Preclinical	serotonin receptor antagonist			
AVN-944	Phase 2	inosine monophosphate dehydrogenase inhibitor	IMPDH1|IMPDH2		
avobenzone	Launched	topical sunscreen agent		dermatology	cosmetic|sunscreen lotion
avoralstat	Phase 3	kallikrein inhibitor			
avridine	Preclinical	immunostimulant			
AX-024	Preclinical	cytokine production inhibitor			
axitinib	Launched	PDGFR tyrosine kinase receptor inhibitor|VEGFR inhibitor	CSF1|FLT1|FLT4|KDR|PLK4	oncology	renal cell carcinoma (RCC)
AY-9944	Preclinical	hedgehog pathway modulator			
AZ-10417808	Preclinical	caspase inhibitor	CASP3		
AZ-10606120	Preclinical	purinergic receptor antagonist	P2RX7		
AZ-12080282	Preclinical	hedgehog pathway inhibitor	DHH		
AZ-628	Preclinical	RAF inhibitor	BRAF|RAF1		
AZ-7371	Preclinical	antibacterial 			
azacitidine	Launched	DNA methyltransferase inhibitor	DNMT1|DNMT3A	hematologic malignancy|hematology	myelodysplastic diseases (MDS)|anemia|chronic myelomonocytic leukemia (CMMoL)
azacyclonol	Preclinical	histamine receptor antagonist	HRH1		
azaguanine-8	Preclinical	purine antagonist	PNP		
azalomycin-B	Preclinical	bacterial 50S ribosomal subunit inhibitor			
azaperone	Launched	dopamine receptor antagonist	DRD2|DRD3	neurology/psychiatry	sedative
azapropazone	Withdrawn	cyclooxygenase inhibitor	PTGS2		
azaserine	Preclinical	purine antagonist			
azasetron	Launched	serotonin receptor antagonist	HTR3A|HTR3B	infectious disease	genitial herpes
azatadine	Launched	histamine receptor antagonist	HRH1	allergy	allergic rhinitis
azathioprine	Launched	dehydrogenase inhibitor	HPRT1|IMPDH1|PPAT	transplant|rheumatology	renal homotransplantation|rheumatoid arthritis
AZD0156	Phase 1	ATM kinase inhibitor			
AZD1080	Phase 1	glycogen synthase kinase inhibitor	GSK3A|GSK3B		
AZD1208	Phase 1	Pim kinase inhibitor	PIM1|PIM2|PIM3		
AZD1283	Preclinical	purinergic receptor antagonist	P2RY12		
AZD1390	Phase 1	ATM kinase inhibitor			
AZD1446	Phase 2	acetylcholine receptor agonist	CHRNA4|CHRNB2		
AZD1480	Phase 1	JAK inhibitor	JAK1|JAK2|JAK3		
AZD1981	Phase 2	CRTH receptor antagonist	PTGDR2		
AZD2014	Phase 2	mTOR inhibitor	MTOR		
AZD2461	Phase 1	PARP inhibitor			
AZD2858	Preclinical	glycogen synthase kinase inhibitor	GSK3B		
AZD3264	Preclinical	IKK inhibitor	IKBKB		
AZD3463	Preclinical	ALK tyrosine kinase receptor inhibitor|insulin growth factor receptor inhibitor	ALK|IGF1R		
AZD3514	Phase 1	androgen receptor modulator	AR		
AZD3759	Phase 2/Phase 3	EGFR inhibitor	EGFR		
AZD3839	Phase 1	beta-secretase inhibitor	BACE1		
AZD3965	Phase 1	monocarboxylate transporter inhibitor	SLC16A1		
AZD3988	Preclinical	diacylglycerol kinase inhibitor	DGAT1		
AZD4282	Phase 1	glutamate receptor antagonist	AGXT|AGXT2|ALAS1|ALAS2|BAAT|GARS|GATM|GCAT|GCSH|GLDC|GLRA1|GLRA2|GLRA3|GLRB|GLYAT|GLYATL1|GLYATL2|GNMT|GPR18|GPRC6A|GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|GRIN3B|GSS|PIPOX|SHMT1|SHMT2|SLC32A1|SLC36A1|SLC6A5|SLC6A9		
AZD4547	Phase 2/Phase 3	FGFR inhibitor	FGFR1|FGFR2|FGFR3|FGFR4|IGF1R|KDR		
AZD4573	Phase 1	CDK9 inhibitor			
AZD4635	Phase 1/Phase 2	adenosine receptor antagonist			
AZD5069	Phase 2	CC chemokine receptor antagonist	CXCR2		
AZD5153	Phase 1	bromodomain inhibitor			
AZD5363	Phase 3	AKT inhibitor	AKT1|AKT2|AKT3		
AZD5438	Phase 1	CDK inhibitor	KCNH2		
AZD5582	Preclinical	XIAP inhibitor	BIRC2|BIRC3|XIAP		
AZD5991	Phase 1	MCL1 inhibitor			
AZD6482	Phase 1	PI3K inhibitor	PIK3CA|PIK3CB|PIK3CD|PIK3CG		
AZD6738	Phase 2	ATR kinase inhibitor	ATR		
AZD6765	Phase 2	glutamate receptor antagonist	GRIN1		
AZD7545	Phase 1	pyruvate dehydrogenase kinase inhibitor	PDK1		
AZD7594	Phase 2	glucocorticoid receptor modulator			
AZD7687	Phase 1	diacylglycerol O acyltransferase inhibitor	DGAT1		
AZD7762	Phase 1	CHK inhibitor	CHEK1|CHEK2		
AZD7986	Phase 1	dipeptidyl peptidase inhibitor			
AZD8055	Phase 1	mTOR inhibitor	MTOR		
AZD8186	Phase 1	PI3K inhibitor	PIK3CB|PIK3CD		
AZD8330	Phase 1	MEK inhibitor	MAP3K1		
AZD8797	Preclinical	CC chemokine receptor antagonist			
AZD8835	Phase 1	PI3K inhibitor	PIK3CA|PIK3CD		
AZD8931	Phase 2	EGFR inhibitor	EGFR|ERBB2|ERBB3		
AZD9056	Phase 2	purinergic receptor antagonist			
AZD9272	Preclinical	glutamate receptor antagonist	GRM5		
AZD9496	Phase 1	estrogen receptor agonist	ESR1		
AZD9668	Phase 2	elastase inhibitor	ELANE		
azelaic-acid	Launched	tyrosinase inhibitor	AKR1D1|SRD5A2|TYR	dermatology	rosacea
azelastine	Launched	histamine receptor antagonist	HRH1	ophthalmology	conjunctivitis
azeliragon	Phase 3	RAGE receptor antagonist	AGER		
azelnidipine	Launched	calcium channel blocker	CACNA1C	cardiology	hypertension
azilsartan	Launched	angiotensin receptor antagonist	AGTR1|AGTR2	cardiology	hypertension
azilsartan-medoxomil	Launched	angiotensin receptor antagonist	AGTR1|AGTR2	cardiology	hypertension
azimilide	Phase 3	potassium channel blocker	KCNA5		
azithromycin	Launched	bacterial 50S ribosomal subunit inhibitor	MLNR	infectious disease	pelvic inflammatory disease|pneumonia
azlocillin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-positive bacterial infections|gram-negative bacterial infections
AZM-475271	Preclinical	SRC inhibitor	SRC		
azodicarbonamide	Phase 2	DNA synthesis inhibitor			
azomycin-(2-nitroimidazole)	Preclinical	protein synthesis inhibitor			
azosemide	Launched	electrolyte reabsorption inhibitor	SLC12A1|SLC12A2	cardiology	edema
aztreonam	Launched	bacterial cell wall synthesis inhibitor		infectious disease	urinary tract infections|respiratory tract infections|bacterial septicemia|skin infections|intra-abdominal infections|gynecologic infections
AZ191	Preclinical	DYRK inhibitor	DYRK1B		
AZ20	Preclinical	ATR kinase inhibitor	ATR|MTOR		
AZ3146	Preclinical	monopolar spindle 1 kinase inhibitor			
AZ505	Preclinical	histone lysine methyltransferase inhibitor	SMYD2		
AZ5104	Preclinical	EGFR inhibitor	EGFR		
AZ7550	Phase 1	insulin growth factor receptor inhibitor			
AZ960	Preclinical	JAK inhibitor	JAK2		
A0001	Phase 2				
A12B4C3	Preclinical	polynucleotide kinase/phosphatase inhibitor	PNKP		
A205804	Preclinical	ICAM1 expression inhibitor	ICAM1|SELE		
A61603	Preclinical	adrenergic receptor agonist	ADRA1A		
A66	Preclinical	PI3K inhibitor	PIK3CA		
A740003	Preclinical	purinergic receptor antagonist	P2RX7		
A77636	Preclinical	dopamine receptor agonist	CALY		
A922500	Preclinical	diacylglycerol O acyltransferase inhibitor	DGAT1		
bacampicillin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-positive bacterial infections|gram-negative bacterial infections
bacitracin	Launched	bacterial cell wall synthesis inhibitor	IDE	infectious disease	first-aid antibiotic
bacitracin-zinc	Launched	bacterial cell wall synthesis inhibitor		infectious disease	first-aid antibiotic
baclofen	Launched	benzodiazepine receptor agonist	GABBR1|GABBR2|KCTD12|KCTD16|KCTD8	neurology/psychiatry	multiple sclerosis|spasms
BADGE	Preclinical	PPAR receptor antagonist	PPARG		
bafetinib	Phase 2	Bcr-Abl kinase inhibitor|LYN tyrosine kinase inhibitor	ABL1|BCR|LYN		
bafilomycin-a1	Preclinical	ATPase inhibitor			
BAG-956	Preclinical	phosphoinositide dependent kinase inhibitor	PIK3CG		
baicalein	Preclinical	lipoxygenase inhibitor	ALOX5|GLO1|PREP|SELL|SELP|TNF|XDH		
baicalin	Launched	beta glucuronidase inhibitor	PREP	neurology/psychiatry	anxiety
bakuchiol	Phase 2	DNA polymerase inhibitor	HIF1A		
balaglitazone	Phase 3	insulin sensitizer|PPAR receptor partial agonist	PPARG		
balapiravir	Phase 2	RNA polymerase inhibitor			
balicatib	Phase 2	cathepsin inhibitor	CTSK		
balofloxacin	Launched	bacterial DNA gyrase inhibitor		infectious disease	gram-negative bacterial infections
baloxavir	Phase 3	endonuclease inhibitor			
baloxavir-marboxil	Launched	endonuclease inhibitor		infectious disease	influenza A virus infection
balsalazide	Launched	cyclooxygenase inhibitor	ALOX5|PPARG|PTGS1|PTGS2	gastroenterology	ulcerative colitis
bamaquimast	Preclinical	proton pump inhibitor			
bambuterol	Launched	adrenergic receptor agonist	ADRB2|BCHE	pulmonary	asthma
BAM7	Preclinical	BAX activator	BAX		
BAN-ORL-24	Preclinical	nociceptin/orphanin FQ receptor antagonist	OPRL1		
banoxantrone	Phase 1/Phase 2	topoisomerase inhibitor	TOP2A		
barasertib	Phase 2/Phase 3	Aurora kinase inhibitor	AURKA|AURKB		
barasertib-HQPA	Phase 2/Phase 3	Aurora kinase inhibitor	AURKB		
bardoxolone	Phase 1	nuclear factor erythroid derived|like (NRF2) activator	NOS2|PPARG		
bardoxolone-methyl	Phase 3	nuclear factor erythroid derived|like (NRF2) activator	PPARG|STAT3		
baricitinib	Launched	JAK inhibitor	JAK1|JAK2	rheumatology	rheumatoid arthritis
barium-6-O-phosphonato-D-glucose	Preclinical				
barnidipine	Launched	calcium channel blocker		cardiology	hypertension
basic-fuchsin	Preclinical				
basimglurant	Phase 2	glutamate receptor antagonist	GRM5		
basmisanil	Phase 2	GABA receptor inverse agonist			
batefenterol	Phase 2	acetylcholine receptor antagonist|adrenergic receptor agonist			
batimastat	Phase 3	matrix metalloprotease inhibitor	ADAM28|ADAMTS5|MMP12|MMP16|MMP2|MMP8		
bavisant	Phase 2	histamine receptor antagonist	HRH3		
BAX-channel-blocker	Preclinical	cytochrome C release inhibitor	BAX		
BAY-K-8644-(+/-)	Preclinical	L-type calcium channel blocker			
BAY-K-8644-(s)-(-)	Preclinical	L-type calcium channel activator	CACNA1C		
BAY-W-9798	Phase 2	antioxidant			
BAY-11-7082	Preclinical	NFkB pathway inhibitor	RELA		
BAY-11-7085	Preclinical	NFkB pathway inhibitor	NFKBIA		
BAY-1251152	Phase 1	CDK9 inhibitor			
BAY-1436032	Phase 1	isocitrate dehydrogenase inhibitor			
BAY-1895344	Phase 1	ATR kinase inhibitor			
BAY-2402234	Phase 1	dihydroorotate dehydrogenase inhibitor			
BAY-41-2272	Preclinical	guanylyl cyclase activator	GUCY1A3|GUCY1B3		
BAY-60-6583	Preclinical	adenosine receptor agonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
BAY-60-7550	Preclinical	phosphodiesterase inhibitor	PDE2A		
BAY-61-3606	Preclinical	SYK inhibitor	SYK		
BAY-8002	Preclinical	monocarboxylate transporter inhibitor			
BAY-85-8050	Phase 1				
BAY-87-2243	Phase 1	hypoxia inducible factor inhibitor	HIF1A		
BAY1125976	Phase 1	AKT inhibitor			
BAY1217389	Phase 1	kinase inhibitor			
bazedoxifene	Launched	selective estrogen receptor modulator (SERM)	ESR1|ESR2	orthopedics|endocrinology	osteoporosis|menopause
BAZ2-ICR	Preclinical	bromodomain inhibitor	ZNF215		
BC-11	Preclinical	urokinase inhibitor	PLAU		
BCI-540	Phase 2	glutamate receptor agonist			
BCTC	Preclinical	TRPV antagonist	TRPV1		
BCX-1470	Phase 1	complement inhibitor|serine protease inhibitor	CFD		
BD-1008	Preclinical	sigma receptor antagonist			
BD-1047	Preclinical	adrenergic receptor antagonist	SIGMAR1		
BD-1063	Preclinical	sigma receptor antagonist	SIGMAR1		
BE-2254	Phase 2	adrenergic receptor antagonist	ADRA1A		
BEBT-908	Preclinical	PI3K inhibitor			
beclabuvir	Phase 2	antiviral			
beclamide	Launched	anticonvulsant		neurology/psychiatry	sedative|seizures
beclomethasone	Launched	glucocorticoid receptor agonist	NR3C1|SERPINA6	allergy	allergic rhinitis
beclomethasone-dipropionate	Launched	glucocorticoid receptor agonist	GPR97|NR3C1	allergy	allergic rhinitis
bedaquiline	Launched	ATPase inhibitor		infectious disease	tuberculosis
befuraline	Phase 2				
begacestat	Phase 1	gamma secretase inhibitor	PSEN1		
bekanamycin	Launched	bacterial 30S ribosomal subunit inhibitor		infectious disease	gram-negative bacterial infections
belinostat	Launched	HDAC inhibitor	HDAC1|HDAC10|HDAC11|HDAC2|HDAC3|HDAC4|HDAC5|HDAC6|HDAC7|HDAC8|HDAC9	hematologic malignancy	peripheral T-cell lymphoma (PTCL)
belizatinib	Preclinical	receptor tyrosine protein kinase inhibitor			
belotecan	Phase 3	topoisomerase inhibitor			
bemegride	Launched	chemoreceptor agonist	GABRA1	critical care	poison antidote
bemesetron	Phase 3	serotonin receptor antagonist	HTR3A|HTR3B		
bemotrizinol	Launched			dermatology	sunscreen lotion
bempedoic-acid	Launched	AMPK inhibitor	ACLY		
benactyzine	Preclinical	butyrylcholinesterase inhibitor			
benaxibine	Phase 1				
benazepril	Launched	angiotensin converting enzyme inhibitor	ACE	cardiology	hypertension
bendamustine	Launched	DNA inhibitor		hematologic malignancy	chronic lymphocytic leukemia (CLL)|non-Hodgkin lymphoma (NHL)
bendazac	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	neurology/psychiatry|rheumatology	muscle pain|joint pain
bendazol	Launched	nitric oxide synthase stimulant			
bendroflumethiazide	Launched	sodium/potassium/chloride transporter inhibitor	SLC12A1|SLC12A3	cardiology	hypertension
benethamine	Preclinical				
benfluorex	Withdrawn	gluconeogenesis inhibitor	HMGCR		
benfluralin	Phase 3		CYP1A1|CYP1A2|CYP2B6|CYP3A4|ESR1|MMP1|SULT2A1|UGT1A1		
benfotiamine	Launched	antioxidant	AGER	rheumatology	lumbago
benidipine	Launched	calcium channel blocker	CACNA1C|CACNA1G	cardiology	hypertension
benperidol	Launched	dopamine receptor antagonist	DRD2	neurology/psychiatry	schizophrenia
benproperine	Launched	antitussive	SCN5A	pulmonary	cough suppressant
benserazide	Launched	DOPA decarboxylase inhibitor	DDC	neurology/psychiatry	Parkinson's Disease
bentiromide	Launched		HPN	gastroenterology	pancreas diagnostic agent
benurestat	Phase 1	urease inhibitor			
benzalkonium	Launched	cationic surfactant		dermatology	abrasions|superficial cuts
benzamil	Phase 2	sodium channel blocker	ASIC1|PKD2L1|SCNN1A|SCNN1B|SCNN1D|SCNN1G|SLC8A1		
benzbromarone	Launched	chloride channel blocker	ABCC1	rheumatology	gout
"benzenemethanol,-2,5-dimethyl-[[(1-methylethyl)amino]methyl]"	Preclinical				
benzethonium	Launched	sodium channel blocker	SCN10A	infectious disease	first-aid antiseptic
benznidazole	Launched	DNA synthesis inhibitor		infectious disease	Chagas disease
benzo[d]thiazole-2(3H)-thione	Phase 1				
benzocaine	Launched	sodium channel blocker	SCN10A	infectious disease	first-aid antiseptic
benzoclidine	Preclinical				
benzofenac	Phase 1				
benzoic-acid	Launched	food preservative	DAO|HRSP12|PRDX5|RAB9A	infectious disease	tinea pedis
benzoin	Preclinical		CES1		
benzonatate	Launched	local anesthetic	SCN5A	pulmonary	cough suppressant
benzoquinonium-dibromide	Preclinical	cholinergic receptor antagonist	CHRNA1		
benzotript	Phase 1	CCK receptor antagonist	CCKAR|CCKBR		
benzoxiquine	Preclinical	antiinfective drug			
benzoyl-peroxide	Launched	oxidizing agent		dermatology	acne vulgaris (AV)
benzoylpas	Preclinical				
benzthiazide	Launched	carbonic anhydrase inhibitor	CA2	cardiology	hypertension|edema
benztropine-mesylate	Launched	acetylcholine receptor antagonist	CHRM1|HRH1|SLC6A3	neurology/psychiatry	extrapyramidal symptoms (EPS)|Parkinson's Disease
benzydamine	Launched	prostanoid receptor antagonist		dental|otolaryngology	mouth inflammation|throat inflammation
benzyl-alcohol	Launched	local anesthetic		infectious disease	virus herpes simplex (HSV)
benzyl-benzoate	Launched	lipase inhibitor	LIPE	allergy	sweet itch
benzyl-isothiocyanate	Preclinical	methylazoxymethanol acetate inhibitor			
benzyldimethylhexadecylammonium	Preclinical	cationic surfactant			
benzyldimethyloctylammonium	Preclinical				
benzylpenicillin	Launched	penicillin binding protein inhibitor		infectious disease	celluitis|meningitis|endocarditis|syphilis|pneumonia|bacterial septicemia
bephenium-hydroxynaphthoate	Launched	anthelmintic agent		infectious disease	ascariasis
bepotastine	Launched	histamine receptor antagonist	HRH1	ophthalmology	conjunctivitis
bepridil	Launched	calcium channel blocker	KCNQ4	cardiology	angina pectoris
berberine	Launched	LDL receptor activator	LDLR		
bergapten	Phase 3				
bergenin	Preclinical	interleukin inhibitor	IL1B|TNF		
besifloxacin	Launched	bacterial DNA gyrase inhibitor		ophthalmology	conjunctivitis
BET-BAY-002	Preclinical	bromodomain inhibitor			
beta-amyloid-synthesis-inhibitor	Preclinical	beta amyloid synthesis inhibitor	APP		
beta-carotene	Launched				
beta-CCB	Launched	benzodiazepine receptor ligand	GABRA1|GABRG2		
beta-elemene	Launched	apoptosis stimulant	MMP2|MMP9		
beta-funaltrexamine	Preclinical	opioid receptor antagonist	OPRD1|OPRK1|OPRM1		
beta-glycerophosphoric-acid	Preclinical				
beta-hydroxy-beta-methylbutyrate	Launched	protein synthesis stimulant	MTOR		
beta-hydroxybutyrate	Phase 1		HCAR2		
beta-lapachone	Phase 2	topoisomerase inhibitor	TOP1		
beta-naphthol	Preclinical				
betahistine	Launched	histamine receptor agonist|histamine receptor antagonist	HRH1|HRH3	neurology/psychiatry	Meniere's disease
betaine	Launched	nitric oxide donor		metabolism	homocystinuria
betamethasone	Launched	glucocorticoid receptor agonist	NR3C1	dermatology	corticosteroid-responsive dermatoses
betamethasone-acetate	Launched	glucocorticoid receptor agonist	NR3C1	dermatology	corticosteroid-responsive dermatoses
betamethasone-butyrate-propionate	Launched			rheumatology	rheumatoid arthritis
betamethasone-dipropionate	Launched	anti-inflammatory agent	NR3C1	dermatology	corticosteroid-responsive dermatoses
betamethasone-phosphate	Launched			rheumatology	rheumatoid arthritis
betamethasone-valerate	Launched	glucocorticoid receptor agonist	NR3C1	dermatology	corticosteroid-responsive dermatoses
betamipron	Launched	panipenem uptake inhibitor		nephrology	renal toxicity
betaxolol	Launched	adrenergic receptor antagonist	ADRB1|ADRB2	ophthalmology	intraocular pressure|glaucoma|ocular hypertension
betazole	Launched	histamine receptor agonist	HRH2	gastroenterology	gastric hypersecretion diagnostic
bethanechol	Launched	acetylcholine receptor agonist	CHRM1|CHRM2|CHRM3|CHRM4	urology	urinary retention
BETP	Preclinical	GLP receptor positive allosteric modulator	GLP1R		
betrixaban	Launched	coagulation factor inhibitor	KCNH2	hematology	deep vein thrombosis (DVT)
betulinic-acid	Phase 1/Phase 2	apoptosis stimulant|NFkB pathway inhibitor	GPBAR1		
bevantolol	Launched	adrenergic receptor antagonist		cardiology	angina pectoris|hypertension
bevenopran	Phase 1	opioid receptor antagonist			
bevirimat-dimeglumine	Phase 2	HIV capsid assembly inhibitor			
bexagliflozin	Phase 3	solute carrier family member inhibitor			
bexarotene	Launched	retinoid receptor agonist	RXRA|RXRB|RXRG	hematologic malignancy	cutaneous T-cell lymphoma (CTCL)
bezafibrate	Launched	PPAR receptor agonist	PPARA|PPARD|PPARG	cardiology	cholesterol
BFH772	Phase 2	VEGFR inhibitor			
BGP-15	Phase 2	PARP inhibitor			
BGT226	Phase 1/Phase 2	PI3K inhibitor	MTOR|PIK3CA|PIK3CB|PIK3CG		
BHQ	Preclinical	ATPase inhibitor	ATP2A1		
BI-D1870	Preclinical	ribosomal protein inhibitor	RPS6KA1|RPS6KA2|RPS6KA3|RPS6KA6		
BI-224436	Phase 1	HIV integrase inhibitor			
BI-2536	Phase 2	PLK inhibitor	BRD4|PLK1|PLK2|PLK3		
BI-409306	Phase 1	phosphodiesterase inhibitor			
BI-78D3	Preclinical	JNK inhibitor	MAPK8		
BI-847325	Phase 1	Aurora kinase inhibitor|MEK inhibitor	AURKA|AURKB|AURKC|MAP2K1|MAP2K2		
BIA-10-2474	Preclinical	Fatty acid hydrolase inhibitor			
biapenem	Launched	bacterial cell wall synthesis inhibitor		infectious disease	bacterial septicemia|pneumonia|urinary tract infections
BIBN4096	Phase 2	calcitonin antagonist	CALCA|CALCRL|RAMP1		
BIBR-1532	Preclinical	telomerase inhibitor	TERT		
BIBU-1361	Preclinical	EGFR inhibitor	EGFR		
BIBX-1382	Phase 1	EGFR inhibitor	EGFR|ERBB2		
bicalutamide	Launched	androgen receptor antagonist	AR	oncology	prostate cancer
bicifadine	Phase 3	dopamine reuptake inhibitor|serotonin receptor antagonist			
bictegravir	Launched	HIV integrase inhibitor		infectious disease	human immunodeficiency virus (HIV-1)
bicuculline-(+)	Preclinical	GABA receptor antagonist	GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|KCNN1		
bicuculline-methochloride-(-)	Preclinical	GABA receptor antagonist			
bicyclol	Launched	NFkB pathway inhibitor	HSPA1A|HSPB1	infectious disease	hepatitis B|hepatitis C
bifemelane	Launched	acetylcholine release enhancer	MAOA|MAOB	ophthalmology|neurology/psychiatry	glaucoma|senile dementia
bifendate	Launched			infectious disease	hepatitis B|hepatitis C
bifonazole	Launched	sterol demethylase inhibitor		infectious disease	tinea pedis|tinea cruris
BIIB021	Phase 2	HSP inhibitor	HSP90AA1		
bilastine	Launched	histamine receptor antagonist	HRH1	ophthalmology	conjunctivitis
bilobalide	Preclinical	GABA receptor modulator	GLRA1|GLRA2|GLRB|HTR3A|HTR3B		
bimatoprost	Launched	prostanoid receptor agonist	AKR1C3|PTGER1|PTGER3|PTGFR	ophthalmology	intraocular pressure|glaucoma|ocular hypertension
BIMU-8	Preclinical	serotonin receptor agonist	HTR4		
BINA	Preclinical	glutamate receptor positive allosteric modulator	GRM2		
bindarit	Phase 2	NFkB pathway inhibitor	CCL2|CCL7|CCL8		
binimetinib	Launched	MEK inhibitor	MAP2K1|MAP2K2	oncology	melanoma
BIO-1211	Phase 2	integrin antagonist	ITGA4|ITGB1		
BIO-5192	Preclinical	integrin inhibitor	ITGA4|ITGB1		
biotin	Launched	vitamin B	ACACA|ACACB|HLCS|MCCC1|MCCC2|PC|PCCA|PCCB|SLC5A6		
bipenamol	Phase 2	dipeptidyl peptidase inhibitor	CTSC		
biperiden	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5	neurology/psychiatry	Parkinson's Disease
birinapant	Phase 2	XIAP inhibitor	BIRC2|XIAP		
BIRT-377	Preclinical	lymphocyte function-associated antigen negative modulator	ICAM1		
bis(maltolato)oxovanadium(IV)	Phase 2	tyrosine phosphatase inhibitor	PTPN1		
bisacodyl	Launched	laxative		gastroenterology	constipation
bisantrene	Phase 2	topoisomerase inhibitor			
bisindolylmaleimide-IX	Preclinical	PKC inhibitor	AKT1|GSK3B|LCK|MAPK1|MAPK11|MAPK12|MAPK14|MAPK8|PRKCA|ROCK1|RPS6KB1|SIRT1		
bismuth(III)-trifluoromethanesulfonate	Preclinical	direct substitution catalyst			
bismuth-oxalate	Preclinical				
bismuth-subcitrate-potassium	Launched			gastroenterology	duodenal ulcer disease
bismuth-subgallate	Launched	nitric oxide synthase inhibitor	NOS1	gastroenterology	internal deoderant
bismuth-subsalicylate	Launched	antacid		gastroenterology	diarrhea
bisoctrizole	Phase 2				
bisoprolol	Launched	adrenergic receptor antagonist	ADRB1	cardiology	hypertension
bisphenol-A	Phase 1	synthetic estrogen	AR|ESR1|ESR2|ESRRG|PPARG		
bithionol	Withdrawn	autotaxin inhibitor	ESR1|ESR2|MCL1		
bitopertin	Phase 3	glycine transporter inhibitor	SLC6A5|SLC6A9		
bitoscanate	Preclinical	anthelmintic agent			
bivalirudin	Launched	thrombin inhibitor	F2	cardiology	angina pectoris
BIX-01294	Preclinical	histone lysine methyltransferase inhibitor	EHMT1|EHMT2		
BIX-02188	Preclinical	MEK inhibitor	MAP2K5		
BIX-02189	Preclinical	MEK inhibitor	MAP2K5|MAPK7		
BL-5583	Preclinical	hypercalcaemic agent			
blebbistatin-(+/-)	Preclinical	ATPase inhibitor	MYH14|MYH2		
blebbistatin-(-)	Preclinical	ATPase inhibitor			
bleomycetin	Launched	EGFR expression inhibitor			
bleomycin	Launched	DNA synthesis inhibitor		hematologic malignancy|pulmonary|oncology	non-Hodgkin lymphoma (NHL)|Hodgkin's lymphoma|pleural effusion|testicular carcinoma|squamous cell carcinoma
blonanserin	Launched	dopamine receptor antagonist|serotonin receptor antagonist	DRD2|HTR2A	neurology/psychiatry	schizophrenia
BLU9931	Preclinical	FGFR inhibitor	FGFR4		
BLZ945	Phase 1/Phase 2	CSF1R inhibitor			
BML-190	Preclinical	cannabinoid receptor inverse agonist	CNR2		
BML-284	Preclinical	WNT agonist			
BMS-CCR2-22	Preclinical	CC chemokine receptor antagonist	CCR2		
BMS-182874	Phase 2	endothelin receptor antagonist	EDNRA		
BMS-191011	Preclinical	potassium channel activator	KCNMA1		
BMS-191095	Phase 1	KATP activator|potassium channel agonist			
BMS-207940	Preclinical	endothelin receptor antagonist			
BMS-214662	Phase 1	farnesyltransferase inhibitor			
BMS-265246	Preclinical	CDK inhibitor	CDK1|CDK2		
BMS-299897	Phase 1	gamma secretase inhibitor			
BMS-309403	Preclinical	fatty acid binding protein inhibitor	FABP4		
BMS-345541	Preclinical	IKK inhibitor	CHUK|IKBKB		
BMS-387032	Phase 1	CDK inhibitor|cell cycle inhibitor|MCL1 inhibitor	CDK2|CDK7|CDK9		
BMS-470539	Preclinical	melanocortin receptor agonist	MC1R		
BMS-536924	Preclinical	IGF-1 inhibitor	AKT1|CCNE1|CDK2|CYP3A4|ERBB2|IGF1R|KDR|LCK|MAPK1|MET|PDGFRA|PDGFRB		
BMS-566419	Preclinical	inosine monophosphate dehydrogenase inhibitor	IMPDH1|IMPDH2		
BMS-582949	Phase 2	p38 MAPK inhibitor			
BMS-587101	Phase 2	integrin antagonist	ITGAL|ITGB2		
BMS-599626	Phase 1	EGFR inhibitor|protein tyrosine kinase inhibitor	EGFR|ERBB2|ERBB4		
BMS-626529	Phase 3	HIV attachment inhibitor			
BMS-626531	Phase 1	p38 MAPK inhibitor			
BMS-649	Preclinical	retinoid receptor agonist	RXRA		
BMS-688521	Preclinical	ICAM1 antagonist|leukocyte function-associated antigen receptor antagonist	ICAM1		
BMS-690514	Phase 2	EGFR inhibitor|VEGFR inhibitor	EGFR|ERBB2|FLT3|KDR		
BMS-707035	Phase 2	HIV integrase inhibitor			
BMS-754807	Phase 2	IGF-1 inhibitor	AKT1|IGF1R		
BMS-770767	Phase 2	11-beta-HSD1 inhibitor			
BMS-777607	Phase 1/Phase 2	AXL kinase inhibitor|c-Met inhibitor|FLT3 inhibitor|hepatocyte growth factor receptor inhibitor|macrophage migration inhibiting factor inhibitor|tyrosine kinase inhibitor	AXL|MERTK|MET|MST1R|TYRO3		
BMS-779788	Phase 1	LXR agonist			
BMS-806	Phase 1	HIV attachment inhibitor			
BMS-813160	Phase 2	CC chemokine receptor antagonist			
BMS-817378	Phase 1	c-Met inhibitor|VEGFR inhibitor	KDR|MET		
BMS-833923	Phase 2	smoothened receptor antagonist	SMO		
BMS-863233	Phase 1/Phase 2	CDC inhibitor	CDC7|PIM1		
BMS-906024	Phase 1	gamma secretase inhibitor			
BMS-911543	Phase 1/Phase 2	JAK inhibitor			
BMS-935177	Preclinical	Bruton's tyrosine kinase (BTK) inhibitor			
BMS-983970	Phase 1	notch signaling inhibitor			
BMS-986020	Phase 2	lysophosphatidic acid receptor antagonist	LPAR1		
BMS-986142	Phase 2	Bruton's tyrosine kinase (BTK) inhibitor			
BMS-986158	Phase 1/Phase 2	bromodomain inhibitor			
BMS-986195	Phase 1	Bruton's tyrosine kinase (BTK) inhibitor			
BMS-986205	Phase 3	"indoleamine 2,3-dioxygenase inhibitor"			
BMY-14802	Phase 2	sigma receptor antagonist	HTR1A		
BMY-45778	Preclinical	IP1 prostacyclin receptor agonist	PTGIR		
BMY-7378	Preclinical	adrenergic receptor antagonist|serotonin receptor antagonist	ADRA1A|ADRA1B|ADRA1D|HTR1A		
BNC105	Phase 2	tubulin polymerization inhibitor			
BNTX	Preclinical	opioid receptor antagonist	OPRD1|OPRK1|OPRM1		
boceprevir	Launched	HCV inhibitor	CMA1|CTSA|CTSF|CTSK|CTSL|CTSS	infectious disease	hepatitis C
bonaphthone	Phase 3				
bopindolol	Launched	adrenergic receptor antagonist		cardiology	hypertension|coronary artery disease (CAD)
bornyl-acetate	Preclinical				
boronophenylalanine	Phase 2				
bortezomib	Launched	NFkB pathway inhibitor|proteasome inhibitor	PSMA1|PSMA2|PSMA3|PSMA4|PSMA5|PSMA6|PSMA7|PSMA8|PSMB1|PSMB10|PSMB11|PSMB2|PSMB3|PSMB4|PSMB5|PSMB6|PSMB7|PSMB8|PSMB9|PSMD1|PSMD2|RELA	hematologic malignancy	multiple myeloma|mantle cell lymphoma (MCL)
BOS-172722	Phase 1	monopolar spindle 1 kinase inhibitor			
bosentan	Launched	endothelin receptor antagonist	EDNRA|EDNRB	pulmonary	pulmonary arterial hypertension (PAH)
bosutinib	Launched	Abl kinase inhibitor|Bcr-Abl kinase inhibitor|SRC inhibitor	ABL1|BCR|CAMK1D|CAMK2G|CDK2|FRK|FYN|HCK|LYN|MAP2K1|MAP2K2|MAP3K2|MAP4K5|SRC|STK10|STK24|STK4|TNK2|TXK	hematologic malignancy	chronic myeloid leukemia (CML)
BP-554	Preclinical	serotonin receptor agonist	HTR1A		
BP-897	Phase 2	dopamine receptor agonist	ADRA1A|ADRA1D|ADRA2A|DRD1|DRD2|DRD3|DRD4|HTR1A|HTR2B		
BQ-123	Phase 2	endothelin receptor antagonist	EDNRA		
BQ-788	Phase 1	endothelin receptor antagonist	EDNRB		
BQU57	Preclinical	Ras GTPase inhibitor	RALA|RALB		
BRD4770	Preclinical	histone lysine methyltransferase inhibitor	EHMT2		
BRD7389	Preclinical	ribosomal protein inhibitor	RPS6KA1|RPS6KA2|RPS6KA3		
BRD9876	Preclinical	kinesin inhibitor	KIF11		
brefeldin-A	Preclinical	protein synthesis inhibitor	ARF1|CYTH2		
bremelanotide	Launched	melanocortin receptor agonist	MC1R|MC2R|MC3R|MC4R|MC5R	neurology/psychiatry	hypoactive sexual desire disorder
brequinar	Phase 2	dihydroorotate dehydrogenase inhibitor	DHODH		
bretazenil	Phase 2	GABA benzodiazepine site receptor partial agonist	GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6		
bretylium	Launched	norepinephrine inhibitor	ATP1A1	cardiology	ventricular arrhythmias|ventricular fibrillation (VF)|ventricular tachycardia (VT)
brexpiprazole	Launched	dopamine receptor partial agonist	DRD2	neurology/psychiatry	depression|schizophrenia
briciclib	Phase 1	cyclin D inhibitor	CCND1		
brigatinib	Launched	ALK tyrosine kinase receptor inhibitor|EGFR inhibitor	ALK|EGFR	oncology	non-small cell lung cancer (NSCLC)
brilliant-green	Launched			infectious disease	antiseptic
brimonidine	Launched	adrenergic receptor agonist	ADRA2A|ADRA2B|ADRA2C	ophthalmology	intraocular pressure|glaucoma|ocular hypertension
brincidofovir	Phase 3	antiviral			
brinzolamide	Launched	carbonic anhydrase inhibitor	CA1|CA12|CA14|CA2|CA4|CA5A|CA7	ophthalmology	intraocular pressure|glaucoma|ocular hypertension
brivanib	Phase 3	FGFR inhibitor|VEGFR inhibitor	CYP3A4|FGFR1|FLT1|KCNH2|KDR		
brivanib-alaninate	Phase 3	FGFR inhibitor|VEGFR inhibitor	FGFR3		
brivudine	Launched	DNA directed DNA polymerase inhibitor		infectious disease	shingles
BRL-15572	Preclinical	serotonin receptor antagonist	HTR1A|HTR1B|HTR1D|HTR1E|HTR1F|HTR2A|HTR2B|HTR2C|HTR6		
BRL-26314	Phase 1	cholesterol inhibitor	LPL		
BRL-37344	Phase 2	adrenergic receptor agonist	ADRB1|ADRB2|ADRB3		
BRL-44408	Preclinical	adrenergic receptor antagonist	ADRA2A|ADRA2B|ADRA2C		
BRL-50481	Preclinical	phosphodiesterase inhibitor	PDE7A|PDE7B		
BRL-52537	Preclinical	opioid receptor agonist	OPRK1		
BRL-54443	Preclinical	serotonin receptor agonist	HTR1E|HTR1F		
brolitene	Launched	muscle relaxant	RYR1	rheumatology	lumbago
bromantan	Launched	dopamine reuptake inhibitor|serotonin reuptake inhibitor		neurology/psychiatry	neurasthenia
bromebric-acid	Preclinical	DNA synthesis inhibitor|purine antagonist			
bromfenac	Withdrawn	cyclooxygenase inhibitor	PTGS1|PTGS2		
bromhexine	Launched	mucolytic agent		pulmonary	chest congestion
bromindione	Phase 2	anticoagulant			
bromisoval	Preclinical	anti-inflammatory agent			
bromocriptine	Launched	dopamine receptor agonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|DRD1|DRD2|DRD3|DRD4|DRD5|HTR1A|HTR1B|HTR1D|HTR2A|HTR2B|HTR2C|HTR6|HTR7	endocrinology|neurology/psychiatry	hyperprolactinemia|Parkinson's Disease|acromegaly
bromopride	Launched	dopamine receptor antagonist	DRD2	gastroenterology	nausea|vomiting|gastroesophageal reflux disease (GERD)
bromosporine	Preclinical	bromodomain inhibitor			
bromperidol	Launched	dopamine receptor antagonist	DRD2	neurology/psychiatry	schizophrenia
brompheniramine	Launched	histamine receptor antagonist	HRH1	allergy|otolaryngology	allergic rhinitis|common cold
bronopol	Launched			obstetrics/gynecology	mastitis
bropirimine	Phase 3	interferon inducer			
broxaldine	Preclinical				
broxaterol	Phase 3	adrenergic receptor agonist	ADRB2		
broxuridine	Phase 2	antimetabolite			
broxyquinoline	Phase 1	antiprotozoal agent			
bruceantin	Phase 2	protein synthesis inhibitor			
brucine	Preclinical	glycine receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5		
BS-181	Preclinical	CDK inhibitor	CDK7		
BT-11	Phase 2	cAMP stimulant			
BTB06584	Preclinical	ATPase inhibitor	ATP5F1		
BTB1	Preclinical	mitotic kinesin inhibitor	KIF18A		
BTK-IN-1	Preclinical	Bruton's tyrosine kinase (BTK) inhibitor			
BTS	Preclinical				
BTS-54505	Withdrawn	dopamine reuptake inhibitor	SLC6A2|SLC6A3|SLC6A4		
BTS-71321	Phase 2				
BTS-72664	Phase 1	GABA receptor antagonist	GABBR1		
BTT-3033	Preclinical	integrin inhibitor	ITGA2|ITGB1		
BTZ043-racemate	Phase 1/Phase 2	DPRE1 inhibitor			
BU-224	Preclinical	imidazoline receptor ligand	MAOA|MAOB		
BU-239	Preclinical	imidazoline receptor agonist|imidazoline receptor ligand			
bucetin	Withdrawn	analgesic agent			
bucillamine	Launched	immunosuppressant		rheumatology	rheumatoid arthritis
bucladesine	Launched	adenosine receptor agonist|cAMP stimulant	PRKACA	dermatology	skin ulcer
buclizine	Launched	histamine receptor antagonist	HRH1	neurology/psychiatry	migraine headache
budesonide	Launched	glucocorticoid receptor agonist	NR3C1	gastroenterology	Crohn's disease
budipine	Launched	glutamate receptor antagonist	GRIN1	neurology/psychiatry	Parkinson's Disease
bufexamac	Withdrawn	cyclooxygenase inhibitor	HDAC10|HDAC6		
buflomedil	Launched	adrenergic receptor antagonist|calcium channel blocker	ADRA1A	cardiology	peripheral artery disease (PAD)
bumetanide	Launched	solute carrier family member inhibitor	CFTR|GPR35|SLC12A1|SLC12A2|SLC12A4|SLC12A5	cardiology	edema|congestive heart failure
bunazosin	Launched	adrenergic receptor antagonist	ADRA1A	ophthalmology	glaucoma|intraocular pressure
buparlisib	Phase 3	PI3K inhibitor	PIK3CA|PIK3CG		
buparvaquone	Launched	antiprotozoal agent		infectious disease	protozoan infection
buphenine	Launched	adrenergic receptor agonist	ADRB2	rheumatology	Raynaud's disease
bupicomide	Phase 1	adrenergic receptor antagonist	ADRB1		
bupivacaine	Launched	sodium channel blocker	KCNA5|SCN10A	neurology/psychiatry	peripheral nerve block|caudal epidural block|lumbar epidural block
bupranolol	Launched	adrenergic receptor antagonist	ADRB1|ADRB2|ADRB3	cardiology|ophthalmology	hypertension|glaucoma
bupropion	Launched	dopamine reuptake inhibitor	SLC6A2|SLC6A3	neurology/psychiatry	depression
buramate	Preclinical	antiepileptic			
buserelin	Launched	gonadotropin releasing factor hormone receptor agonist		oncology|obstetrics/gynecology	prostate cancer|endometriosis
buspirone	Launched	serotonin receptor agonist	DRD2|HTR1A	neurology/psychiatry	generalized anxiety disorder (GAD)
busulfan	Launched	DNA inhibitor		hematologic malignancy	chronic myeloid leukemia (CML)
butabindide	Preclinical	tripeptidyl peptidase inhibitor	TPP2		
butacaine	Launched	local anesthetic		neurology/psychiatry	local anesthetic
butaclamol	Phase 2	dopamine receptor antagonist	DRD1|DRD2|DRD3|DRD4|DRD5|HTR1A|HTR2A		
butalbital	Launched	GABA receptor antagonist	CHRNA4|CHRNA7|GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ|GRIA2|GRIK2	neurology/psychiatry	headache|muscle relaxant
butamben	Withdrawn	sodium channel blocker			
butaprost	Preclinical	prostaglandin receptor agonist			
butein	Preclinical	EGFR inhibitor|SRC inhibitor	ACE		
butenafine	Launched	fungal squalene epoxidase inhibitor	SQLE	infectious disease	tinea pedis|tinea cruris|tinea corporis
buthionine-sulfoximine	Phase 1	glutathione transferase inhibitor	GCLM		
butibufen	Withdrawn	cyclooxygenase inhibitor			
butoconazole	Launched	bacterial cell wall synthesis inhibitor		infectious disease	vulvovaginal candidiasis
butofilolol	Phase 2	adrenergic receptor antagonist			
butyl-paraben	Preclinical	DNA synthesis inhibitor			
butylated-hydroxyanisole	Preclinical	antioxidant			
butylated-hydroxytoluene	Phase 1	carbonic anhydrase inhibitor	CA2		
butylidenephthalide	Phase 1/Phase 2	cyclooxygenase inhibitor			
butylphthalide	Launched	potassium channel antagonist	KCNK2	neurology/psychiatry	stroke
butylscopolamine-bromide	Launched	cholinergic receptor antagonist		gastroenterology	abdominal pain
BU226	Preclinical	imidazoline receptor ligand			
BVD-523	Phase 2	MAP kinase inhibitor			
BVT-2733	Preclinical	11-beta hydroxysteroid dehydrogenase inhibitor	HSD17B1		
BVT-948	Preclinical	tyrosine phosphatase inhibitor	PTPN1|PTPN11|PTPN2		
BW-A4C	Phase 1	lipoxygenase inhibitor	ALOX5		
BW-B70C	Preclinical	lipoxygenase inhibitor	ALOX5		
BW-180C	Phase 2	opioid receptor agonist	OPRD1|OPRM1		
BW-348U87	Preclinical	antiviral			
BW-373U86	Preclinical	opioid receptor agonist	OPRD1		
BW-616U	Preclinical	monoamine oxidase inhibitor	MAOA		
BW-723C86	Preclinical	serotonin receptor agonist	HTR2A|HTR2B|HTR2C		
BX-795	Preclinical	IKK inhibitor	CDK2|CHEK1|GSK3B|KDR|PDK1|PDPK1		
BX-912	Preclinical	pyruvate dehydrogenase kinase inhibitor	CDK2|CHEK1|GSK3B|KDR|PDK1|PDPK1		
BYK-204165	Preclinical	PARP inhibitor	PARP1		
C-021	Preclinical	CC chemokine receptor antagonist	CCR4		
C-1	Preclinical	protein kinase inhibitor	PRKCA		
C-751	Preclinical				
CA-4948	Phase 1	kinase inhibitor			
cabagin	Launched			gastroenterology	dyspepsia
cabaletta	Phase 2	pharmacological chaperone			
cabazitaxel	Launched	microtubule inhibitor	TUBA1A|TUBA1B|TUBA1C|TUBA3C|TUBA3D|TUBA3E|TUBA4A|TUBB|TUBB1|TUBB2A|TUBB2B|TUBB3|TUBB4A|TUBB4B|TUBB6|TUBB8	oncology	prostate cancer
cabergoline	Launched	dopamine receptor agonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|ADRB1|ADRB2|DRD1|DRD2|DRD3|DRD4|DRD5|HTR1A|HTR1B|HTR1D|HTR2A|HTR2B|HTR2C|HTR7	endocrinology	hyperprolactinemia
cabotegravir	Phase 3	HIV integrase inhibitor			
cabozantinib	Launched	RET tyrosine kinase inhibitor|VEGFR inhibitor	KDR|MET|RET	oncology	medullary thyroid cancer (MTC)
CaCCinh-A01	Preclinical	calcium-activated chloride channel inhibitor	CLCA1		
cadazolid	Phase 3	antibacterial 			
cadralazine	Launched	adrenergic receptor antagonist		cardiology	hypertension
cafestol	Launched	pregnane X receptor agonist			
caffeic-acid	Preclinical	HIV integrase inhibitor|lipoxygenase inhibitor|nitric oxide production inhibitor|tumor necrosis factor production inhibitor	ALOX5|MIF		
caffeic-acid-phenethyl-ester	Preclinical	HIV integrase inhibitor	RELA		
caffeine	Launched	adenosine receptor antagonist|phosphodiesterase inhibitor	ADORA1|ADORA2A|ADORA2B|ADORA3|ATM|ITPR1|ITPR2|ITPR3|PDE10A|PDE11A|PDE1A|PDE1B|PDE1C|PDE2A|PDE3A|PDE3B|PDE4A|PDE4B|PDE4C|PDE4D|PDE5A|PDE6A|PDE6B|PDE6C|PDE7A|PDE7B|PDE8A|PDE8B|PDE9A|PIK3CA|PIK3CB|PIK3CD|PRKDC|RYR1|RYR2|RYR3	neurology/psychiatry	fatigue|drowsiness
calcifediol	Launched	vitamin D receptor agonist	VDR	endocrinology	hyperparathyroidism
calcipotriol	Launched	vitamin D receptor agonist	VDR	dermatology	psoriasis
calcitonin	Launched	calcitonin agonist		orthopedics	osteoporosis
calcitriol	Launched	vitamin D receptor agonist	VDR	endocrinology|orthopedics	hypocalcemia|hypoparathyroidism|osteoporosis
calcium-gluceptate	Launched				
calcium-levofolinate	Launched				
Calhex-231	Preclinical	calcium sensing receptor negative allosteric modulator	CASR		
calpeptin	Preclinical	calpain inhibitor			
camicinal	Phase 2	motilin receptor agonist	MLNR		
CaMKII-IN-1	Preclinical	calcium/calmodulin dependent protein kinase inhibitor	AKT1|CAMK2A|CAMK4|MYLK		
camobucol	Preclinical	anti-inflammatory agent			
camostat-mesilate	Launched	protease inhibitor	PRSS1	gastroenterology	pancreatitis
camphor-(+)	Phase 2				
camphor-(1R)	Phase 1	TRPV activator	TRPV1		
camptothecin	Phase 3	topoisomerase inhibitor	TOP1		
camylofine-chlorhydrate	Launched			gastroenterology	abdominal pain
canagliflozin	Launched	sodium/glucose cotransporter inhibitor	SLC5A1|SLC5A2	endocrinology	diabetes mellitus
candesartan	Launched	angiotensin receptor antagonist	AGTR1	cardiology	hypertension|congestive heart failure
candesartan-cilexetil	Launched	angiotensin receptor antagonist		cardiology	hypertension|congestive heart failure|hypertension
candicidin	Launched	fungal ergosterol inhibitor		infectious disease	vulvovaginal candidiasis
canertinib	Phase 3	EGFR inhibitor	AKT1|EGFR|ERBB2|ERBB4		
cangrelor	Launched	purinergic receptor antagonist		cardiology	myocardial infarction
canrenone	Withdrawn	mineralocorticoid receptor antagonist	NR3C2		
cantharidin	Launched	protein phosphatase inhibitor		dermatology	blisters
capadenoson	Phase 2	adenosine receptor agonist	ADORA1		
capecitabine	Launched	DNA synthesis inhibitor|thymidylate synthase inhibitor	TYMS	oncology	breast cancer|colorectal cancer
capobenic-acid	Preclinical				
capreomycin	Launched	protein synthesis inhibitor		infectious disease	tuberculosis
capromorelin	Preclinical	growth hormone secretagogue receptor agonist			
caprylic-acid	Launched				
capsaicin	Launched	TRPV agonist	CFTR|TRPV1	neurology/psychiatry|rheumatology	muscle pain|rheumatoid arthritis
capsazepine	Preclinical	TRPV agonist	TRPV1|TRPV4		
captamine	Preclinical				
captan	Phase 1				
captopril	Launched	angiotensin converting enzyme inhibitor	ACE|LTA4H|MMP2|MMP9	cardiology|endocrinology|nephrology	hypertension|congestive heart failure|myocardial infarction|diabetes mellitus|diabetic nephropathy
caracemide	Phase 2	ribonucleotide reductase inhibitor	RRM1		
caramiphen	Launched	cholinergic receptor antagonist	CHRM1|CHRM2	neurology/psychiatry	Parkinson's Disease
carazolol	Launched	adrenergic receptor antagonist	ADRB1|ADRB2|ADRB3	cardiology	angina pectoris|cardiac arrythmia|hypertension|myocardial infarction
carbachol	Launched	cholinergic receptor agonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|CHRNA2	ophthalmology	intraocular pressure
carbadox	Launched	other antibiotic		infectious disease|gastroenterology	dysentry|enteritis
carbamazepine	Launched	carboxamide antiepileptic	SCN10A|SCN11A|SCN1A|SCN2A|SCN3A|SCN4A|SCN5A|SCN7A|SCN8A|SCN9A	neurology/psychiatry	seizures
carbaril	Launched	acetylcholinesterase inhibitor			
carbarsone	Launched	antiprotozoal agent		infectious disease	amebiasis
carbazochrome	Launched			hematology	hemorrhage
carbendazim	Launched	microtubule inhibitor|tubulin polymerization inhibitor	TP53|TUBB	infectious disease	fungicide
carbenicillin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-negative bacterial infections
carbenoxolone	Launched	11-beta hydroxysteroid dehydrogenase inhibitor	GJA1|GJA10|GJA3|GJA4|GJA5|GJA8|GJA9|GJB1|GJB2|GJB3|GJB4|GJB5|GJB6|GJB7|GJC1|GJC2|GJC3|GJD2|GJD3|GJD4|GJE1|HSD11B1|PANX1|PANX2|PANX3	gastroenterology|dental	peptic ulcer disease (PUD)|mouth inflammation
carbetapentane	Launched	acetylcholine receptor antagonist	CHRM2	otolaryngology|pulmonary	common cold|nasal congestion|bronchitis
carbetocin	Launched	oxytocin receptor agonist	OXTR	hematology	hemorrhage
carbidopa	Launched	aromatic L-amino acid decarboxylase inhibitor	DDC	neurology/psychiatry	Parkinson's Disease
carbimazole	Launched	antithyroid agent	TPO	endocrinology	hyperthyroidism
carbinoxamine	Launched	histamine receptor antagonist	HRH1	allergy|ophthalmology|otolaryngology|dermatology	allergic rhinitis|conjunctivitis|vasomotor rhinitis|dermatographism
carboplatin	Launched	DNA alkylating agent|DNA inhibitor		oncology	ovarian cancer
carboxyamidotriazole	Phase 3	calcium channel blocker	CXCL8		
carboxylosartan	Phase 1	angiotensin antagonist	AGTR1		
carboxypyridine-disulfide	Phase 2				
cardiogenol-C	Preclinical	cardiomyogenesis inducer			
cardionogen-1	Preclinical	WNT signaling inhibitor	CTNNB1		
carebastine	Phase 1	histamine receptor antagonist	HRH1		
carfilzomib	Launched	proteasome inhibitor	PSMA1|PSMA2|PSMA3|PSMA4|PSMA5|PSMA6|PSMA7|PSMA8|PSMB1|PSMB10|PSMB11|PSMB2|PSMB3|PSMB4|PSMB5|PSMB6|PSMB7|PSMB8|PSMB9	hematologic malignancy	multiple myeloma
carglumic-acid	Launched	carbamoyl phosphate synthase activator	CPS1	metabolism	hyperammonemia
caricotamide	Phase 2	NADPH quinone oxidoreductase inhibitor	NQO2		
cariporide	Phase 3	sodium/hydrogen exchanger inhibitor	SLC9A1		
cariprazine	Launched	dopamine receptor antagonist	DRD2|DRD3	neurology/psychiatry	schizophrenia
carmofur	Launched	thymidylate synthase inhibitor	TYMS	oncology	breast cancer|colorectal cancer
carmoterol	Phase 2	adrenergic receptor agonist	ADRB2		
carmoxirole	Phase 2	dopamine receptor agonist	DRD2		
carmustine	Launched	DNA alkylating agent|DNA inhibitor	GSR	hematologic malignancy|oncology	non-Hodgkin lymphoma (NHL)|Hodgkin's lymphoma|multiple myeloma|glioblastoma|brainstem glioma|medulloblastoma|astrocytoma|ependymoma
carnitine-(D/L)	Phase 3				
carnosine	Phase 2	antiglycating agent			
caroverin	Phase 3	cytochrome P450 inhibitor			
caroxazone	Withdrawn	monoamine oxidase inhibitor	MAOA|MAOB		
carprofen	Launched	cyclooxygenase inhibitor	PTGS2	rheumatology	osteoarthritis
carsalam	Preclinical	analgesic agent			
carteolol	Launched	adrenergic receptor antagonist	ADRB1|ADRB2|ADRB3	ophthalmology	intraocular pressure|glaucoma|ocular hypertension
carumonam	Launched	bacterial cell wall synthesis inhibitor		infectious disease	urinary tract infections|gram-negative bacterial infections
carvedilol	Launched	adrenergic receptor antagonist	ADRB1|ADRB2|ADRB3	cardiology	myocardial infarction|hypertension
carzenide	Preclinical		CA1|CA12|CA14|CA2|CA6|CA9		
casanthranol-variant	Launched			gastroenterology	constipation
casin	Preclinical	GTPase inhibitor	CDC42		
caspofungin	Launched	"bacterial cell wall synthesis inhibitor|fungal 1,3-beta-D-glucan synthase inhibitor"		infectious disease	candidemia|esophageal candidiasis|aspergillosis|peritonitis|fungal infection
castanospermine	Phase 2	glucosidase inhibitor	GAA|GBA		
catharanthine	Preclinical	tubulin polymerization inhibitor			
cathepsin-inhibitor-1	Preclinical	cathepsin inhibitor	CTSB|CTSL|CTSV		
CAY10505	Preclinical	PI3K inhibitor	PIK3CG		
CB-03-01	Phase 3	androgen receptor antagonist	AR		
CB-10-277	Phase 1	DNA synthesis inhibitor			
CB-5083	Phase 1	valosin-containing protein inhibitor	VCP		
CB-839	Phase 2	glutaminase inhibitor	GLS		
CBiPES	Preclinical	glutamate receptor positive allosteric modulator	GRM2		
cbl0137	Phase 1	histone chaperone inhibitor			
CBS-1114	Phase 1	lipoxygenase inhibitor	ALOX5		
CC-115	Phase 2	DNA protein kinase inhibitor|mTOR inhibitor	MTOR		
CC-223	Phase 2	mTOR inhibitor	MTOR		
CC-401	Phase 1	JNK inhibitor	MAPK8		
CC-90003	Phase 1	MAP kinase inhibitor			
CC-930	Phase 2	JNK inhibitor			
CCG-1423	Preclinical	apoptosis stimulant	RHOC|SRF		
CCG-50014	Preclinical	G protein signaling inhibitor	RGS4|RGS8		
CCG-63802	Preclinical	G protein signaling inhibitor	RGS4		
CCG-63808	Preclinical	G protein signaling inhibitor	RGS4		
CCMI	Preclinical	acetylcholine receptor allosteric modulator	CHRNA7		
CCMQ	Preclinical	homoquinolinic acid binding inhibitor			
CCT-031374	Preclinical	WNT signaling inhibitor	CTNNB1		
CCT018159	Preclinical	HSP inhibitor	HSP90AA1|HSP90AB1		
CCT128930	Preclinical	AKT inhibitor			
CCT129202	Preclinical	Aurora kinase inhibitor	AURKA|AURKB|AURKC		
CCT137690	Preclinical	Aurora kinase inhibitor	AURKA|AURKB|AURKC		
CCT196969	Preclinical	RAF inhibitor			
CCT245737	Preclinical	kinase inhibitor			
CC4	Preclinical	nicotinic receptor agonist	CHRNB2		
CD-1530	Preclinical	retinoid receptor agonist	RARG		
CD-437	Preclinical	retinoid receptor agonist	RARG		
CDBA	Phase 3				
CDK1-5-inhibitor	Preclinical	CDK inhibitor|glycogen synthase kinase inhibitor	CDK1|CDK5|GSK3B		
CDK9-IN-6	Preclinical	CDK inhibitor	CDK9		
CDPPB	Preclinical	glutamate receptor positive allosteric modulator	GRM5		
cebranopadol	Phase 3	opioid receptor agonist	OPRL1|OPRM1		
cediranib	Phase 3	KIT inhibitor|VEGFR inhibitor	CSF1R|FLT1|FLT3|FLT4|KDR|KIT|PDGFRA|PDGFRB		
cedrol	Phase 2				
cedrol-(+)	Phase 2	sedative			
cefaclor	Launched	bacterial cell wall synthesis inhibitor		infectious disease|otolaryngology	pneumonia|skin infections|urinary tract infections|respiratory tract infections|tonsillitis|pharyngitis
cefadroxil	Launched	bacterial cell wall synthesis inhibitor	SLC15A1|SLC15A2|SLC22A6|SLC22A8	infectious disease|otolaryngology	urinary tract infections|skin infections|tonsillitis|pharyngitis
cefalonium	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-positive bacterial infections
cefamandole	Launched	bacterial cell wall synthesis inhibitor		infectious disease	skin infections|urinary tract infections|respiratory tract infections
cefamandole-nafate	Launched	bacterial cell wall synthesis inhibitor		infectious disease	skin infections|urinary tract infections|respiratory tract infections
cefathiamidine	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-positive bacterial infections
cefazolin	Launched	bacterial cell wall synthesis inhibitor	PON1	infectious disease	urinary tract infections|skin infections|bacterial septicemia|endocarditis|surgical prophylaxis|bone and joint infections
cefcapene-pivoxil	Launched	bacterial cell wall synthesis inhibitor		infectious disease	skin infections|pneumonia|urinary tract infections
cefdinir	Launched	bacterial cell wall synthesis inhibitor	MPO	infectious disease|otolaryngology|pulmonary	pneumonia|tonsillitis|pharyngitis|bronchitis|skin infections|otitis|sinusitis
cefditoren-pivoxil	Launched	bacterial cell wall synthesis inhibitor		infectious disease|pulmonary|otolaryngology	pneumonia|bronchitis|skin infections|tonsillitis|pharyngitis
cefepime	Launched	bacterial cell wall synthesis inhibitor		infectious disease	pneumonia|urinary tract infections|skin infections|intra-abdominal infections
cefetamet	Launched	bacterial cell wall synthesis inhibitor		infectious disease|otolaryngology|pulmonary	ear infections|pneumonia|otitis|sinusitis|bronchitis|urinary tract infections
cefetamet-pivoxil	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-positive bacterial infections
cefiderocol	Launched	antibacterial 			
cefixime	Launched	bacterial cell wall synthesis inhibitor		infectious disease|otolaryngology|pulmonary	urinary tract infections|otitis|pharyngitis|tonsillitis|gonorrhea|bronchitis
cefmenoxime	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-negative bacterial infections
cefmetazole	Launched	bacterial cell wall synthesis inhibitor		infectious disease	urinary tract infections|skin infections
cefminox	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-negative bacterial infections
cefodizime	Launched	bacterial cell wall synthesis inhibitor		infectious disease	respiratory tract infections|skin infections|gonorrhea
cefonicid	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-positive bacterial infections
cefoperazone	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-negative bacterial infections
ceforanide	Launched	penicillin binding protein inhibitor		infectious disease	gram-negative bacterial infections
cefoselis	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-negative bacterial infections|gram-positive bacterial infections
cefotaxime	Launched	bacterial cell wall synthesis inhibitor		infectious disease	respiratory tract infections|bone and joint infections|pelvic inflammatory disease|intra-abdominal infections|skin infections|meningitis|urinary tract infections|bacterial septicemia|gynecologic infections
cefotetan	Launched	bacterial cell wall synthesis inhibitor		infectious disease	urinary tract infections|respiratory tract infections|skin infections|gynecologic infections|chlamydia|intra-abdominal infections|bone and joint infections|surgical prophylaxis
cefotiam	Launched	bacterial cell wall synthesis inhibitor		infectious disease	bacterial septicemia|bone and joint infections|respiratory tract infections|skin infections|urinary tract infections
cefotiam-cilexetil	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-negative bacterial infections|gram-positive bacterial infections
cefoxitin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	respiratory tract infections|urinary tract infections|intra-abdominal infections|gynecologic infections|bacterial septicemia|bone and joint infections|skin infections
cefozopran	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-negative bacterial infections|gram-positive bacterial infections
cefpiramide	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-negative bacterial infections
cefpirome	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-negative bacterial infections
cefpodoxime	Launched	bacterial cell wall synthesis inhibitor		otolaryngology|infectious disease|pulmonary	pharyngitis|pneumonia|bronchitis|gonorrhea|skin infections|urinary tract infections|sinusitis|tonsillitis
cefprozil	Launched	bacterial cell wall synthesis inhibitor		otolaryngology|infectious disease|pulmonary	pharyngitis|tonsillitis|otitis|sinusitis|respiratory tract infections|skin infections|bronchitis
cefradine	Launched	bacterial cell wall synthesis inhibitor	CYP3A4	infectious disease|otolaryngology	respiratory tract infections|otitis|skin infections|urinary tract infections|tonsillitis|pharyngitis|pneumonia
cefsulodin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-negative bacterial infections
ceftaroline-fosamil	Launched	bacterial cell wall synthesis inhibitor		infectious disease	skin infections|pneumonia
ceftazidime	Launched	bacterial cell wall synthesis inhibitor		infectious disease	respiratory tract infections|skin infections|bacterial septicemia|bone and joint infections|gynecologic infections|intra-abdominal infections|meningitis
ceftibuten	Launched	bacterial cell wall synthesis inhibitor		pulmonary|otolaryngology	bronchitis|otitis|pharyngitis|tonsillitis
ceftiofur	Launched	bacterial cell wall synthesis inhibitor		infectious disease	pneumonia|respiratory tract infections
ceftizoxim	Launched	bacterial cell wall synthesis inhibitor		infectious disease	respiratory tract infections|urinary tract infections|gonorrhea|pelvic inflammatory disease|intra-abdominal infections|bacterial septicemia|skin infections|bone and joint infections|meningitis
ceftobiprole	Phase 3	antiinfective drug			
ceftriaxone	Launched	bacterial cell wall synthesis inhibitor		infectious disease|otolaryngology	gonorrhea|pneumonia|otitis|skin infections|urinary tract infections|pelvic inflammatory disease|bacterial septicemia|bone and joint infections|intra-abdominal infections|meningitis|surgical prophylaxis
cefuroxime	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-negative bacterial infections
cefuroxime-axetil	Launched	bacterial cell wall synthesis inhibitor		otolaryngology	pharyngitis|tonsillitis|otitis|sinusitis
celecoxib	Launched	cyclooxygenase inhibitor	CA12|PDPK1|PTGS2	rheumatology|endocrinology	osteoarthritis|rheumatoid arthritis|ankylosing spondylitis|primary dysmenorrhea (PD)
celgosivir	Phase 2	glucosidase inhibitor			
celiprolol	Launched	adrenergic receptor antagonist	ADRA2A|ADRB1|ADRB2	genetics	Ehlers-Danlos syndrome (EDS)
cenerimod	Phase 2	sphingosine 1-phosphate receptor modulator			
cenicriviroc	Phase 3	CC chemokine receptor antagonist			
cenobamate	Launched	GABA receptor modulator|voltage-gated sodium channel blocker			
centanafadine	Phase 3	dopamine reuptake inhibitor			
centazolone	Phase 1	monoamine oxidase inhibitor			
centhaquin	Phase 1	analgesic agent			
centpropazine	Phase 3	inositol monophosphatase inhibitor			
CEP-32496	Phase 1/Phase 2	RAF inhibitor	BRAF|RAF1		
CEP-33779	Preclinical	JAK inhibitor	JAK2		
CEP-37440	Phase 1	ALK tyrosine kinase receptor inhibitor	ALK		
CEP-40783	Preclinical	AXL kinase inhibitor			
cephalexin	Launched	bacterial cell wall synthesis inhibitor		infectious disease|otolaryngology	respiratory tract infections|otitis|skin infections|bone and joint infections|genitourinary tract infections
cephalomannine	Preclinical	DNA polymerase inhibitor			
cephalosporin-c-zn	Preclinical	bacterial cell wall synthesis inhibitor			
cephalothin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	skin infections|surgical prophylaxis
cephapirin	Launched	bacterial cell wall synthesis inhibitor		obstetrics/gynecology	mastitis
cepharanthine	Phase 2	NFkB pathway inhibitor			
cephradine	Launched	bacterial cell wall synthesis inhibitor		infectious disease	skin infections|respiratory tract infections|urinary tract infections
ceramide	Launched	phosphoenolpyruvate carboxylase activator|serine/threonine protein phosphatase activator		dermatology	cosmetic
ceritinib	Launched	ALK tyrosine kinase receptor inhibitor	ALK|FLT3|IGF1R|INSR|TSSK1B	oncology	non-small cell lung cancer (NSCLC)
cerulenin	Launched	fatty acid synthase inhibitor	FASN	infectious disease	fungal infection
ceruletide	Preclinical	CCK receptor agonist	CCKAR		
cetaben	Phase 2	ACAT inhibitor|cholesterol inhibitor	PPARA		
cetilistat	Phase 3	triacylglycerol lipase inhibitor	PNLIP		
cetirizine	Launched	histamine receptor antagonist	HRH1	allergy	allergic rhinitis
cetrimonium	Launched			dermatology	cosmetic
cetrorelix	Launched	gonadotropin releasing factor hormone receptor antagonist	GNRHR|LHCGR	endocrinology	premature luteinizing hormone surges
cetylpyridinium	Launched			dental	gingivitis|mouth inflammation
cevimeline	Launched	acetylcholine receptor agonist	CHRM3	rheumatology	sjogren's syndrome
cevipabulin	Phase 1	microtubule stimulant|tubulin polymerization inhibitor	TUBB		
CE3F4	Preclinical	rap guanine nucleotide exchange factor inhibitor	RAPGEF3		
CFI-400945	Phase 2	serine/threonine kinase inhibitor			
CFI-402257	Phase 1/Phase 2	dual specificity protein kinase inhibitor			
CFM-1571	Preclinical	guanylate cyclase activator			
CFM-2	Preclinical	glutamate receptor antagonist			
CFTRinh-172	Preclinical	chloride channel blocker	CFTR		
CF102	Phase 2	adenosine receptor agonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
CG-400549	Phase 2	FABI inhibitor			
CGH2466	Preclinical	adenosine receptor antagonist	ADORA1|ADORA2B|ADORA3		
CGK-733	Preclinical	ATM kinase inhibitor|ATR kinase inhibitor	ATM|ATR		
CGM097	Phase 1	MDM inhibitor	MDM2		
CGP-12177	Phase 1	adrenergic receptor agonist	ADRB1|ADRB2|ADRB3		
CGP-13501	Preclinical	GABA receptor modulator	GABBR1		
CGP-20712A	Preclinical	adrenergic receptor antagonist	ADRB1|ADRB3		
CGP-25454A	Preclinical	dopamine receptor antagonist			
CGP-37157	Preclinical	mitochondrial Na+/Ca2+ exchanger antagonist|sodium/calcium exchange inhibitor	SLC8A1		
CGP-37849	Phase 1	glutamate receptor antagonist	GRIN2A|GRIN2B|GRIN2C|GRIN2D		
CGP-39551	Preclinical	NMDA receptor antagonist			
CGP-52411	Preclinical	EGFR inhibitor	EGFR		
CGP-53353	Preclinical	EGFR inhibitor|PKC inhibitor	EGFR|PRKCB		
CGP-54626	Preclinical	GABA receptor antagonist	GABBR1|GABBR2|KCTD12|KCTD16|KCTD8		
CGP-55845	Preclinical	GABA receptor antagonist	GABBR1|GABBR2|KCTD12|KCTD16|KCTD8		
CGP-57380	Preclinical	MAP kinase inhibitor	AURKB|LCK|MKNK1|MKNK2|SGK1		
CGP-60474	Preclinical	CDK inhibitor	CDK1|CDK2		
CGP-71683	Preclinical	neuropeptide receptor antagonist	NPY5R		
CGP-74514	Preclinical	CDK inhibitor	CDK1		
CGP-78608	Preclinical	glutamate receptor antagonist			
CGP-7930	Preclinical	GABA receptor modulator	GABBR1		
CGS-15943	Preclinical	adenosine receptor antagonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
CGS-20625	Phase 1	benzodiazepine receptor agonist|GABA benzodiazepine site receptor partial agonist	GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6		
CGS-21680	Preclinical	adenosine receptor agonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
CGS-9896	Preclinical	GABA receptor antagonist	GABRA1|GABRB2|GABRG2		
CH-170	Phase 1				
CH-5183284	Phase 2	fibroblast growth factor inhibitor	FGFR1|FGFR2|FGFR3		
CHC	Preclinical	monocarboxylate transporter inhibitor	SLC16A1		
chenodeoxycholic-acid	Launched	11-beta hydroxysteroid dehydrogenase inhibitor|FXR agonist	HSD11B1|NR1H4	cardiology|gastroenterology	cerebral cholesterosis|gallstones
CHF5074	Phase 2	gamma secretase modulator	PSEN1		
chicago-sky-blue-6b	Preclinical	glutamate inhibitor|macrophage migration inhibiting factor inhibitor	MIF		
chidamide	Launched	HDAC inhibitor	HDAC10|HDAC3	hematologic malignancy	peripheral T-cell lymphoma (PTCL)
chiniofon	Launched	antiprotozoal agent		infectious disease	amebiasis
CHIR-124	Preclinical	CHK inhibitor	CHEK1		
CHIR-98014	Preclinical	glycogen synthase kinase inhibitor	GSK3A|GSK3B		
CHIR-99021	Preclinical	glycogen synthase kinase inhibitor	CDK1|GSK3A|GSK3B|MAPK1		
chloralose	Preclinical				
chlorambucil	Launched	DNA inhibitor		hematologic malignancy	chronic lymphocytic leukemia (CLL)|Hodgkin's lymphoma
chloramine-T	Launched			infectious disease	bacterial gill disease
chloramphenicol	Launched	bacterial 50S ribosomal subunit inhibitor	CD55	infectious disease|endocrinology	meningitis|fever|cholera
chloramphenicol-palmitate	Launched	protein synthesis inhibitor		infectious disease|endocrinology	meningitis|fever|cholera
chloramphenicol-sodium-succinate	Launched	protein synthesis inhibitor		infectious disease	gram-negative bacterial infections
chlorazanil	Preclinical				
chlorcyclizine	Launched	histamine receptor antagonist		allergy	allergic rhinitis
chlorfenson	Phase 2	other antifungal			
chlorhexidine	Launched	membrane integrity inhibitor		dermatology|infectious disease|dental	cosmetic|skin infections|gingivitis
chlorindanol	Preclinical				
chlorindione	Preclinical				
chlorisondamine-diiodide	Preclinical	acetylcholine receptor antagonist	CHRNA1		
chlormadinone-acetate	Launched	5 alpha reductase inhibitor	PGR	endocrinology	hypermenorrhea|amenorrhea|oligomenorrhea|polymenorrhea
chlormezanone	Withdrawn	GABA receptor modulator	GABRA1		
chlormidazole	Launched	fungal lanosterol demethylase inhibitor		infectious disease	fungal infection
chlorobutanol	Launched			neurology/psychiatry	anesthetic|sedative
chlorocresol	Launched	ryanodine receptor activator		infectious disease	first-aid antiseptic
chlorogenic-acid	Launched	antioxidant	SLC37A4	neurology/psychiatry|pulmonary|allergy	headache|chest congestion|allergic rhinitis
chlorophyllin	Preclinical			urology	urinary incontinence
chlorophyllin-copper	Phase 1	cytochrome P450 inhibitor			
chloroprocaine	Launched	sodium channel blocker	ATP1A1|CHRNA10|GRIN3A|HTR3A|SCN10A|SLC6A3	neurology/psychiatry	local anesthetic
chloropyramine	Launched	histamine receptor antagonist	HRH1	cardiology|ophthalmology|allergy|pulmonary	edema|conjunctivitis|allergic rhinitis|asthma
chloroquine	Launched	antimalarial agent	MRGPRX1	infectious disease	malaria|amebiasis
chlorothiazide	Launched	diuretic	CA1|CA2|CA4|SLC12A3	cardiology	hypertension
chlorothymol	Launched				
chlorotrianisene	Launched	estrogenic hormone	ESR1|ESR2	endocrinology|oncology	menopause|prostate cancer
chloroxine	Launched	opioid receptor antagonist	OPRK1	gastroenterology|infectious disease|dermatology	diarrhea|inflammatory bowel disease|giardiasis|dandruff
chloroxoquinoline	Launched				
chloroxylenol	Launched	ATP synthase inhibitor		infectious disease	skin infections
chlorphenamine	Launched	histamine receptor antagonist		allergy	allergic rhinitis|urticaria
chlorphenesin	Launched	muscle relaxant		neurology/psychiatry	muscle relaxant|sedative
chlorphenoxamine	Preclinical	histamine receptor antagonist			
chlorphensin-carbamate	Launched	muscle relaxant		neurology/psychiatry	spasms
chlorproguanil	Launched	dihydrofolate reductase inhibitor	DHFR	infectious disease	malaria
chlorpromazine	Launched	dopamine receptor antagonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|CALM1|CHRM1|CHRM3|DRD1|DRD2|DRD3|DRD4|DRD5|HRH1|HRH4|HTR1A|HTR2A|HTR2B|HTR2C|HTR6|HTR7|KCNH2|ORM1|ORM2|SMPD1|TRPC5	neurology/psychiatry|gastroenterology|hematology|infectious disease	schizophrenia|nausea|vomiting|acute intermittent porphyria (AIP)|tetanus
chlorpropamide	Launched	ATP channel blocker	ABCC8|KCNJ10	endocrinology	diabetes mellitus
chlorpropham	Phase 1	antiviral			
chlorprothixene	Launched	dopamine receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|DRD1|DRD2|DRD3|HRH1|HTR2A|HTR2B|HTR2C	neurology/psychiatry	schizophrenia|bipolar disorder
chlorpyrifos	Launched	acetylcholinesterase inhibitor	ACHE		
chlorquinaldol	Launched	other antibiotic		infectious disease	fungal infection
chlortetracycline	Launched	protein synthesis inhibitor		ophthalmology	conjunctivitis
chlorthalidone	Launched	carbonic anhydrase inhibitor	CA1|CA12|CA14|CA2|CA4|CA7|SLC12A1	cardiology|gastroenterology|rheumatology|nephrology	hypertension|edema|congestive heart failure|hepatic cirrhosis|nephrotic syndrome|acute glomerulonephritis (AGN)|chronic renal failure
chlorzoxazone	Launched	bacterial 30S ribosomal subunit inhibitor	KCNMA1|KCNN4	neurology/psychiatry	muscle relaxant
cholecalciferol	Launched		VDR	endocrinology	vitamin D deficiency
cholesterol	Preclinical		RORA		
cholic-acid	Launched	bile acid	ADH1C|CES1|COX4I1|COX5A|COX5B|COX6A2|COX6B1|COX6C|COX7A1|COX7B|COX7C|COX8A|ESRRG|FABP6|FECH|GPBAR1|MT-CO1|MT-CO2|MT-CO3|PLA2G1B	gastroenterology|neurology/psychiatry|genetics	bile acid synthesis disorders|peroxisomal disorders|Zellweger syndrome
choline	Phase 3	acetylcholine precursor	ACHE|BCHE|CHRNA2|PCYT1A|PCYT1B|PHOSPHO1|PLD1|PLD2		
choline-alfoscerate	Launched	acetylcholine precursor			
CHPG	Preclinical	glutamate receptor agonist	GRM5		
CHR-6494	Preclinical	serine/threonine kinase inhibitor	GSG2		
chromanol-(+/-)	Preclinical	potassium channel blocker			
"chromanol-293B-(-)-[3R,4S]"	Preclinical	potassium channel blocker			
chromium-picolinate	Launched	insulin sensitizer		endocrinology	diabetes mellitus
chromocarb	Launched	antispasmodic			
chrysin	Phase 1	breast cancer resistance protein inhibitor	AKR1B1|CDK6|CYP19A1|CYP1B1		
chrysophanic-acid	Preclinical	EGFR inhibitor	EGFR|MTOR		
chuanxiongzine	Phase 2				
CH223191	Preclinical	aryl hydrocarbon receptor antagonist	AHR		
CH5132799	Phase 1	PI3K inhibitor	MTOR|PIK3CA|PIK3CB|PIK3CD|PIK3CG		
CH55	Preclinical	retinoid receptor binder	RARA|RARB		
CI-844	Phase 2				
CI-923	Phase 1	acetylcholine receptor antagonist			
CI-953	Phase 1	voltage-gated sodium channel blocker			
CI-966	Phase 1	GAT inhibitor	SLC6A1		
CI-976	Phase 1	ACAT inhibitor	ACAT1|CES1		
ciaftalan-zinc	Phase 1	reactive oxygen species stimulant			
cianidanol	Withdrawn	fatty acid synthase inhibitor	PTGS1		
cibenzoline	Launched	sodium channel blocker		cardiology	cardiac arrythmia
ciclesonide	Launched	glucocorticoid receptor agonist	NR3C1|SERPINA6	allergy	allergic rhinitis
ciclopirox	Launched	membrane integrity inhibitor	ATP1A1	infectious disease	onychomycosis
cicloprofen	Preclinical	cyclooxygenase inhibitor	PTGS1|PTGS2		
CID-16020046	Preclinical	G protein-coupled receptor antagonist	GPR55		
CID-2011756	Preclinical	protein kinase inhibitor	PKD1		
CID-2745687	Preclinical	G protein-coupled receptor antagonist	GPR35		
CID-5458317	Preclinical	MAP kinase phosphatase inhibitor	MAPK3		
cidofovir	Launched	DNA polymerase inhibitor		infectious disease	acquired immunodeficiency syndrome (AIDS)|cytomegalovirus retinitis
ciglitazone	Phase 2	PPAR receptor agonist	PPARG		
cilastatin	Launched	dehydropeptidase inhibitor	DPEP1		
cilazapril	Launched	angiotensin converting enzyme inhibitor	ACE	cardiology	hypertension|congestive heart failure
cilengitide	Phase 3	integrin antagonist	ITGAV|ITGB3		
cilnidipine	Launched	calcium channel blocker	CACNA1B	cardiology	hypertension
cilofexor	Phase 3	FXR agonist			
cilomilast	Phase 3	phosphodiesterase inhibitor	PDE4A|PDE4B|PDE4D		
cilostamide	Preclinical	phosphodiesterase inhibitor	PDE3A|PDE3B		
cilostazol	Launched	phosphodiesterase inhibitor	PDE3A|PDE3B	cardiology	claudication
ciluprevir	Preclinical	serine protease inhibitor			
CIM-0216	Preclinical	transient receptor potential channel agonist	TRPM3		
cimaterol	Preclinical	adrenergic receptor agonist	ADRB1|ADRB2|ADRB3		
cimetidine	Launched	histamine receptor antagonist	HRH2|SLC29A4|SLC47A1|SLC47A2	gastroenterology|hematologic malignancy|endocrinology	duodenal ulcer disease|peptic ulcer disease (PUD)|gastroesophageal reflux disease (GERD)|aggressive systemic mastocytosis (ASM)|Zollinger-Ellison syndrome|endocrine adenoma
cimetropium	Launched	acetylcholine receptor antagonist	CHRM1	gastroenterology	irritable bowel syndrome
cinacalcet	Launched	calcium channel activator	CASR	endocrinology|nephrology|oncology	hyperparathyroidism|chronic kidney disease (CKD)|parathyroid carcinoma|hypercalcemia
cinaciguat	Phase 2	guanylate cyclase activator	GUCY1A3|GUCY1B3		
cinalukast	Phase 2	leukotriene receptor antagonist	CYSLTR1		
cinanserin	Preclinical	serotonin receptor antagonist	HTR2A		
cinchocaine	Launched	sodium channel blocker	CALM1|SCN10A|SCN5A	neurology/psychiatry	local anesthetic
cinchonidine	Phase 1	P glycoprotein inhibitor			
cinchonine	Preclinical	P glycoprotein inhibitor	CYP2D6		
cinchophen	Launched	analgesic agent		rheumatology	gout
cinepazet	Launched	vasodilator			
cinepazide	Withdrawn	calcium channel activator			
cinflumide	Phase 2	muscle relaxant			
cinnamaldehyde	Preclinical	aldose reductase inhibitor|TRPV agonist	TRPA1		
cinnarazine	Launched	calcium channel blocker		neurology/psychiatry|gastroenterology|ophthalmology	Meniere's disease|nausea|vomiting|Cogan's syndrome
cinobufotalin	Phase 1	anticancer agent			
cinoctramide	Preclinical				
cinoxacin	Launched	topoisomerase inhibitor		infectious disease	urinary tract infections
cinoxate	Launched			dermatology	sunscreen lotion
CINPA-1	Preclinical	CAR antagonist	NR1H4|NR1I3|PPARG		
cinromide	Phase 3				
cintirorgon	Phase 1/Phase 2	ROR agonist			
cintriamide	Preclinical				
cipamfylline	Phase 2	phosphodiesterase inhibitor			
cipargamin	Phase 2	antimalarial agent			
cipemastat	Phase 3	metalloproteinase inhibitor	ADAM17|MMP1|MMP13|MMP2|MMP3|MMP8|MMP9		
ciprofibrate	Launched	PPAR receptor agonist	PPARA	endocrinology	hyperlipidemia
ciprofloxacin	Launched	bacterial DNA gyrase inhibitor	TOP2A	otolaryngology	otitis
ciproxifan	Preclinical	histamine receptor antagonist	ADRA2A|ADRA2C|HRH3|HRH4|HTR3A		
CIQ	Preclinical	glutamate receptor potentiator	GRIN2C|GRIN2D		
cirazoline	Preclinical	adrenergic receptor agonist	ADRA1A		
cis-aconitic-acid	Preclinical		ACO2		
cis-ACPD	Preclinical	glutamate receptor agonist	GRM2|GRM3|GRM6|GRM7|GRM8		
"cis-exo-camphanediol-2,3"	Phase 1	nitric oxide stimulant	NOS3		
cis-urocanic-acid	Phase 2	serotonin receptor agonist	HTR2A		
"cis-9,trans-11-conjugated-linoleic-acid"	Launched				
cisapride	Withdrawn	serotonin receptor agonist	HTR2A|HTR3A|HTR4|KCNH2		
cisatracurium	Launched	acetylcholine receptor antagonist	CHRNA2	neurology/psychiatry|critical care	muscle relaxant|endotracheal intubation
cisplatin	Launched	DNA alkylating agent|DNA synthesis inhibitor	XIAP	oncology	testicular carcinoma|ovarian cancer|bladder cancer
citalopram	Launched	selective serotonin reuptake inhibitor (SSRI)	ADRA1A|CHRM1|HRH1|SLC6A2|SLC6A3|SLC6A4	neurology/psychiatry	depression
citarinostat	Phase 1	HDAC inhibitor			
CITCO	Preclinical	constitutive androstane receptor (CAR) agonist	NR1I3		
citicoline	Launched	glutathione transferase stimulant|membrane permeability enhancer	ACHE|SLC1A2	neurology/psychiatry|ophthalmology	stroke|Alzheimer's disease|senile dementia|Parkinson's Disease|attention-deficit/hyperactivity disorder (ADHD)|glaucoma
citiolone	Preclinical	lipotropic|mucolytic agent			
citric-acid	Preclinical	coagulation factor inhibitor	AKR1B1|ANG|APRT|BHMT|C8G|CA4|CPB1|CS|CTDSP1|GNMT|HGS|HS3ST3A1|IL4I1|ITPA|LSM6|MDH2|MIF|PDE5A|PKD2L1|PLEKHA1|RNASE1|RNASE3|SRC|TNFSF13B|UCK2		
CJ-033466	Preclinical	serotonin receptor agonist	HTR4		
CJ-13610	Phase 2	lipoxygenase inhibitor			
CK-101	Preclinical	EGFR inhibitor			
CK-636	Preclinical	actin related protein inhibitor	ACTR2|ACTR3|ARPC1B|ARPC2|ARPC3|ARPC4|ARPC5		
CKD-712	Phase 1	NFkB pathway inhibitor	JAK2|STAT1		
CKI-7	Preclinical	casein kinase inhibitor	CSNK1G2		
CL-218872	Phase 1	benzodiazepine receptor agonist	GABRA1|GABRA2|GABRA3|GABRA5|GABRB2|GABRG2		
CL-225385	Phase 2				
cladribine	Launched	adenosine deaminase inhibitor|ribonucleotide reductase inhibitor	ADA|PNP|POLA1|POLE|POLE2|POLE3|POLE4|RRM1|RRM2|RRM2B	hematologic malignancy	hairy cell leukemia
clamikalant	Preclinical	ATP-sensitive potassium channel antagonist			
clanfenur	Preclinical	anticancer agent			
clarithromycin	Launched	bacterial 50S ribosomal subunit inhibitor	CYP3A4	otolaryngology|pulmonary|infectious disease	pharyngitis|tonsillitis|sinusitis|bronchitis|pneumonia|skin infections|otitis
clavulanate	Launched	beta lactamase inhibitor		otolaryngology	otitis
clebopride	Launched	dopamine receptor antagonist	ACHE|DRD2	gastroenterology	nausea
clemastine	Launched	histamine receptor antagonist	HRH1	allergy	allergic rhinitis|urticaria
clemizole	Launched	HCV inhibitor		allergy	allergic rhinitis
clenbuterol	Launched	adrenergic receptor agonist	ABCC8|ADRB2|KCNJ11	pulmonary	chronic obstructive pulmonary disease (COPD)|asthma
cleviprex	Launched	calcium channel blocker	CACNA1C|CACNA1D|CACNA1F|CACNA1S	cardiology	hypertension
clevudine	Launched	DNA polymerase inhibitor		infectious disease	hepatitis B
clidinium	Launched	acetylcholine receptor antagonist	CHRM1|CHRM3	gastroenterology	peptic ulcer disease (PUD)|irritable bowel syndrome|enterocolitis
climbazole	Launched	enzyme inducer		dermatology	dandruff|eczema
clinafloxacin	Phase 3	bacterial DNA gyrase inhibitor			
clindamycin	Launched	protein synthesis inhibitor		infectious disease	respiratory tract infections|pneumonia|skin infections|gynecologic infections|intra-abdominal infections|bacterial septicemia|bone and joint infections
clindamycin-palmitate	Launched	bacterial 50S ribosomal subunit inhibitor		infectious disease	intra-abdominal infections|skin infections|pneumonia|peritonitis|gynecologic infections
clindamycin-phosphate	Launched	protein synthesis inhibitor		obstetrics/gynecology	bacterial vaginosis
clinofibrate	Launched	lipase clearing factor inhibitor	LPL	endocrinology	hypertriglyceridemia
clioquinol	Withdrawn	chelating agent	OPRK1		
clobenpropit	Preclinical	histamine receptor antagonist	HRH1|HRH2|HRH3|HRH4		
clobetasol-propionate	Launched	glucocorticoid receptor agonist	NR3C1|PLA2G1B	dermatology	corticosteroid-responsive dermatoses
clobetasone-butyrate	Launched	corticosteroid agonist	NR3C1	dermatology	eczema|psoriasis|dermatitis
clobutinol	Withdrawn	antitussive			
clocortolone-pivalate	Launched	steroid	NR3C1|PLA2G1B	dermatology	corticosteroid-responsive dermatoses
clodronic-acid	Launched	bone resorption inhibitor	SLC25A4|SLC25A5|SLC25A6	orthopedics|endocrinology|hematologic malignancy	osteoporosis|hyperparathyroidism|hypercalcemia|multiple myeloma
clofarabine	Launched	ribonucleotide reductase inhibitor	POLA1|POLD1|POLE|RRM1|RRM2|RRM2B	hematologic malignancy	acute lymphoblastic leukemia (ALL)
clofazimine	Launched	GK0582 inhibitor		infectious disease	leprosy
clofedanol	Launched	histamine receptor antagonist	HRH1	pulmonary	cough suppressant
clofibrate	Launched	PPAR receptor agonist	LPL|PPARA	endocrinology|cardiology	hyperlipidemia|cholesterol
clofibric-acid	Launched	PPAR receptor agonist	PPARA	endocrinology	hyperlipidemia
clofilium	Phase 2	potassium channel blocker	KCNA5|KCNH1		
clofoctol	Launched	protein synthesis inhibitor		infectious disease	gram-positive bacterial infections
clomesone	Phase 1	DNA inhibitor			
clomethiazole	Launched	GABA receptor antagonist|GABA receptor modulator	GABRA1	neurology/psychiatry	Parkinson's Disease|sedative|muscle relaxant
clomifene	Launched	estrogen receptor antagonist	ESR1	obstetrics/gynecology	infertility
clomipramine	Launched	serotonin transporter (SERT) inhibitor	GSTP1|HTR2A|HTR2B|HTR2C|SLC6A2|SLC6A3|SLC6A4	neurology/psychiatry	obsessive compulsive disorder (OCD)
clonidine	Launched	adrenergic receptor agonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C	cardiology|neurology/psychiatry	hypertension|attention-deficit/hyperactivity disorder (ADHD)
clonixin	Preclinical	cyclooxygenase inhibitor	PTGS1|PTGS2	rheumatology|infectious disease	rheumatoid arthritis|soft tissue infection
clonixin-lysinate	Launched	cyclooxygenase inhibitor		neurology/psychiatry	pain relief
clopamide	Launched	sodium/chloride cotransporter inhibitor		cardiology	hypertension
cloperastine	Launched	antitussive		pulmonary	cough suppressant
cloperastine-fendizoate	Preclinical	potassium channel antagonist			
clopidogrel	Launched	purinergic receptor antagonist	P2RY12	cardiology|neurology/psychiatry	myocardial infarction|stroke|peripheral artery disease (PAD)|acute coronary syndrome (ACS)
clopidol	Launched			infectious disease	coccidiosis
cloprostenol-(+/-)	Launched	prostaglandin receptor agonist	PTGDR|PTGER1|PTGER3|PTGFR|TBXA2R	obstetrics/gynecology	endometriosis
cloranolol	Launched	adrenergic receptor antagonist	ADRB1|ADRB2|ADRB3	cardiology	hypertension
clorgiline	Phase 2	monoamine oxidase inhibitor	MAOA		
clorotepine	Launched	adrenergic receptor antagonist|dopamine receptor antagonist	ADRA1A|ADRA1B|ADRA1D|DRD2|HRH1|HTR2C|HTR6	neurology/psychiatry	psychosis
clorprenaline	Launched	adrenergic receptor agonist	ADRB1|ADRB2	pulmonary	asthma
clorsulon	Launched	glycolysis inhibitor		infectious disease	gastrointestinal roundworms|lungworms|liver flukes|lice|mites
closantel	Launched	chitinase inhibitor|NFkB pathway inhibitor		infectious disease	liver flukes
clotiapine	Launched			neurology/psychiatry	psychosis
clotrimazole	Launched	cytochrome P450 inhibitor|imidazoline receptor ligand	CYP3A4|KCNN4|NR1I2|NR1I3|TRPM2|TRPM4|TRPM8	infectious disease	vulvovaginal candidiasis|oropharyngeal candidiasis
cloxacillin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-positive bacterial infections
cloxyquin	Preclinical	potassium channel activator	KCNK18		
clozapine	Launched	dopamine receptor antagonist|serotonin receptor antagonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|CALY|CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|DRD1|DRD2|DRD3|DRD4|DRD5|HRH1|HRH4|HTR1A|HTR1B|HTR1D|HTR1E|HTR1F|HTR2A|HTR2B|HTR2C|HTR3A|HTR5A|HTR6|HTR7	neurology/psychiatry	schizophrenia
CL316243	Phase 2	adrenergic receptor agonist	ADRB3|UCP1|UCP2|UCP3		
CM-4620	Phase 2	calcium release activated channel modulator			
CMPD-1	Preclinical	p38 MAPK inhibitor	GNRHR|MAPK14		
CNQX	Phase 1	glutamate receptor antagonist	GRIA1|GRIA2|GRIA3|GRIA4		
CNX-2006	Preclinical	EGFR inhibitor	EGFR		
CNX-774	Preclinical	Bruton's tyrosine kinase (BTK) inhibitor	BTK		
CO-101244	Preclinical	glutamate receptor antagonist	GRIN2B		
CO-102862	Phase 1	sodium channel blocker	SCN4A|SCN9A		
cobicistat	Launched	cytochrome P450 inhibitor	CYP3A4|CYP3A43|CYP3A5|CYP3A7	infectious disease	human immunodeficiency virus (HIV-1)
cobimetinib	Launched	MEK inhibitor	MAP2K1	oncology	melanoma
coenzyme-A	Launched		ACAT2|CRAT|CS|DBI|HMGCR|KAT2A|KAT2B|KAT5		
coenzyme-I	Phase 2		AASS|ACADS|ADH1A|ADH1B|ADH1C|ADH4|ADH5|ADH7|AKR1B1|AKR1C1|AKR1C2|AKR1C3|AKR1C4|ALDH1A1|ALDH1A2|ALDH1A3|ALDH1B1|ALDH2|ALDH3A1|ALDH3A2|ALDH3B1|ALDH3B2|ALDH4A1|ALDH5A1|ALDH6A1|ALDH7A1|ALDH9A1|AMT|BDH1|BLVRA|BLVRB|CDO1|CYB5R3|CYP17A1|CYP4A11|DHCR7|DHFR|DLAT|DLD|EHHADH|GAPDH|GAPDHS|GLUD1|GLUD2|GPD1|GSR|H6PD|HADH|HADHA|HIBADH|HMGCR|HMOX1|HMOX2|HPGD|HSD11B1|HSD11B2|HSD17B1|HSD17B10|HSD17B2|HSD17B3|HSD17B4|HSD17B7|HSD17B8|HSD3B1|HSD3B2|IDH3A|IDH3B|IDH3G|IMPDH1|IMPDH2|LDHA|LDHAL6A|LDHAL6B|LDHB|LDHC|MDH1|MDH2|ME1|ME2|ME3|MSMO1|MT-ND1|MT-ND2|MT-ND3|MT-ND4|MT-ND4L|MT-ND5|MT-ND6|MTHFD1|MTHFD2|NDUFA1|NDUFA10|NDUFA11|NDUFA12|NDUFA13|NDUFA2|NDUFA3|NDUFA4|NDUFA4L2|NDUFA5|NDUFA6|NDUFA7|NDUFA8|NDUFA9|NDUFAB1|NDUFB1|NDUFB10|NDUFB2|NDUFB3|NDUFB4|NDUFB5|NDUFB6|NDUFB7|NDUFB8|NDUFB9|NDUFC1|NDUFC2|NDUFS1|NDUFS2|NDUFS3|NDUFS4|NDUFS5|NDUFS6|NDUFS7|NDUFS8|NDUFV1|NDUFV2|NDUFV3|NNT|NQO2|NSDHL|OGDH|PDHA1|PDHA2|PDHB|PHGDH|PYCR1|PYCR2|QDPR|RDH5|SORD|TSTA3|TYR|UGDH		
coenzyme-Q10	Launched				
COH29	Phase 1	ribonucleotide reductase inhibitor			
colchicine	Launched	microtubule inhibitor	GLRA1|GLRA2|TUBA1A|TUBA1B|TUBA1C|TUBA3C|TUBA3D|TUBA3E|TUBA4A|TUBB|TUBB1|TUBB2A|TUBB2B|TUBB3|TUBB4A|TUBB4B|TUBB6|TUBB8	rheumatology|endocrinology	gout|fever
colforsin	Phase 2	adenylyl cyclase activator	ADCY2|ADCY5		
colforsin-daproate	Launched	adenylyl cyclase activator			
colfosceril-palmitate	Launched	pulmonary surfactant		pulmonary	respiratory distress syndrome (RDS)
colistimethate	Launched	bacterial permeability inducer		infectious disease	gram-negative bacterial infections
colistin	Launched	bacterial permeability inducer		infectious disease	gram-negative bacterial infections|gram-negative bacterial infections
combretastatin-A-4	Phase 2	tubulin polymerization inhibitor			
compound-w	Preclinical	beta-secretase inhibitor	BACE1		
compound-401	Preclinical	DNA dependent protein kinase inhibitor	MTOR|PRKDC		
compound-58112	Preclinical				
conivaptan	Launched	vasopressin receptor antagonist	AVPR1A|AVPR2	endocrinology	hyponatremia
convallatoxin	Preclinical	cardiac glycoside			
copanlisib	Launched	PI3K inhibitor	PIK3CA|PIK3CB|PIK3CD|PIK3CG	hematologic malignancy	follicular lymphoma
copper-histidine	Phase 3		SLC15A3|SLC15A4|SLC38A5		
COR-170	Preclinical	cannabinoid receptor inverse agonist	CNR2		
cordycepin	Phase 1/Phase 2	DNA inhibitor			
corosolic-acid	Phase 2	PKC inhibitor|protein tyrosine kinase inhibitor	HSD11B1|PTPN1		
CORT-108297	Preclinical	glucocorticoid receptor antagonist			
corticosterone	Preclinical	mineralocorticoid receptor agonist	HSD11B1|NCOA1|NR3C2		
cortisone	Launched	glucocorticoid receptor agonist	NR3C1	gastroenterology|rheumatology|dermatology	ulcerative colitis|rheumatoid arthritis|psoriasis|joint inflammation|eczema
cortisone-acetate	Launched	glucocorticoid receptor agonist	NR3C1	pulmonary|rheumatology|allergy|dermatology|ophthalmology|gastroenterology|infectious disease	asthma|rheumatoid arthritis|urticaria|osteoarthritis|psoriasis|allergic rhinitis|conjunctivitis|ulcerative colitis|meningitis
cortodoxone	Phase 3	androgen receptor antagonist	AR		
costunolide	Preclinical	telomerase inhibitor			
cot-inhibitor-1	Preclinical	MAPK-interacting kinase inhibitor	MAP3K8		
cot-inhibitor-2	Preclinical	MAPK-interacting kinase inhibitor	MAP3K8		
COTI-2	Phase 1	anticancer agent			
cotinine	Phase 2	nicotine metabolite			
coumarin	Launched	vitamin K antagonist	CA1|CA12|CA14|CA2|CA4|CA6|CA9|CYP2A6	gastroenterology|pulmonary	ulcerative colitis|asthma|celiac disease
coumophos	Preclinical	cholinesterase inhibitor			
"CP-105,696"	Preclinical	leukotriene receptor antagonist			
CP-316819	Preclinical	glycogen phosphorylase inhibitor	PYGL		
CP-339818	Preclinical	potassium channel blocker	KCNA3		
CP-376395	Phase 1	corticotropin releasing factor receptor antagonist	CRHR1		
CP-471474	Preclinical	matrix metalloprotease inhibitor	MMP1|MMP13|MMP2|MMP3|MMP9		
CP-532623	Phase 1	cholesteryl ester transfer protein inhibitor	CETP		
CP-547632	Phase 2	kinase inhibitor			
CP-640186	Preclinical	acetyl-CoA carboxylase inhibitor	ACACA|ACACB		
CP-673451	Preclinical	PDGFR tyrosine kinase receptor inhibitor	KIT|PDGFRA|PDGFRB		
CP-724714	Phase 2	EGFR inhibitor|protein tyrosine kinase inhibitor	ERBB2		
CP-775146	Preclinical	PPAR receptor agonist	PPARA		
CP-91149	Preclinical	glycogen phosphorylase inhibitor	PYGL		
CP-93129	Preclinical	serotonin receptor agonist	HTR1A		
CP-94253	Preclinical	serotonin receptor agonist	HTR1B		
"CP-945,598"	Phase 3	cannabinoid receptor antagonist	CNR1		
CP-99994	Phase 2	tachykinin antagonist	TACR1		
CPA-inhibitor	Preclinical	carboxypeptidase inhibitor	CPA1|CPA2		
CPCCOEt	Preclinical	glutamate receptor antagonist	GRM1		
CPI-0610	Phase 2	bromodomain inhibitor	BRD4		
CPI-1189	Phase 2	tumor necrosis factor release inhibitor	TNF		
CPI-1205	Phase 1/Phase 2	EZH2 inhibitor			
CPI-169	Preclinical	histone lysine methyltransferase inhibitor	EZH2		
CPI-203	Preclinical	bromodomain inhibitor	BRD4		
CPI-360	Preclinical	histone lysine methyltransferase inhibitor	EZH2		
CPI-444	Phase 1/Phase 2	adenosine receptor antagonist			
CPI-613	Phase 3	pyruvate dehydrogenase inhibitor	PDHA1		
CPP	Phase 2	glutamate receptor antagonist	GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D		
CPSI-1306-(+/-)	Preclinical	macrophage migration inhibiting factor inhibitor	MIF		
CQS	Preclinical				
creatine	Launched		CKB|CKM|CKMT1A|CKMT2|GAMT|SLC6A8		
creatinine	Preclinical				
creatinol-phosphate	Launched				
crenigacestat	Preclinical	notch signaling inhibitor			
crenolanib	Phase 3	PDGFR tyrosine kinase receptor inhibitor	CSF1R|FLT3|KIT|PDGFRA|PDGFRB		
cresol	Launched				
cresopirine	Preclinical				
cridanimod	Launched	progesterone receptor agonist	PGR	infectious disease	influenza A virus infection
crisaborole	Launched	phosphodiesterase inhibitor	PDE4A|PDE4B|PDE4C|PDE4D	dermatology	dermatitis
crisdesalazine	Preclinical	free radical scavenger			
crizotinib	Launched	ALK tyrosine kinase receptor inhibitor	ALK|MET	oncology	non-small cell lung cancer (NSCLC)
crizotinib-(S)	Preclinical	MTH1 inhibitor	NUDT1		
croconazole	Launched	bacterial cell wall synthesis inhibitor		infectious disease	fungal infection
crolibulin	Phase 1/Phase 2	tubulin polymerization inhibitor			
cromakalim	Phase 2		KCNJ8		
cromoglicic-acid	Launched	immunosuppressant	KCNMA1|S100P	pulmonary|ophthalmology|allergy|gastroenterology	asthma|conjunctivitis|urticaria|ulcerative colitis
crotamiton	Launched	antipruritic		infectious disease	scabies
CRT0044876	Preclinical				
cryptotanshinone	Preclinical	acetylcholinesterase inhibitor|STAT inhibitor	STAT3		
crystal-violet	Launched	other antibiotic			
CR8-(R)	Preclinical	CDK inhibitor	CCNA2		
CS-110266	Preclinical	dopamine receptor agonist	SLC6A3		
CS-917	Phase 2	fructose biphosphate inhibitor	FBP1		
CT-7758	Phase 2	integrin antagonist	ITGA4		
CTEP	Preclinical	glutamate receptor antagonist	GRM5		
CTS-1027	Phase 2	metalloproteinase inhibitor	MMP1|MMP13|MMP2|MMP3|MMP9		
CTS21166	Phase 1	beta-secretase inhibitor	BACE1		
CT7001	Phase 1/Phase 2	CDK inhibitor			
CU-CPT-4a	Preclinical	toll-like receptor inhibitor	TLR3		
CU-T12-9	Preclinical	toll-like receptor agonist	TLR1|TLR2		
CUDC-101	Phase 1	EGFR inhibitor	EGFR|ERBB2		
CUDC-427	Phase 1	apoptosis inhibitor	XIAP		
CUDC-907	Phase 2	PI3K inhibitor	HDAC2|PIK3R1		
CUR-61414	Phase 1	smoothened receptor antagonist	DHH|IHH|SMO		
curcumin	Launched	cyclooxygenase inhibitor|histone acetyltransferase inhibitor|lipoxygenase inhibitor|NFkB pathway inhibitor	APP|CA1|CA12|CA14|CA2|CA4|CA6|CA9|CHRM3|CYP3A4|DNMT3B|EP300|MMP13|MMP9|NOS2|PTGS1|PTGS2|XDH		
curcumol	Phase 1	JAK inhibitor	JAK1|JAK2|JAK3		
cutamesine	Phase 2	sigma receptor agonist	SIGMAR1		
CV-1808	Preclinical	adenosine receptor agonist	ADORA2A		
CVT-10216	Phase 1	aldehyde dehydrogenase inhibitor	ALDH2		
CW-008	Preclinical	PKA activator	PRKACA		
CX-4945	Phase 1/Phase 2	casein kinase inhibitor	CSNK2A1|CSNK2A2|DAPK3|HIPK3		
CX-516	Phase 2/Phase 3	glutamate receptor modulator			
CX-5461	Phase 1	RNA polymerase inhibitor			
CXD101	Phase 1/Phase 2	HDAC inhibitor			
cyacetacide	Preclinical				
cyamemazine	Launched	serotonin receptor antagonist	HTR1A|HTR2A|HTR2C|HTR7	neurology/psychiatry	schizophrenia|anxiety
cyanocobalamin	Launched	methylmalonyl CoA mutase stimulant|vitamin B	MUT	hematology|infectious disease|gastroenterology	anemia|fish tapeworm infestation|celiac disease
cyanopindolol	Phase 2	adrenergic receptor antagonist	ADRB1|HTR1A|HTR1D		
cyclamic-acid	Preclinical				
cyclandelate	Launched	calcium channel blocker		cardiology|rheumatology	claudication|arteriosclerosis|Raynaud's disease
cyclic-AMP	Preclinical		CNGA3|TRPM7		
cyclizine	Launched	histamine receptor modulator	HRH1|SULT1E1	gastroenterology|neurology/psychiatry	nausea|vomiting|vertigo|motion sickness
cyclobenzaprine	Launched	adrenergic receptor agonist|serotonin receptor agonist	HTR2A	neurology/psychiatry	spasms
cyclocreatine	Phase 1	creatine kinase substrate			
cyclocytidine	Preclinical	DNA synthesis inhibitor|RNA synthesis inhibitor			
cycloheximide	Preclinical	protein synthesis inhibitor	RPL3		
cyclopamine	Preclinical	hedgehog pathway inhibitor			
cyclopenthiazide	Launched	thiazide diuretic		cardiology	hypertension|congestive heart failure
cyclopentolate	Launched	acetylcholine receptor antagonist		ophthalmology	mydriasis|cycloplegia
cyclophosphamide	Launched	DNA alkylating agent	CYP2A6|CYP2B6|CYP2C18|CYP2C19|CYP2C8|CYP2C9|CYP2D6|CYP3A4|CYP3A5|CYP3A7	hematologic malignancy|oncology	Hodgkin's lymphoma|small lymphocytic lymphoma (SLL)|breast cancer|neuroblastoma|Burkitt's lymphoma|multiple myeloma|chronic lymphocytic leukemia (CLL)|acute myeloid leukemia (AML)|acute lymphoblastic leukemia (ALL)|chronic myeloid leukemia (CML)|true histiocytic lymphoma (THL)|retinoblastoma|ovarian cancer
cyclopiazonic-acid	Preclinical	ATPase inhibitor	ATP2A1		
cycloserine-(D)	Launched	bacterial cell wall synthesis inhibitor	GRIN1	infectious disease	tuberculosis|tuberculosis
cyclosporin-A	Launched	calcineurin inhibitor	ABCB11|CAMLG|FPR1|PPIA|PPIF|PPP3CA|PPP3R2|SLC10A1|SLCO1B1|SLCO1B3	rheumatology|dermatology	rheumatoid arthritis|psoriasis
cyclothiazide	Launched	glutamate receptor modulator	CA2|GRIA1|GRIA2|GRIA3|GRIA4|SLC12A3	cardiology	hypertension
cyclovalone	Launched	breast cancer resistance protein inhibitor	ABCG2	gastroenterology	bile stimulation
cyclovirobuxin-D	Preclinical	calcium channel modulator			
CycLuc1	Preclinical				
CYC065	Phase 1	CDK inhibitor			
CYC116	Phase 1	Aurora kinase inhibitor	AURKA|AURKB|KDR		
CYM-50260	Preclinical	sphingosine 1-phosphate receptor agonist	S1PR4		
CYM-50358	Preclinical	sphingosine 1-phosphate receptor antagonist	S1PR4		
CYM-50769	Preclinical	neuropeptide receptor antagonist	NPBWR1		
CYM-5442	Preclinical	sphingosine 1-phosphate receptor agonist	S1PR1		
CYM-5520	Preclinical	sphingosine 1-phosphate receptor agonist	S1PR2		
CYM-5541	Preclinical	sphingosine 1-phosphate receptor agonist	S1PR3		
cypermethrin	Launched			infectious disease	flea control
cyproheptadine	Launched	histamine receptor antagonist	ADRA1A|ADRA1B|ADRA1D|CHRM1|CHRM2|CHRM3|HRH1|HTR2A|HTR2C|HTR6|HTR7	allergy|otolaryngology|ophthalmology|dermatology	allergic rhinitis|vasomotor rhinitis|conjunctivitis|urticaria|dermatographism
cyproterone-acetate	Launched	androgen receptor antagonist	ADORA1|AR	oncology	prostate cancer
cyromazine	Launched				
cysteamine	Launched	tissue transglutaminase inhibitor	NPY2R|SST	metabolism	cystinosis
CYT-997	Phase 2	tubulin polymerization inhibitor	TUBB		
cytarabine	Launched	ribonucleotide reductase inhibitor	POLA1|POLB|POLD1|POLE	hematologic malignancy	acute lymphoblastic leukemia (ALL)|chronic lymphocytic leukemia (CLL)|acute myeloid leukemia (AML)|non-Hodgkin lymphoma (NHL)
cytidine	Launched				
cytisine	Launched	acetylcholine receptor agonist	CHRNA2|CHRNA3|CHRNA4|CHRNA6|CHRNA7|CHRNB2|CHRNB4	neurology/psychiatry	nicotinism
cytochalasin-B	Phase 2	microtubule inhibitor	ACTB		
cytochlor	Phase 1				
cyt387	Phase 3	JAK inhibitor	JAK1|JAK2|JAK3		
CY208-243	Phase 2	dopamine receptor agonist	CALY		
CZC-54252	Preclinical	leucine rich repeat kinase inhibitor	LRRK2		
CZC24832	Preclinical	PI3K inhibitor	PIK3CG		
C106	Phase 3				
C11-Acetate	Phase 3		ABAT|ACE|AKR1C3|CA2|CELA1|ESR2|FFAR2|FFAR3|HPRT1|LTA4H|MMP12|NOS1|NOS3|PLA2G1B|PTPN1|SOD1|TXN		
C188-9	Preclinical	STAT inhibitor			
C34	Preclinical	toll-like receptor inhibitor	TLR4		
C646	Preclinical	histone acetyltransferase inhibitor	EP300		
"D,L-mevalonic-acid-lactone"	Preclinical				
D-(+)-maltose	Preclinical		MGAM		
D-alpha-tocopheryl-succinate	Launched				
D-delta-tocopherol	Launched				
D-limonene	Phase 1				
D-phenylalanine	Preclinical	enkephalinase inhibitor	CCBL1|CRH|HCAR3		
D-serine	Launched	glutamate receptor agonist	GLRA1|GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|SERPINB3		
D-157495	Preclinical	decapping scavenger enzyme inhibitor			
D-3263	Phase 1	transient receptor potential channel agonist			
D-4476	Preclinical	TGF beta receptor inhibitor	CSNK1A1|CSNK1D|TGFB1		
D-64131	Preclinical	microtubule inhibitor	TUBB		
D-7193	Phase 2				
DAA-1106	Preclinical	benzodiazepine receptor agonist	TSPO		
dabigatran	Launched	thrombin inhibitor	F2	neurology/psychiatry|hematology	stroke|systemic embolism|pulmonary embolism (PE)|deep vein thrombosis (DVT)
dabigatran-etexilate	Launched	thrombin inhibitor	F2	neurology/psychiatry|hematology	stroke|systemic embolism|pulmonary embolism (PE)|deep vein thrombosis (DVT)
dabrafenib	Launched	RAF inhibitor	BRAF|LIMK1|NEK11|RAF1|SIK1	oncology	melanoma
dacarbazine	Launched	DNA alkylating agent	PGD|POLA2	oncology|hematologic malignancy	melanoma|Hodgkin's lymphoma
dacinostat	Phase 1	HDAC inhibitor	HDAC1|HDAC2|HDAC3|HDAC4|HDAC5|HDAC6|HDAC7|HDAC8|HDAC9		
daclatasvir	Launched	HCV inhibitor		infectious disease	hepatitis C
dacomitinib	Launched	EGFR inhibitor	EGFR|ERBB2|ERBB4		
dactinomycin	Launched	RNA polymerase inhibitor	POLR2A	oncology	testicular carcinoma|Wilm's tumor|rhabdomyosarcoma|Ewing's sarcoma|gestational trophoblastic disease (GTD)
daidzein	Phase 2	estrogen receptor agonist	ESRRA|ESRRB|ESRRG|TRPC5		
daidzin	Phase 1	antioxidant	ALDH2		
dalargin	Phase 2	opioid receptor agonist	OPRM1		
dalbavancin	Launched	bacterial cell wall synthesis inhibitor	PNLIP	infectious disease	skin infections
dalcetrapib	Phase 3	cholesteryl ester transfer protein inhibitor	CETP		
dalfampridine	Launched	potassium channel blocker	KCNA1|KCNA10|KCNA2|KCNA3|KCNA4|KCNA5|KCNA6|KCNA7|KCNB1|KCNB2|KCNC1|KCNC2|KCNC3|KCNC4|KCND1|KCND2|KCND3|KCNF1|KCNG1|KCNG2|KCNG3|KCNG4|KCNH1|KCNH2|KCNH3|KCNH4|KCNH5|KCNH6|KCNH7|KCNH8|KCNJ13|KCNJ5|KCNQ1|KCNQ2|KCNQ3|KCNQ4|KCNQ5|KCNS1|KCNS2|KCNS3|KCNV1|KCNV2	neurology/psychiatry	multiple sclerosis
dalfopristin	Preclinical	antibacterial 			
daltroban	Phase 3	thromboxane receptor antagonist	TBXA2R		
daminozide	Preclinical	KDM2A inhibitor	KDM2A|KDM7A|PHF8		
danazol	Launched	estrogen receptor antagonist|progesterone receptor agonist	AR|CCL2|ESR1|GNRHR|GNRHR2|PGR	obstetrics/gynecology|cardiology	endometriosis|angioedema
danegaptide	Phase 2	gap junction modulator			
danirixin	Phase 2	CC chemokine receptor antagonist	CXCR2		
danofloxacin	Launched	bacterial DNA gyrase inhibitor		pulmonary	bovine respiratory disease (BRD)
danoprevir	Phase 3	HCV inhibitor			
dantrolene	Launched	calcium channel blocker	RYR1|RYR3	neurology/psychiatry|endocrinology	spasms|malignant hyperthermia (MH)
dantron	Withdrawn	laxative			
danusertib	Phase 2	Aurora kinase inhibitor|growth factor receptor inhibitor	AURKA|AURKB|AURKC|FGFR1|NTRK1|RET|SLK		
dapagliflozin	Launched	sodium/glucose cotransporter inhibitor	SLC5A1|SLC5A2	endocrinology	diabetes mellitus
dapansutrile	Phase 2	anti-inflammatory agent			
daphnetin	Preclinical	protein kinase inhibitor			
dapiprazole	Launched	adrenergic receptor antagonist	ADRA1A|ADRA1B|ADRA1D	ophthalmology	mydriasis
dapivirine	Phase 3	non-nucleoside reverse transcriptase inhibitor	CYP3A4|CYP3A5		
dapoxetine	Launched	selective serotonin reuptake inhibitor (SSRI)	HTR1A|HTR1B|HTR2C|SLC6A4	urology	premature ejaculation (PE)
daprodustat	Phase 3	hypoxia inducible factor inhibitor	EGLN1		
dapsone	Launched	bacterial antifolate	DHFR	dermatology|infectious disease	dermatitis herpetiformis (DH)|leprosy
DAPT	Preclinical	gamma secretase inhibitor			
daptomycin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	skin infections|endocarditis
darapladib	Phase 3	phospholipase inhibitor	PLA2G7		
darglitazone	Phase 2	PPAR receptor antagonist	PPARG		
darifenacin	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5	urology	urinary incontinence
darolutamide	Launched	androgen receptor antagonist	AR	oncology	prostate cancer
darunavir	Launched	HIV protease inhibitor	CYP3A4	infectious disease	human immunodeficiency virus (HIV-1)
darusentan	Phase 3	endothelin receptor antagonist	EDNRA		
dasabuvir	Launched	HCV inhibitor		infectious disease	hepatitis C
dasatinib	Launched	Bcr-Abl kinase inhibitor|ephrin inhibitor|KIT inhibitor|PDGFR tyrosine kinase receptor inhibitor|SRC inhibitor|tyrosine kinase inhibitor	ABL1|ABL2|BLK|EPHA2|FGR|FRK|FYN|HCK|KIT|LCK|LYN|PDGFRB|SRC|SRMS|STAT5B|YES1	hematologic malignancy	chronic myeloid leukemia (CML)|acute lymphoblastic leukemia (ALL)
dasotraline	Phase 3	dopamine-norepinephrine-serotonin reuptake inhibitor			
DAU-5884	Preclinical	acetylcholine receptor antagonist	CHRM3		
daucosterol	Phase 2	apoptosis stimulant			
daunorubicin	Launched	RNA synthesis inhibitor|topoisomerase inhibitor	TOP2A|TOP2B	hematologic malignancy	acute myeloid leukemia (AML)|acute lymphoblastic leukemia (ALL)
dazmegrel	Phase 2	thromboxane synthase inhibitor	TBXAS1		
dazoxiben	Phase 2	thromboxane synthase inhibitor	TBXAS1		
DBeQ	Preclinical	ATPase inhibitor	CASP3		
DBPR-211	Preclinical	cannabinoid receptor antagonist			
DBPR108	Phase 1	dipeptidyl peptidase inhibitor	DPP4		
DC-260126	Preclinical	free fatty acid receptor antagonist	FFAR1		
DCC-2618	Phase 1	KIT inhibitor|PDGFR tyrosine kinase receptor inhibitor	KIT|PDGFRA		
DCEBIO	Preclinical	potassium channel activator	KCNN2|KCNN3|KCNN4		
DCP-LA	Preclinical	protein kinase activator			
DCPIB	Preclinical	chloride channel blocker|gap junction modulator|glutamate inhibitor	SLC1A2		
DDR1-IN-1	Preclinical	discoidin domain receptor inhibitor	DDR1|DDR2		
deazaguanine	Preclinical	DNA synthesis inhibitor			
Debio-0932	Phase 1	HSP inhibitor			
debrisoquin	Launched	adrenergic neuron blocker	SLC6A2	cardiology	hypertension
decamethonium	Launched	acetylcholine receptor agonist	ACHE|CHRNA2	neurology/psychiatry	muscle relaxant
decamethoxine	Phase 2	antiseptic			
decernotinib	Phase 2/Phase 3	JAK inhibitor	JAK3		
decitabine	Launched	DNA methyltransferase inhibitor	DNMT1|DNMT3A	hematologic malignancy|hematology	myelodysplastic diseases (MDS)|anemia|chronic myeloid leukemia (CML)
declopramide	Preclinical	cell cycle inhibitor			
decloxizine	Preclinical	histamine receptor antagonist			
decoquinate	Launched	antiprotozoal agent		infectious disease	coccidiosis
defactinib	Phase 2	focal adhesion kinase inhibitor	PTK2		
deferasirox	Launched	chelating agent	CYP3A4	hematology	transfusional hemosiderosis|thalassemia|iron overload
deferasirox-iron-chelate	Launched				
deferiprone	Launched	chelating agent	UGT1A6	hematology	transfusional hemosiderosis|thalassemia|iron overload
deferoxamine-mesylate	Launched	chelating agent		hematology	acute iron intoxication|iron overload
deflazacort	Launched	glucocorticoid receptor agonist	NR3C1	rheumatology	joint inflammation
deforolimus	Phase 3	mTOR inhibitor	MTOR		
degarelix	Launched	gonadotropin releasing factor hormone receptor antagonist	GNRHR	oncology	prostate cancer
dehydroacetic-acid	Preclinical				
dehydrocholate	Preclinical				
dehydrocholate-acid	Preclinical				
dehydrocorydaline	Phase 3	acetylcholinesterase inhibitor	ACHE		
dehydroepiandrosterone	Launched	protein synthesis stimulant	ESR1|ESR2|G6PD|GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ|GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|GRIN3A|GRIN3B|HSD17B1|NR1I2|NR1I3|PPARA|SIGMAR1|SULT2A1|SULT2B1	endocrinology	menopause
dehydroepiandrosterone-sulfate	Launched	androgen receptor agonist|estrogen receptor agonist	AR|ESR1|ESR2	endocrinology	menopause
delafloxacin	Phase 3	antiinfective drug			
delamanid	Launched	bacterial cell wall synthesis inhibitor		infectious disease	tuberculosis
delanzomib	Phase 1/Phase 2	proteasome inhibitor	CMA1|CTSG|CYP3A4|ELANE		
delapril	Launched	angiotensin converting enzyme inhibitor	ACE	cardiology	hypertension
delavirdine	Launched	non-nucleoside reverse transcriptase inhibitor	CYP3A4	infectious disease	human immunodeficiency virus (HIV-1)
delcasertib	Phase 1	PKC inhibitor			
delgocitinib	Phase 2	JAK inhibitor			
delivert	Launched	angiotensin receptor agonist	AGTR1|AGTR2	critical care	sepsis
delpazolid	Phase 2	antibacterial			
delphinidin	Phase 2	membrane permeability inhibitor	GLO1		
delta-tocotrienol	Phase 1	HMGCR inhibitor	HMGCR		
deltarasin	Preclinical	phosphodiesterase inhibitor	KRAS		
demecarium	Launched	acetylcholinesterase inhibitor	ACHE|BCHE	ophthalmology	intraocular pressure|glaucoma
demeclocycline	Launched	bacterial 30S ribosomal subunit inhibitor		endocrinology|infectious disease|ophthalmology|urology	fever|respiratory tract infections|psittacosis|trachoma|conjunctivitis|urethritis|chancroid|cholera|syphilis|listeria|anthrax|actinomycosis|tularemia|brucellosis
denatonium-benzoate	Preclinical				
denopamine	Launched	adrenergic receptor agonist		cardiology	angina pectoris
denotivir	Launched	antiviral		infectious disease	virus herpes simplex (HSV)|skin infections
deoxyarbutin	Preclinical	tyrosinase inhibitor			
deoxycholic-acid	Launched	biliverdin reductase A activator|G protein-coupled receptor agonist	FPR1|GPBAR1	endocrinology	submental fat
deoxycorticosterone-acetate	Preclinical	progestogen hormone	NR3C2		
deoxyepinephrine	Preclinical	adrenergic receptor agonist|dopamine receptor agonist	ADRA1A|DRD1|DRD2		
deptropine	Preclinical	histamine receptor antagonist	HRH1		
dequalinium	Launched	PKC inhibitor	KCNN1|KCNN3	infectious disease	first-aid antiseptic
deracoxib	Launched	cyclooxygenase inhibitor	PTGS2	rheumatology	osteoarthritis
derazantinib	Phase 2	tyrosine kinase inhibitor			
deserpidine	Launched	angiotensin converting enzyme inhibitor	ACE|SLC18A2	cardiology	hypertension
desidustat	Preclinical	hypoxia inducible factor prolyl hydroxylase inhibitor			
desipramine	Launched	tricyclic antidepressant	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|ADRB1|ADRB2|CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|DRD2|HRH1|HTR1A|HTR2A|HTR2C|SLC6A2|SLC6A4|SMPD1	neurology/psychiatry	depression
desisobutyryl-ciclesonide	Launched	cytochrome P450 inhibitor		allergy	allergic rhinitis
deslanoside	Launched	Na/K-ATPase inhibitor	ATP1A1|ATP1A2|ATP1A3|ATP1A4|ATP1B1|ATP1B2|ATP1B3|FXYD2	cardiology	congestive heart failure|cardiac arrythmia
desloratadine	Launched	histamine receptor antagonist	HRH1	allergy	allergic rhinitis|urticaria
deslorelin	Phase 2	gonadotropin releasing factor hormone receptor agonist			
desmethylclozapine	Phase 2	acetylcholine receptor agonist	HTR2C		
desmopressin-acetate	Launched	vasopressin receptor agonist	AVPR1A|AVPR1B|AVPR2|OXTR	endocrinology|urology	central diabetes insipidus|nocturnal enuresis
desogestrel	Launched	progesterone receptor agonist	ESR1|PGR	endocrinology	contraceptive
desonide	Launched	glucocorticoid receptor agonist	NR3C1|PLA2G1B	gastroenterology	Crohn's disease
desoximetasone	Launched	glucocorticoid receptor agonist	NR3C1|PLA2G1B	dermatology	corticosteroid-responsive dermatoses
desoxycorticosterone-pivalate	Launched	corticosteroid agonist	NR3C2	endocrinology	Addison's disease
desoxycortone	Preclinical	mineralocorticoid receptor agonist	NR3C1|NR3C2		
desoxypeganine	Phase 1	acetylcholinesterase inhibitor|monoamine oxidase inhibitor	ACHE		
desvenlafaxine	Launched	serotonin–norepinephrine reuptake inhibitor (SNRI)	SLC6A2|SLC6A3|SLC6A4	neurology/psychiatry	depression
detomidine	Launched	adrenergic receptor agonist	ADRA2A	neurology/psychiatry	sedative
devazepide	Preclinical	CCK receptor antagonist			
dexamethasone	Launched	glucocorticoid receptor agonist	ANXA1|NOS2|NR0B1|NR3C1|NR3C2	endocrinology|rheumatology|allergy|gastroenterology|hematology|neurology/psychiatry|dermatology	hypercalcemia|rheumatoid arthritis|psoriatic arthritis|osteoarthritis|allergic rhinitis|ulcerative colitis|anemia|multiple sclerosis|enteritis|lupus|dermatitis herpetiformis (DH)|nephrotic syndrome|psoriasis
dexamethasone-acetate	Launched	glucocorticoid receptor agonist		endocrinology|rheumatology|allergy|gastroenterology|hematology|neurology/psychiatry|dermatology	hypercalcemia|rheumatoid arthritis|psoriatic arthritis|osteoarthritis|allergic rhinitis|ulcerative colitis|anemia|multiple sclerosis|enteritis|lupus|dermatitis herpetiformis (DH)|nephrotic syndrome|psoriasis
dexchlorpheniramine	Launched	histamine receptor antagonist		allergy|cardiology	allergic conjunctivitis|allergic rhinitis|urticaria|angioedema
dexfosfoserine	Preclinical	membrane integrity inhibitor	CFTR|GRM4|GRM6|GRM7|GRM8|KCNC4|PDPK1|PIM1|PRKACA|PRKCQ|PYGL|PYGM|REG1A|RHO|SERPINB3|SMAD2|TAOK2		
dexlansoprazole	Launched	ATPase inhibitor	ATP4A	gastroenterology	gastroesophageal reflux disease (GERD)|erosive esophagitis (EE)
dexloxiglumide	Phase 3	CCK receptor antagonist	CCKAR		
dexmedetomidine	Launched	adrenergic receptor agonist	ADRA2A|ADRA2B|ADRA2C	neurology/psychiatry	sedative
dexniguldipine	Phase 2	calmodulin antagonist	ADORA3		
dexpanthenol	Launched			gastroenterology	paralytic ileus
dexrazoxane	Launched	chelating agent|topoisomerase inhibitor	TOP2A|TOP2B	cardiology	cardiomyopathy
dextran	Launched			hematology|critical care	thrombosis|hypovolemia
dextromethorphan	Launched	glutamate receptor antagonist|sigma receptor agonist	CHRNA2|CHRNA3|CHRNA4|CHRNA7|CHRNB2|CHRNB4|CYBA|CYBB|GRIN3A|NCF1|NCF2|NCF4|OPRD1|OPRK1|OPRM1|PGRMC1|RAC1|RAC2|SIGMAR1|SLC6A2|SLC6A4	pulmonary	cough suppressant
dextrorotation-nimorazole-phosphate-ester	Preclinical	antiinfective drug			
dextrose	Launched			endocrinology	hypoglycemia
DFB	Preclinical	glutamate receptor agonist	GRM5		
DG-172	Preclinical	PPAR receptor inverse agonist	PPARD		
DG051	Preclinical	leukotriene synthesis inhibitor			
DH-97	Preclinical	melatonin receptor antagonist	MTNR1B		
DHBP	Preclinical	ryanodine receptor blocker			
diacerein	Launched	interleukin inhibitor	IL1B	rheumatology	osteoarthritis
diacetamate	Preclinical				
diadenosine-tetraphosphate	Phase 1	adenosine kinase inhibitor	P2RY13|P2RY2		
dianhydrogalactitol	Phase 3	DNA alkylating agent			
diarylpropionitrile	Preclinical	estrogen receptor agonist	ESR2		
diatrizoic-acid	Launched			radiology	contrast agent
diaveridine	Launched	dihydrofolate reductase inhibitor		infectious disease	coccidiosis
diazoxide	Launched	potassium channel activator	ATP1A1|CA1|CA2|KCNJ11|KCNJ8|KCNMA1|SLC12A3	endocrinology	hypoglycemia
dibekacin	Launched	bacterial 30S ribosomal subunit inhibitor		infectious disease	gram-negative bacterial infections
dibenzepine	Preclinical	norepinephrine reputake inhibitor			
dibenzothiophene	Preclinical				
dibutyl-phthalate	Preclinical		TRPA1		
dichlorisone-acetate	Phase 2				
dichloroacetate	Phase 3	pyruvate dehydrogenase kinase inhibitor			
dichlorophen	Launched	anticestodal agent		infectious disease	hookworm|tapeworm
dichlorvos	Launched	acetylcholinesterase inhibitor			
diclazuril	Launched	antiprotozoal agent		infectious disease	equine protozoal myeloencephalitis (EPM)
diclofenac	Launched	cyclooxygenase inhibitor	AKR1C3|ALOX5|ASIC1|ASIC3|KCNQ2|KCNQ3|PLA2G2A|PPARG|PTGS1|PTGS2|SCN4A	rheumatology|neurology/psychiatry	rheumatoid arthritis|osteoarthritis|migraine headache
diclofenamide	Launched	carbonic anhydrase inhibitor	CA1|CA12|CA2|CA4|CA7	ophthalmology|neurology/psychiatry	glaucoma|epilepsy
diclofensine	Phase 3	dopamine reuptake inhibitor	DRD1|MAOA|MAOB		
dicloralurea	Preclinical				
dicloxacillin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-positive bacterial infections
dicoumarol	Launched	NADPH inhibitor	CRYZ|NQO1|VKORC1	hematology	deep vein thrombosis (DVT)
dicyclohexylamine	Preclinical				
dicycloverine	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3	gastroenterology	irritable bowel syndrome
didanosine	Launched	nucleoside reverse transcriptase inhibitor	PNP	infectious disease	human immunodeficiency virus (HIV-1)
dideoxyadenosine	Phase 1	nucleoside reverse transcriptase inhibitor			
didox	Launched	ribonucleotide reductase inhibitor	RRM1	oncology	breast cancer
dienestrol	Launched	estrogen receptor agonist	ESR1	endocrinology	menopause
dienogest	Launched	progesterone receptor agonist	PGR	endocrinology|obstetrics/gynecology	contraceptive|endometriosis
diethylcarbamazine	Launched	lipoxygenase inhibitor	ALOX5|PTGS1	infectious disease	filariasis
diethylstilbestrol	Withdrawn	estrogen receptor agonist	ESR1|ESR2|ESRRB|ESRRG		
diethyltoluamide	Launched	ionotropic receptor IR40a activator		dermatology	sunscreen lotion
difenpiramide	Launched	cyclooxygenase inhibitor|prostaglandin inhibitor		neurology/psychiatry	pain relief
diflorasone-diacetate	Launched	glucocorticoid receptor agonist	NR3C1	dermatology	corticosteroid-responsive dermatoses
difloxacin	Launched	bacterial DNA gyrase inhibitor		infectious disease	skin infections|urinary tract infections
diflunisal	Launched	prostanoid receptor antagonist	PTGS1|PTGS2	rheumatology	rheumatoid arthritis|osteoarthritis
difluprednate	Launched	glucocorticoid receptor agonist	NR3C1	ophthalmology	endogenous uveitis
diftalone	Launched	cyclooxygenase inhibitor		endocrinology	thyroiditis
digitoxigenin	Preclinical	ATPase inhibitor	ATP1A1		
digitoxin	Launched	ATPase inhibitor	ATP1A1|ATP1A2|ATP1A3|ATP1A4|ATP1B1|ATP1B2|ATP1B3|FXYD2	cardiology	congestive heart failure|cardiac arrythmia
digoxigenin	Preclinical	steroid			
digoxin	Launched	ATPase inhibitor	ATP1A1	cardiology	congestive heart failure|atrial fibrillation (AF)
dihomo-gamma-linolenic-acid	Phase 2	prostanoid receptor agonist	PTGS1|PTGS2		
dihydrexidine	Phase 2	dopamine receptor agonist	DRD1|DRD2|DRD3|DRD4|DRD5		
dihydroartemisinin	Launched	antimalarial agent		infectious disease	malaria
dihydroergocristine	Launched	adrenergic receptor antagonist|prolactin inhibitor	ADRA1A|ADRB1|DRD1|DRD2|DRD3|DRD4|DRD5|HTR1A|HTR2A|HTR3A|HTR4|HTR5A|HTR6|HTR7	neurology/psychiatry	senile dementia|cerebrovascular insufficiency
dihydroergotamine	Launched	serotonin receptor agonist	ADRA2A|DRD2|HTR1B|HTR1D|HTR1E|HTR1F|HTR2B|HTR7	neurology/psychiatry	migraine headache
dihydromyricetin	Preclinical				
dihydrostreptomycin	Withdrawn	bacterial 30S ribosomal subunit inhibitor			
dihydrotachysterol	Launched	vitamin analog	VDR	orthopedics|endocrinology	rickets|hypocalcemia|osteomalacia
dihydroxyacetone	Launched			dermatology	skin protectant
dihydroxyphenylglycine	Preclinical	glutamate receptor agonist	GRM1|GRM5		
diiodothyropropionic-acid	Phase 2	thyroid hormone stimulant			
dilazep	Launched	adenosine reuptake inhibitor	SLC29A1	cardiology	coronary heart disease
dilmapimod	Phase 1	p38 MAPK inhibitor			
diloxanide	Launched	protein synthesis inhibitor		infectious disease	amebiasis
diltiazem	Launched	calcium channel blocker	CACNA1C|CACNA1S|CACNA2D1|CACNG1|HTR3A|KCNA5	cardiology	hypertension|angina pectoris
DIM-C-pPhCO2Me	Preclinical	nuclear receptor antagonist			
dimaprit	Preclinical	histamine receptor agonist	HRH2|HRH3|HRH4		
dimemorfan	Launched	sigma receptor agonist	SIGMAR1	pulmonary	cough suppressant
dimenhydrinate	Launched	histamine receptor antagonist	HRH1	neurology/psychiatry|gastroenterology	motion sickness|nausea|vomiting
dimercaprol	Launched	chelating agent		neurology/psychiatry	metal toxicity
dimercaptosuccinic-acid	Launched	chelating agent	DNMT1	neurology/psychiatry	metal toxicity
dimesna	Phase 3	tubulin polymerization inhibitor			
dimethadione	Preclinical	oxazolidine antiepileptic			
dimethicone	Launched			dermatology	cosmetic
dimethindene-(S)-(+)	Preclinical	acetylcholine receptor antagonist	HRH1		
dimethisoquin	Launched	local anesthetic		neurology/psychiatry	local anesthetic
dimethyl-fumarate	Launched	nuclear factor erythroid derived|like (NRF2) activator	KEAP1	neurology/psychiatry	multiple sclerosis
dimethyl-isosorbide	Preclinical	cosmetic moisturizer			
dimetindene	Launched	cholinergic receptor antagonist|histamine receptor antagonist	HRH1	allergy	allergic rhinitis
dimetridazole	Launched	bacterial DNA inhibitor		infectious disease	protozoan infection
diminazene-aceturate	Phase 3	angiotensin converting enzyme activator	AOC1|PRDX5|PRSS1		
dimpylate	Launched	acetylcholinesterase inhibitor	ACHE	infectious disease	flea control
dinaciclib	Phase 3	CDK inhibitor	CDK1|CDK2|CDK5|CDK9		
dinitolmide	Launched			infectious disease	coccidiosis
dinoprost	Launched	prostacyclin analog	PTGDR|PTGDR2|PTGER1|PTGER2|PTGER3|PTGER4|PTGFR|TBXA2R	obstetrics/gynecology	labor induction
dinoprostone	Withdrawn	prostanoid receptor agonist	CATSPER1|CATSPER2|CATSPER3|CATSPER4|PTGDR|PTGDR2|PTGER1|PTGER2|PTGER3|PTGER4|PTGFR|TBXA2R		
dioscin	Preclinical	apoptosis stimulant	CXCR3		
diosgenin	Preclinical	steroid			
diosmetin	Launched	aryl hydrocarbon receptor agonist	CYP1B1	dermatology	cosmetic
diosmin	Launched	aryl hydrocarbon receptor agonist|capillary stabilizing agent	AHR	cardiology|hematology|dermatology	chronic venous insufficiency (CVI)|edema|deep vein thrombosis (DVT)|statis dermatitis|heavy leg syndrome
dioxybenzone	Preclinical	topical sunscreen agent			
dipeptamin	Launched				
diperodon	Preclinical	local anesthetic			
diphemanil	Launched	acetylcholine receptor antagonist	CHRM3	neurology/psychiatry	spasms
diphencyprone	Phase 2	immunostimulant			
diphenhydramine	Launched	histamine receptor antagonist	HRH1	neurology/psychiatry	headache
diphenidol	Launched	acetylcholine receptor agonist	CHRM1|CHRM2|CHRM3|CHRM4	neurology/psychiatry	vertigo
diphenyleneiodonium	Preclinical	nitric oxide synthase inhibitor	NOS2|NOS3		
diphenylguanidine	Preclinical				
diphenylpyraline	Launched	dopamine reuptake inhibitor	HRH1|SLC6A3	allergy	allergic rhinitis
dipivefrine	Launched	adrenergic receptor agonist		ophthalmology	glaucoma|intraocular pressure
dipraglurant	Phase 2	glutamate receptor negative allosteric modulator	GRM5		
DIPT	Launched	dopamine reuptake inhibitor|serotonin reuptake inhibitor	HTR1A|HTR2A|HTR2C		
dipyridamole	Launched	phosphodiesterase inhibitor	ADA|PDE10A|PDE1A|PDE1B|PDE1C|PDE2A|PDE3A|PDE3B|PDE4A|PDE4B|PDE4C|PDE4D|PDE5A|PDE6A|PDE6B|PDE6C|PDE6D|PDE6G|PDE6H|PDE7A|PDE7B|PDE8A|PDE8B|PDE9A|SLC29A1	cardiology	coronary artery disease (CAD)|peripheral artery disease (PAD)|hypertension
dipyrocetyl	Launched	chelating agent		endocrinology|neurology/psychiatry	fever|pain relief
diquafosol	Phase 3	purinergic receptor activator			
dirithromycin	Launched	bacterial 50S ribosomal subunit inhibitor		pulmonary	bronchitis
diroximel-fumarate	Phase 3	anti-inflammatory agent			
disodium-sebacate	Phase 1		HBB		
disopyramide	Launched	sodium channel blocker	CHRM1|CHRM2|CHRM3|KCND2|KCND3|KCNH2|SCN5A	cardiology	ventricular tachycardia (VT)|ventricular arrhythmias
disulfiram	Launched	aldehyde dehydrogenase inhibitor|DNA methyltransferase inhibitor|TRPV agonist	ALDH2|DBH	neurology/psychiatry	abstinence from alcohol
dithranol	Launched	DNA synthesis inhibitor		dermatology	psoriasis
ditiocarb-sodium-trihydrate	Phase 3	immunostimulant	CA1|CA2|CA4		
ditolylguanidine	Preclinical	sigma receptor agonist	GRIN1|GRIN2A|GRIN2B|SIGMAR1		
dixanthogen	Preclinical				
dixyrazine	Preclinical	antipsychotic			
dizocilpine-(+)	Preclinical	glutamate receptor antagonist	GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D		
dizocilpine-(-)	Phase 1	glutamate receptor antagonist			
DMAB-anabaseine	Preclinical	adrenergic receptor agonist	CHRNA7		
DMeOB	Preclinical	glutamate receptor modulator	GRM5		
DMH1	Preclinical	ALK tyrosine kinase receptor inhibitor	ACVR1		
DMH4	Preclinical	VEGFR inhibitor	KDR		
DMNB	Preclinical	DNA dependent protein kinase inhibitor			
DMP-543	Phase 2	acetylcholine release enhancer			
DMP-777	Phase 2	elastase inhibitor	MPO		
DMPS	Phase 1	chelating agent			
DMSO	Preclinical	control vehicle			
DNQX	Preclinical	glutamate receptor antagonist	GRIA1|GRIA2|GRIK1|GRIN1|GRIN2A|GRIN2B		
dobutamine	Launched	adrenergic receptor agonist	ADRB1|ADRB2	cardiology	congestive heart failure
docebenone	Phase 2	lipoxygenase inhibitor	ALOX5		
docetaxel	Launched	tubulin polymerization inhibitor	BCL2|MAP2|MAP4|MAPT|NR1I2|TUBA1A|TUBA1B|TUBA1C|TUBA3C|TUBA3D|TUBA3E|TUBA4A|TUBB|TUBB1|TUBB2A|TUBB2B|TUBB3|TUBB4A|TUBB4B|TUBB6|TUBB8	oncology	breast cancer|non-small cell lung cancer (NSCLC)|prostate cancer|gastric adenocarcinoma|head and neck squamous cell carcinoma (HNSCC)
doconexent	Launched	PPAR receptor agonist	FFAR1|PTGS1|PTGS2		
doconexent-ethyl-ester	Launched	omega 3 fatty acid stimulant		endocrinology	hypertriglyceridemia
docosanol	Launched	lipase clearing factor inhibitor	TLR7	dental	cold sore
docusate	Launched	laxative		gastroenterology	constipation
dodecyl-sulfate	Preclinical		LYZ		
dofequidar	Phase 3	MRP inhibitor|P glycoprotein inhibitor	ABCB1		
dofetilide	Withdrawn	potassium channel blocker	KCNH1|KCNH2|KCNJ12|KCNK2		
dolasetron	Launched	serotonin receptor antagonist	HTR3A	gastroenterology	nausea|vomiting
dolastatin-10	Phase 2	tubulin polymerization inhibitor	TUBB		
dolutegravir	Launched	HIV integrase inhibitor	CYP3A4|CYP3A5|CYP3A7|POU2F2|UGT1A1	infectious disease	human immunodeficiency virus (HIV-1)
domiphen	Preclinical				
domperidone	Launched	dopamine receptor antagonist	DRD2|DRD3	infectious disease	fescue toxicosis
donepezil	Launched	acetylcholinesterase inhibitor	ACHE	neurology/psychiatry	Alzheimer's disease
donitriptan	Phase 2	serotonin receptor agonist	HTR1A|HTR1B|HTR1D|HTR1E|HTR1F|HTR2A|HTR5A|HTR6		
dopamine	Launched	dopamine receptor agonist	DBH|DRD1|DRD2|DRD3|DRD4|DRD5|HTR1A|HTR7|SLC6A2|SLC6A3|SLC6A4	cardiology|neurology/psychiatry	ventricular arrhythmias|depression|headache|tremors
doramapimod	Phase 2	p38 MAPK inhibitor	MAPK11|MAPK12|MAPK13|MAPK14		
doramectin	Launched			infectious disease	gastrointestinal roundworms
doravirine	Launched	non-nucleoside reverse transcriptase inhibitor			
doripenem	Launched	bacterial cell wall synthesis inhibitor	DPEP1	infectious disease	intra-abdominal infections|urinary tract infections|pyelonephritis
dorsomorphin	Preclinical	AMPK inhibitor	ACVR1|BMPR1A|BMPR1B|EPHA2|FKBP1A|FLT1|FLT3|KDR|LCK|MKNK1|PRKAA1|RPS6KA1|SRC		
dorzolamide	Launched	carbonic anhydrase inhibitor	CA1|CA12|CA14|CA2|CA4|CA7	ophthalmology	intraocular pressure|glaucoma
dosulepin	Launched	norepinephrine reuptake inhibitor|serotonin–norepinephrine reuptake inhibitor (SNRI)|tricyclic antidepressant	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|HRH1|SLC6A2|SLC6A4	neurology/psychiatry	depression
DOTMP	Preclinical				
dovitinib	Phase 3	EGFR inhibitor|FGFR inhibitor|FLT3 inhibitor|PDGFR tyrosine kinase receptor inhibitor|VEGFR inhibitor	CSF1R|EGFR|FGFR1|FGFR2|FGFR3|FLT1|FLT3|FLT4|INSR|KDR|KIT|PDGFRA|PDGFRB		
doxapram	Launched	potassium channel blocker		pulmonary|neurology/psychiatry	respiratory depression|central nervous system depression|acute hypercapnia (AHC)
doxazosin	Launched	adrenergic receptor antagonist	ADRA1A|ADRA1B|ADRA1D	urology|cardiology	benign prostatic hyperplasia (BPH)|hypertension
doxepin	Launched	histamine receptor antagonist	HRH1|SLC6A2|SLC6A4	neurology/psychiatry	depression|anxiety
doxercalciferol	Launched	vitamin D receptor agonist	VDR	nephrology|endocrinology	chronic kidney disease (CKD)|hyperparathyroidism
doxifluridine	Launched	thymidylate synthase inhibitor	TYMS	oncology	colorectal cancer
doxofylline	Launched	adenosine receptor antagonist	ADORA1|PDE4A|PDE4B|PDE4C|PDE4D	pulmonary	asthma
doxorubicin	Launched	topoisomerase inhibitor	TOP2A	hematologic malignancy|oncology	acute lymphoblastic leukemia (ALL)|acute myeloid leukemia (AML)|Wilm's tumor|breast cancer|ovarian cancer|Hodgkin's lymphoma|bladder cancer|multiple myeloma
doxycycline	Launched	bacterial 30S ribosomal subunit inhibitor|metalloproteinase inhibitor	MMP8	dental	periodontitis
doxylamine	Launched	histamine receptor antagonist	HRH1	neurology/psychiatry	sedative
DpC	Phase 1				
DPC-681	Phase 1	HIV protease inhibitor			
DPCPX	Phase 1	adenosine receptor antagonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
DPI-201106	Phase 2	sodium channel activator	ADRB2		
DPO-1	Preclinical	potassium channel blocker	KCNA5		
DPPE	Phase 3	histamine receptor antagonist	ABCB1|HRH1		
DQP-1105	Preclinical	glutamate receptor antagonist	GRIN2C|GRIN2D		
DR-2313	Preclinical	PARP inhibitor	PARP1|PARP3		
DR-4485	Preclinical	serotonin receptor antagonist	HTR7		
DRF053-(R)	Preclinical	CDK inhibitor	CSNK1A1		
drofenine	Launched			neurology/psychiatry	spasms
droloxifene	Phase 3	selective estrogen receptor modulator (SERM)	ESR1		
dromostanolone-propionate	Launched	androgen receptor modulator	AR	oncology	breast cancer
dronedarone	Launched	adrenergic receptor antagonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|ADRB1|CACNA1C|CACNA1D|CACNA1F|CACNA1S|CACNB1|CACNB2|CACNB3|CACNB4|KCNA5|KCNH2|KCNK2|SCN1A	cardiology	atrial fibrillation (AF)
droperidol	Launched	dopamine receptor antagonist	ADRA1A|DRD2|DRD3|DRD4|HTR2A	gastroenterology	nausea|vomiting
dropropizine	Launched	antitussive		pulmonary	cough suppressant
drospirenone	Launched	mineralocorticoid receptor antagonist	AR|NR3C2|PGR	endocrinology	contraceptive
drotaverine	Launched	phosphodiesterase inhibitor		obstetrics/gynecology	labor induction
droxicam	Launched	cyclooxygenase inhibitor	PTGS1	rheumatology	rheumatoid arthritis|osteoarthritis
droxidopa	Launched	norepinephrine precursor	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|ADRB1|ADRB2|ADRB3|PAH	cardiology|neurology/psychiatry	hypertension|Parkinson's Disease
droxinostat	Preclinical	HDAC inhibitor	HDAC6|HDAC8		
DSM265	Phase 2	dihydroorotate dehydrogenase inhibitor			
DSPC	Preclinical				
DSR-6434	Preclinical	toll-like receptor agonist	TLR7		
DS2-(806622)	Preclinical				
DU-728	Phase 1	structural glycoprotein antagonist	ITGA2B|ITGB3		
duloxetine	Launched	norepinephrine reuptake inhibitor|serotonin–norepinephrine reuptake inhibitor (SNRI)	HTR2A|HTR2C|HTR6|SLC6A2|SLC6A3|SLC6A4	neurology/psychiatry	depression|generalized anxiety disorder (GAD)|muscle pain|peripheral neuropathy
DUP-697	Phase 1	cyclooxygenase inhibitor	PTGS2		
dutasteride	Launched	5 alpha reductase inhibitor	SRD5A1|SRD5A2|SRD5A3	urology	benign prostatic hyperplasia (BPH)
duvelisib	Launched	PI3K inhibitor	PIK3CA|PIK3CB|PIK3CD|PIK3CG		
DVD-111	Phase 2				
DWK-1339	Preclinical	beta amyloid aggregation inhibitor			
dyclonine	Launched	sodium channel blocker	SCN10A|SCN5A	neurology/psychiatry	local anesthetic
dydrogesterone	Launched	progesterone receptor agonist	PGR	obstetrics/gynecology	infertility
dynasore	Preclinical	dynamin inhibitor	DNM1|DNM1L|DNM2		
dynole-34-2	Preclinical	dynamin inhibitor	DNM1		
dyphylline	Launched	adenosine receptor antagonist|phosphodiesterase inhibitor	PDE4A	pulmonary	asthma|bronchitis|emphysema
DY131	Preclinical	estrogen-related receptor agonist	ESRRB|ESRRG		
D609	Preclinical	phospholipase inhibitor			
E-2001	Preclinical	antioxidant			
E-2012	Phase 1	gamma secretase modulator	APH1A|APH1B|PSENEN		
E-4031	Phase 1	potassium channel blocker	KCNH1|KCNH2		
E-64	Preclinical	calpain inhibitor|cysteine protease inhibitor	CTSS		
eact	Preclinical	calcium-activated chloride channel inhibitor	ANO1		
EB-47	Preclinical	PARP inhibitor	PARP1		
ebastine	Launched	histamine receptor antagonist	CYP3A4|HRH1	allergy	allergic rhinitis|urticaria
EBPC	Preclinical	aldose reductase inhibitor	AKR1B1		
ebrotidine	Withdrawn	histamine receptor antagonist	HRH2		
ebselen	Phase 2/Phase 3	cyclooxygenase inhibitor|glutathione peroxidase agonist|H+/K+-ATPase inhibitor|nitric oxide synthase inhibitor	ALB		
EC-144	Preclinical	HSP inhibitor	HSP90AA1|HSP90AB1		
EC-23	Preclinical	retinoid receptor agonist	RARA|RARB|RARG		
ecabapide	Phase 3				
ecabet	Launched	gastrin inhibitor|urease inhibitor	NOXO1	ophthalmology	dry eye syndrome
ecamsule-triethanolamine	Launched			dermatology	skin protectant|sunscreen lotion
echinomycin	Phase 2	DNA intercalating agent			
econazole	Launched	lanosterol demethylase inhibitor|sterol demethylase inhibitor	NPY1R|NPY2R|TRPM2|TRPV5	infectious disease	tinea pedis|tinea cruris|tinea corporis|tinea versicolor|cutaneous candidiasis
ectoine	Launched	anti-inflammatory agent			
edaglitazone	Phase 2	PPAR receptor agonist	PPARG		
edaravone	Launched	nootropic agent	BCL2	neurology/psychiatry	stroke
edasalonexent	Phase 3	NFkB pathway inhibitor			
edelfosine	Phase 2	phospholipase inhibitor			
editol	Preclinical				
EDO-S101	Phase 1/Phase 2	HDAC inhibitor			
edonerpic-maleate	Preclinical	beta amyloid inhibitor			
edoxaban	Launched	coagulation factor inhibitor	F10	neurology/psychiatry|hematology|cardiology	stroke|pulmonary embolism (PE)|systemic embolism|deep vein thrombosis (DVT)|atrial fibrillation (AF)
edoxudine	Launched	DNA directed DNA polymerase inhibitor		infectious disease	virus herpes simplex (HSV)
edrophonium	Launched	acetylcholinesterase inhibitor	ACHE|BCHE	neurology/psychiatry	myasthenia gravis
EDTMP	Preclinical	chelating agent			
EED226	Preclinical	polycomb protein inhibitor	EED		
efaproxiral	Phase 3	hemoglobin oxygen release stimulant	HBA1|HBB		
efaroxan	Phase 2	adrenergic receptor antagonist	ADORA2A		
efatutazone	Phase 2	PPAR receptor agonist	PPARG		
efavirenz	Launched	HIV protease inhibitor	CYP1A2|CYP2B6|CYP2C19|CYP2C9|CYP2D6|CYP3A4	infectious disease	human immunodeficiency virus (HIV-1)
efinaconazole	Launched	lanosterol demethylase inhibitor	CYP51A1	infectious disease	onychomycosis
efletirizine	Phase 3	antihistamine			
eflornithine	Launched	ornithine decarboxylase inhibitor	ARG2|ODC1	dermatology	facial hair reduction
efloxate	Preclinical	vasodilator			
efonidipine	Launched	calcium channel blocker		cardiology	hypertension
EF5	Phase 2	cytochrome P450 activator			
EGF816	Phase 2	EGFR inhibitor	EGFR		
eglumetad	Phase 2	glutamate receptor agonist	GRM2|GRM3|GRM6|GRM8		
EG00229	Preclinical	neuropilin receptor antagonist	NRP1		
EHop-016	Preclinical	Ras GTPase inhibitor	RAC1|RAC3		
EIPA	Preclinical	sodium/hydrogen exchanger inhibitor|transient receptor potential polycystic inhibitor	ADRA2A|ASIC1|PKD2L1		
EIT-hydrobromide	Preclinical	nitric oxide synthase inhibitor	NOS2|NOS3		
EI1	Preclinical	histone lysine methyltransferase inhibitor	EZH2		
elacestrant	Phase 3	estrogen receptor degrader			
elacridar	Phase 1	P glycoprotein inhibitor	ABCB1		
elactocin	Phase 1	exportin antagonist	XPO1		
elacytarabine	Phase 3	antineoplastic agent	DCK		
elafibranor	Phase 3	PPAR receptor agonist	PPARA|PPARD|PPARG		
elagolix	Launched	gonadotropin releasing factor hormone receptor antagonist	GNRHR		
elbasvir	Launched	HCV inhibitor		infectious disease	hepatitis C
eldecalcitol	Phase 3	bone formation stimulant	VDR		
eleclazine	Phase 3	late sodium current inhibitor			
elemene	Phase 3	VEGFR inhibitor			
elesclomol	Phase 3	oxidative stress inducer	HSPA1A		
eletriptan	Launched	serotonin receptor agonist	HTR1A|HTR1B|HTR1D|HTR1E|HTR1F|HTR2B|HTR7	neurology/psychiatry	migraine headache
eliglustat	Launched	glycosyl transferase inhibitor	UGCG	hematology	Gaucher disease
elinogrel	Phase 2	purinergic receptor antagonist	P2RY12		
eliprodil	Phase 3	glutamate receptor antagonist	GRIN1|GRIN2B		
ellagic-acid	Phase 2	glutathione transferase inhibitor|non-nucleoside reverse transcriptase inhibitor	CA1|CA12|CA14|CA2|CA3|CA4|CA5A|CA5B|CA6|CA7|CA9|CSNK2A1|GSK3B|PRKACA|PRKCA|PRKCB|SQLE|SYK		
ELN-441958	Preclinical	bradykinin receptor antagonist	BDKRB1		
eltanexor	Preclinical	exportin inhibitor			
eltanolone	Phase 3	GABA receptor positive allosteric modulator	GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB2|GABRG2		
eltoprazine	Phase 2	serotonin receptor agonist	HTR1A|HTR1B		
eltrombopag	Launched	thrombopoietin receptor agonist	MPL	hematology|infectious disease	anemia|hepatitis C|thrombocytopenia
eluxadoline	Launched	opioid receptor agonist|opioid receptor antagonist	OPRD1|OPRK1|OPRM1	gastroenterology	irritable bowel syndrome
elvitegravir	Launched	HIV integrase inhibitor		infectious disease	human immunodeficiency virus (HIV-1)
emamectin	Preclinical	GABA receptor agonist			
embelin	Preclinical	HCV inhibitor|XIAP inhibitor	XIAP		
EMD-1214063	Phase 2	hepatocyte growth factor receptor inhibitor	MET		
EMD-386088	Preclinical	serotonin receptor agonist	HTR6		
EMD-53998	Phase 1	phosphodiesterase inhibitor	TNNC1		
EMD-66684	Preclinical	angiotensin receptor antagonist	AGTR1		
EMD534085	Preclinical	kinesin inhibitor			
emedastine	Launched	histamine receptor antagonist	HRH1	ophthalmology	conjunctivitis
emeramide	Phase 2	antioxidant			
emetine	Phase 2	protein synthesis inhibitor	RPS2		
emiglitate	Preclinical	alpha glucoside inhibitor			
emixustat	Phase 3	retinoid isomerohydrolase inhibitor			
emodepside	Phase 1	nematocide			
emodin	Preclinical	11-beta hydroxysteroid dehydrogenase inhibitor	CSNK2A1		
emorfazone	Launched	anti-inflammatory agent|cyclooxygenase inhibitor		dental	mouth inflammation
emoxipin	Phase 3				
empagliflozin	Launched	sodium/glucose cotransporter inhibitor	SLC5A1|SLC5A2	endocrinology	diabetes mellitus
emricasan	Phase 2	caspase inhibitor	CASP1|CASP3|CASP7		
emtricitabine	Launched	nucleoside reverse transcriptase inhibitor		infectious disease	human immunodeficiency virus (HIV-1)
enalapril	Launched	angiotensin converting enzyme inhibitor	ACE	cardiology	hypertension|congestive heart failure|left ventricular systolic dysfunction (LVSD)
enalaprilat	Launched	angiotensin converting enzyme inhibitor	ACE	cardiology	hypertension
enasidenib	Launched	isocitrate dehydrogenase inhibitor	IDH1	hematologic malignancy	acute myeloid leukemia (AML)
enbucrilate	Launched			dermatology	skin lacerations|tissue adhesive
enciprazine	Phase 3	GABA receptor modulator	GABRA1		
encorafenib	Launched	RAF inhibitor	BRAF	oncology	melanoma
endo-IWR-1	Preclinical	PARP inhibitor	TNKS|TNKS2		
endoxifen	Phase 2	estrogen receptor antagonist	ESR1		
enflurane	Launched	membrane permeability inhibitor	GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ|GLRA1|GLRB|KCNK10|KCNK18|KCNK2|KCNK3|KCNK9	neurology/psychiatry	anesthetic
enilconazole	Launched	sterol demethylase inhibitor	CYP19A1|CYP1A2|CYP2B6|CYP2C9|CYP2J2|CYP3A4|CYP3A5|NR1I2|PPARA|PTGER2	infectious disease	skin infections
eniluracil	Phase 3	dihydropyrimidine dehydrogenase inhibitor	AOX1|DPYD|XDH		
eniporide	Preclinical	sodium/hydrogen antiport inhibitor			
enisamium-iodide	Launched				
ENMD-2076	Phase 2	Aurora kinase inhibitor|FLT3 inhibitor|VEGFR inhibitor	AURKA|FLT3|KDR|PDGFRA|PTK2|SRC		
enocitabine	Launched	DNA synthesis inhibitor	CMPK1|RRM1|TYMS	hematologic malignancy	acute myeloid leukemia (AML)
enoxacin	Launched	topoisomerase inhibitor	TOP2A	infectious disease	urinary tract infections|gonorrhea
enoximone	Launched	phosphodiesterase inhibitor	PDE3A	cardiology	congestive heart failure
enoxolone	Launched	gap junction modulator	HSD11B1	gastroenterology|otolaryngology	peptic ulcer disease (PUD)|common cold
enprofylline	Phase 3	phosphodiesterase inhibitor	ADORA1|ADORA2A|ADORA2B|ADORA3|PDE4A|PDE4B		
enrofloxacin	Launched	bacterial DNA gyrase inhibitor		infectious disease	gram-negative bacterial infections
entacapone	Launched	catechol O methyltransferase inhibitor	COMT	neurology/psychiatry	Parkinson's Disease
entasobulin	Preclinical	tubulin polymerization inhibitor			
entecavir	Launched	DNA replication inhibitor|nucleoside reverse transcriptase inhibitor		infectious disease	hepatitis B
entinostat	Phase 3	HDAC inhibitor	HDAC1|HDAC2|HDAC3|HDAC9		
entrectinib	Launched	ALK tyrosine kinase receptor inhibitor|proto-oncogene tyrosine protein kinase inhibitor	ALK|NTRK1|NTRK2|NTRK3|ROS1	oncology	non-small cell lung cancer (NSCLC)
enzalutamide	Launched	androgen receptor antagonist	AR	oncology	prostate cancer
enzastaurin	Phase 3	PKC inhibitor	AKT1|GSK3B|PRKCA|PRKCB|PRKCD|PRKCG		
EN460	Preclinical	endoplasmic reticulum oxidation inhibitor	ERO1A		
EO-1428	Preclinical	p38 MAPK inhibitor	MAPK11|MAPK14		
epacadostat	Phase 3	"indoleamine 2,3-dioxygenase inhibitor"	IDO1		
epalrestat	Launched	aldose reductase inhibitor	AKR1B1	nephrology	diabetic nephropathy
eperezolid	Phase 1	bacterial 30S ribosomal subunit inhibitor			
eperisone	Launched	acetylcholine receptor antagonist	CYP2J2	neurology/psychiatry	amyotrophic lateral sclerosis (ALS)|spasms|head injury|spinal injury
epetraborole	Preclinical	leucyl-tRNA synthetase inhibitor			
ephedrine	Launched	adrenergic receptor agonist	ACHE|ADRA1A|ADRB2|SLC18A2|SLC6A2	cardiology|pulmonary|neurology/psychiatry|endocrinology	hypotension|asthma|narcolepsy|obesity
ephedrine-(racemic)	Launched	adrenergic receptor agonist	ADRA1A|ADRA2A|ADRB1|ADRB2|ATF1|ATF2|ATF3|ATF4|ATF5|ATF6|ATF7|FOS|IL2|JDP2|JUN|NFATC1|SLC6A2|SLC6A3|SLC6A4|TNF	cardiology|pulmonary|neurology/psychiatry|endocrinology	hypotension|asthma|narcolepsy|obesity
epiandrosterone	Preclinical	steroid	G6PD		
epicatechin-gallate-(-)	Phase 2	bacterial DNA gyrase inhibitor	BACE1|FASN		
epiestriol	Preclinical				
epigallocatechin-(-)	Phase 2				
epigallocatechin-gallate-(-)	Phase 2/Phase 3	bacterial DNA gyrase inhibitor	ELANE|EP300|FASN|KAT2B|MMP14|MMP2		
epinastine	Launched	histamine receptor antagonist	HRH1	ophthalmology	conjunctivitis
epinephrine	Launched	adrenergic receptor agonist|carbonic anhydrase activator|neurotransmitter	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|ADRB1|ADRB2|ADRB3|PAH|TNF	cardiology|allergy|pulmonary	cardiac arrest|anaphylactic shock|asthma
epirizole	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	neurology/psychiatry	pain relief
epirubicin	Launched	topoisomerase inhibitor	CHD1|TOP2A	oncology	breast cancer
epitiostanol	Launched	androgen receptor agonist	AR	oncology	breast cancer
eplerenone	Launched	cytochrome P450 inhibitor	NR3C2	cardiology	congestive heart failure|hypertension
epomediol	Launched	cholesterol inhibitor	CYP7A1	neurology/psychiatry	itching
epoprostenol	Launched	prostacyclin analog	P2RY12|PTGER1|PTGER4|PTGIR|PTGIS	cardiology	hypertension
epothilone-A	Preclinical	microtubule stabilizing agent			
epothilone-B	Phase 3	microtubule stabilizing agent|tubulin polymerization inhibitor	TUBB		
epothilone-D	Phase 2	microtubule stabilizing agent|tubulin polymerization inhibitor	TUBB		
EPPTB	Preclinical	trace amine associated receptor antagonist	TAAR1		
eprazinone	Launched	mucolytic agent		pulmonary	bronchospasm
eprinomectin	Launched	benzodiazepine receptor agonist		infectious disease	gastrointestinal roundworms|lungworms
epristeride	Preclinical	5 alpha reductase inhibitor			
eprobemide	Launched	monoamine oxidase inhibitor	MAOA	neurology/psychiatry	depression
eprodisate	Phase 3	amyloid protein inhibitor|antiamyloidogenic agent	SAA1		
eprosartan	Launched	angiotensin receptor antagonist	AGTR1	cardiology	hypertension
eptifibatide	Launched	platelet aggregation inhibitor	ITGA2B|ITGB3	cardiology	acute coronary syndrome (ACS)|percutaneous coronary intervention (PCI)
EPZ-5676	Phase 1	histone lysine methyltransferase inhibitor	DOT1L		
EPZ004777	Preclinical	histone lysine methyltransferase inhibitor	DOT1L		
EPZ005687	Preclinical	histone lysine methyltransferase inhibitor	EZH2		
EPZ011989	Preclinical	histone lysine methyltransferase inhibitor	EZH2		
EPZ015666	Preclinical	protein arginine N-methyltransferase inhibitor	PRMT5		
EPZ020411	Preclinical	protein arginine N-methyltransferase inhibitor	PRMT6		
equilin	Preclinical	estrogen receptor agonist	HSD17B1		
equol	Launched	estrogen receptor agonist	ESR1|ESR2		
ER-27319	Preclinical	mediator release inhibitor|SYK inhibitor	SYK		
ER-50891	Preclinical	retinoid receptor antagonist	RARA		
erastin	Preclinical	ion channel antagonist	VDAC2		
eravacycline	Launched	antibacterial			
erbstatin-analog	Preclinical	EGFR inhibitor|tyrosine kinase inhibitor	EGFR		
ercalcitriol	Phase 1	vitamin D receptor agonist	VDR		
erdafitinib	Launched	FGFR inhibitor	FGFR1|FGFR2|FGFR3|FGFR4		
erdosteine	Launched	mucolytic agent		pulmonary|infectious disease	bronchitis|cough suppressant|chronic obstructive pulmonary disease (COPD)|respiratory tract infections
ergocalciferol	Launched	vitamin analog	VDR	endocrinology|orthopedics	hypoparathyroidism|rickets|hypophosphatemia
ergonovine	Launched	adrenergic receptor agonist|serotonin receptor agonist	ADRA1A|HTR1E	hematology	postpartum hemorrhage (PPH)
ergosterol	Preclinical	vitamin D precursor			
ergotamine	Launched	adrenergic receptor antagonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|DRD1|DRD2|DRD5|HTR1A|HTR1B|HTR1D|HTR1E|HTR1F|HTR2A|HTR2B|HTR2C|HTR5A|HTR6|SLC6A2	neurology/psychiatry	migraine headache
eribulin	Launched	microtubule inhibitor		oncology	breast cancer
ERK5-IN-1	Preclinical	MAP kinase inhibitor	MAPK7		
erlotinib	Launched	EGFR inhibitor	EGFR|NR1I2	oncology	non-small cell lung cancer (NSCLC)|pancreatic cancer
ertapenem	Launched	bacterial cell wall synthesis inhibitor		infectious disease	intra-abdominal infections|skin infections|pneumonia|urinary tract infections|gynecologic infections|postpartum endomyometritis
erteberel	Phase 2	estrogen receptor agonist	ESR1|ESR2		
ertugliflozin	Launched	sodium/glucose cotransporter inhibitor	SLC5A2	endocrinology	diabetes mellitus
erythritol	Launched				
erythromycin	Launched	NFkB pathway inhibitor	MLNR	infectious disease	listeria|respiratory tract infections|skin infections|syphilis|amebiasis|pelvic inflammatory disease|chlamydia|diphtheria|erythrasma
erythromycin-estolate	Launched	bacterial 50S ribosomal subunit inhibitor	ABCB1|ALB|CYP3A4|CYP51A1|KCNH2|MLNR|SLC47A1	infectious disease	listeria|respiratory tract infections|skin infections|syphilis|amebiasis|pelvic inflammatory disease|chlamydia|diphtheria|erythrasma
erythromycin-ethylsuccinate	Launched	cytochrome P450 inhibitor|protein synthesis inhibitor	ABCB1|ALB|CYP3A4|CYP51A1|KCNH2|MLNR|SLC47A1	infectious disease	listeria|respiratory tract infections|skin infections|syphilis|amebiasis|pelvic inflammatory disease|chlamydia|diphtheria|erythrasma
erythrosine	Preclinical	coloring agent			
esaprazole	Phase 2				
esaxerenone	Preclinical	mineralocorticoid receptor antagonist			
escin	Launched	nitric oxide synthase stimulant		dermatology	varicose veins
escitalopram	Launched	selective serotonin reuptake inhibitor (SSRI)	SLC6A4	neurology/psychiatry	depression|generalized anxiety disorder (GAD)
esculin	Phase 1	antioxidant			
eseroline-(-)	Preclinical	acetylcholinesterase inhibitor	OPRD1|OPRM1		
ESI-09	Preclinical	EPAC inhibitor	RAPGEF3|RAPGEF4		
eslicarbazepine-acetate	Launched	sodium channel blocker	SCN10A|SCN11A|SCN1A|SCN2A|SCN3A|SCN4A|SCN5A|SCN7A|SCN8A|SCN9A	neurology/psychiatry	seizures
esmolol	Launched	adrenergic receptor antagonist	ADRB1	cardiology	ventricular tachycardia (VT)|hypertension
esomeprazole	Launched	ATPase inhibitor	ATP4A	gastroenterology	gastroesophageal reflux disease (GERD)|Zollinger-Ellison syndrome|peptic ulcer disease (PUD)
esonarimod	Preclinical	antirheumatic drug			
estetrol	Phase 3	selective estrogen receptor modulator (SERM)	ESR1		
estradiol	Launched	estrogen receptor agonist	ESR1|ESR2|GPER1|KCNMA1|NR1I2	endocrinology	contraceptive
estradiol-acetate	Launched	estrogen receptor agonist	ESR1	endocrinology|obstetrics/gynecology	menopause|vaginal atrophy
estradiol-benzoate	Preclinical	contraceptive agent	ESR1		
estradiol-cypionate	Launched	estrogen receptor agonist	ESR1	endocrinology	hypoestrogenism|menopause
estradiol-valerate	Launched	estrogen receptor agonist	ESR1	oncology|endocrinology|obstetrics/gynecology	prostate cancer|hypoestrogenism|menopause|vaginal atrophy
estradiol-3-O-sulfamate	Phase 2	steryl sulfatase inhibitor			
estramustine	Launched	DNA alkylating agent	ESR1|ESR2|MAP1A|MAP2	oncology	prostate cancer
estramustine-phosphate	Launched	DNA synthesis inhibitor|microtubule inhibitor	ESR1|ESR2|MAP1A|MAP2	oncology	prostate cancer
estriol	Launched	estrogen receptor agonist	ESR1|ESR2	endocrinology|obstetrics/gynecology|infectious disease	menopause|vaginal atrophy|urinary tract infections
estrone	Launched	estrogen receptor agonist|estrogenic hormone	ESR1|ESR2	endocrinology	menopause
estropipate	Launched	estrogen receptor agonist	ESR1|ESR2	orthopedics|endocrinology|obstetrics/gynecology	osteoporosis|menopause|vaginal atrophy|hypoestrogenism
etacrynic-acid	Launched	sodium/potassium/chloride transporter inhibitor	ATP1A1|SLC12A1	cardiology|gastroenterology|nephrology|rheumatology	hypertension|congestive heart failure|edema|hepatic cirrhosis|chronic renal failure|nephrotic syndrome
etafenone	Launched	calcium channel blocker			
etamsylate	Launched	hemostatic agent		hematology	hemorrhage
etanidazole	Phase 3	bacterial cell wall synthesis inhibitor			
etazolate	Phase 2	phosphodiesterase inhibitor	GABRB3|PDE4A		
ETC-159	Phase 1	beta catenin inhibitor|porcupine inhibitor	PORCN		
ETC-206	Phase 1	MAPK-interacting kinase inhibitor			
etebenecid	Preclinical	uricosuric blocker			
eterobarb	Phase 2	anticonvulsant			
ethacizin	Launched	anticonvulsant		cardiology	ventricular tachycardia (VT)|Wolff-Parkinson-White Syndrome (WPW)
ethacridine-lactate-monohydrate	Preclinical	DNA intercalating agent			
ethambutol	Launched	bacterial cell wall synthesis inhibitor		infectious disease	tuberculosis
ethamivan	Preclinical	respiratory stimulant			
ethanolamine-oleate	Launched	immunostimulant	F12|FABP4|FFAR1|FFAR4|PLD2	gastroenterology	esophageal varices
ethaverine	Launched	calcium channel blocker		neurology/psychiatry	muscle relaxant|spasms
ethenzamide	Launched	analgesic agent		neurology/psychiatry|endocrinology|otolaryngology	headache|fever|common cold
ethimizol	Phase 1				
ethinyl-estradiol	Launched	estrogen receptor agonist|estrogenic hormone	ESR1|ESR2|NR1I2	endocrinology	contraceptive
ethionamide	Launched	mycolic synthesis inhibitor		infectious disease	tuberculosis
ethisterone	Launched	progestogen hormone	TYR	endocrinology	amenorrhea
ethopabate	Launched	antiprotozoal agent		infectious disease	coccidiosis
ethosuximide	Launched	succinimide antiepileptic	CACNA1G|CACNA1H|CACNA1I	neurology/psychiatry	epilepsy
ethotoin	Launched	hydantoin antiepileptic	SCN5A	neurology/psychiatry	seizures
ethoxyquin	Preclinical	antioxidant			
ethoxzolamide	Launched	carbonic anhydrase inhibitor	CA1|CA12|CA13|CA14|CA2|CA3|CA4|CA5A|CA5B|CA6|CA7|CA9	ophthalmology|gastroenterology	glaucoma|duodenal ulcer disease
ethyl-paraben	Preclinical				
ethyl-pyruvate	Phase 2	tumor necrosis factor production inhibitor			
ethyl-vanillin	Preclinical				
ethyl-2-(carbamoyloxy)benzoate	Phase 1				
ethylenediaminetetraacetic-acid	Launched	PKC inhibitor		neurology/psychiatry	metal toxicity
ethylnorepinephrine	Preclinical	bronchodilator			
ethynodiol-diacetate	Launched		ESR1|PGR	endocrinology	contraceptive
ethynylcytidine	Preclinical	antimetabolite			
eticlopride	Preclinical	dopamine receptor antagonist	DRD2|DRD3|DRD4		
etidronic-acid	Launched	bone resorption inhibitor	ATP6V1A|PTPRS	endocrinology|orthopedics	Paget's disease|heterotopic ossification
etifenin	Preclinical	renal function diagnostic agent			
etifoxine	Launched	GABA receptor modulator	GABRA1|GABRA2|GABRA3|GABRA5	neurology/psychiatry	anxiety
etilefrine	Launched	adrenergic receptor agonist	ADRA1A|ADRB1	neurology/psychiatry|otolaryngology|endocrinology|pulmonary	headache|nasal congestion|fever|cough suppressant|common cold
etilevodopa	Phase 3	dopamine receptor agonist	DRD3		
etizolam	Launched	benzodiazepine receptor agonist	GABRA1	neurology/psychiatry	insomnia|anxiety
etodolac	Launched	cyclooxygenase inhibitor	PTGS2	rheumatology	osteoarthritis|rheumatoid arthritis
etofenamate	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	neurology/psychiatry|rheumatology	muscle pain|joint pain
etofibrate	Launched	PPAR receptor agonist	PPARA	endocrinology	hypertriglyceridemia
etofylline	Launched	adenosine receptor antagonist	ADORA1	pulmonary	asthma|bronchitis
etofylline-clofibrate	Launched	platelet aggregation inhibitor	PPARA	endocrinology	hyperlipidemia
etomidate	Launched	GABA receptor modulator	ADRA2B|GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ	neurology/psychiatry	general anaesthetic
etomoxir	Phase 2	carnitine palmitoyltransferase inhibitor	CPT1A		
etonogestrel	Launched	progesterone receptor agonist	ESR1|PGR	endocrinology	contraceptive
etoposide	Launched	topoisomerase inhibitor	TOP2A|TOP2B	oncology	non-small cell lung cancer (NSCLC)
etoposide-phosphate	Launched	topoisomerase inhibitor	TOP2A	oncology	testicular carcinoma|small cell lung cancer
etoricoxib	Launched	cyclooxygenase inhibitor	PTGS2	rheumatology	rheumatoid arthritis|psoriatic arthritis|osteoarthritis|gout|ankylosing spondylitis
etosalamide	Preclinical	anti-inflammatory agent			
etoxybamide	Phase 2				
ETP-45658	Preclinical	PI3K inhibitor	PIK3CA|PIK3CB|PIK3CD|PIK3CG		
ETP-46464	Preclinical	ATR kinase inhibitor			
etrabamine	Phase 2	dopamine receptor agonist			
etrasimod	Phase 3	sphingosine 1-phosphate receptor antagonist			
etravirine	Launched	non-nucleoside reverse transcriptase inhibitor	CYP2C19|CYP2C9|CYP3A4	infectious disease	human immunodeficiency virus (HIV-1)
etretinate	Withdrawn	protein synthesis inhibitor	RARA|RXRG		
eucalyptol	Launched	acetylcholinesterase inhibitor	ACHE	dental	gingivitis
eucatropine	Preclinical	acetylcholine receptor antagonist			
eugenol	Launched	androgen receptor antagonist	AR	dental	toothache
EUK-134	Preclinical	catalase stimulant	APP|SOD2		
eupatilin	Launched	mucus protecting agent			
evacetrapib	Phase 3	cholesteryl ester transfer protein inhibitor	CETP		
evans-blue	Launched	glutamate receptor negative allosteric modulator	GRIA1|PTPN1		
evatanepag	Phase 2	prostaglandin inhibitor	PTGER2|PTGER4		
evenamide	Phase 2	voltage-gated sodium channel blocker			
everolimus	Launched	mTOR inhibitor	MTOR	oncology|neurology/psychiatry|genetics|urology	breast cancer|neuroendocrine tumors of pancreatic origin (PNET)|renal cell carcinoma (RCC)|subependymal giant cell astrocytoma (SEGA)|tuberous sclerosis complex (TSC)|renal angiomyolipoma
evobrutinib	Phase 2	Bruton's tyrosine kinase (BTK) inhibitor			
evocalcet	Phase 3	calcium sensitizer			
evodiamine	Preclinical	ATPase inhibitor|TRPV agonist	TRPV1		
EVP-6124	Phase 3	acetylcholine receptor agonist	CHRNA7		
EVP4593	Preclinical	NFkB pathway inhibitor			
EW-7197	Phase 2	TGF beta receptor inhibitor	ACVR1B|TGFBR1		
EX-527	Phase 2	SIRT inhibitor	SIRT1		
exalamide	Launched	membrane permeability inhibitor			
examorelin	Phase 2	growth hormone releasing factor agonist	GHRHR|GHSR		
exatecan-mesylate	Phase 3	topoisomerase inhibitor	TOP1		
exemestane	Launched	aromatase inhibitor	CYP19A1	oncology	breast cancer
exenatide	Launched	GLP receptor agonist	GLP1R	endocrinology	diabetes mellitus
exherin	Phase 2	cadherin antagonist	CDH2		
exifone	Withdrawn	nootropic agent	TYR		
exisulind	Phase 3	phosphodiesterase inhibitor	PDE5A		
exo-IWR-1	Preclinical	WNT signaling inhibitor negative control	TNKS		
EXO-1	Preclinical	ARF inhibitor			
ezatiostat	Phase 2	glutathione transferase inhibitor	GSTP1		
ezetimibe	Launched	cholesterol inhibitor|Niemann-Pick C1-like 1 protein antagonist	ANPEP|NPC1L1|SOAT1	endocrinology|metabolism	hyperlipidemia|hypercholesterolemia|sitosterolemia
ezutromid	Phase 2	utrophin enhancer	UTRN		
E3330	Preclinical	NFkB pathway inhibitor			
E7046	Phase 1	prostanoid receptor antagonist			
E7449	Phase 2	PARP inhibitor	PARP1|PARP2|TNKS|TNKS2		
E7820	Phase 2	angiogenesis inhibitor			
F-11440	Phase 2	serotonin receptor agonist	HTR1A		
F-16915	Preclinical				
fadrozole	Launched	aromatase inhibitor	CYP11B1|CYP19A1	oncology	breast cancer
fagomine	Phase 2	glucosidase inhibitor	GLB1		
falecalcitriol	Launched	vitamin D receptor agonist	VDR	endocrinology	hyperparathyroidism
famciclovir	Launched	DNA polymerase inhibitor		dental|infectious disease	cold sore|genitial herpes|shingles
famotidine	Launched	histamine receptor antagonist	HRH2	gastroenterology	heartburn
famprofazone	Preclinical	cyclooxygenase inhibitor			
fananserin	Phase 2	dopamine receptor antagonist|serotonin receptor antagonist	HTR2A		
fanetizole	Phase 3	neutrophil superoxide production			
fantofarone	Preclinical	calcium channel blocker			
farampator	Preclinical	ionotropic glutamate receptor agonist			
farnesyl-thiosalicylic-acid-amide	Phase 1	Ras GTPase inhibitor	HRAS		
faropenem	Launched	lactamase inhibitor		infectious disease|pulmonary|otolaryngology	pneumonia|bronchitis|skin infections|urinary tract infections|sinusitis
faropenem-medoxomil	Launched	lactamase inhibitor		otolaryngology|infectious disease|pulmonary	sinusitis|pneumonia|bronchitis|skin infections|urinary tract infections
fasoracetam	Preclinical	GABA receptor antagonist			
fasudil	Launched	rho associated kinase inhibitor	PKIA|PRKACA|ROCK1|ROCK2	neurology/psychiatry	cerebral vasospasm
favipiravir	Phase 3	RNA polymerase inhibitor			
FCE-22250	Phase 1	DNA directed DNA polymerase inhibitor			
fdcyd	Phase 2	DNA methyltransferase inhibitor			
febuprol	Launched	choleretic agent			
febuxostat	Launched	xanthine oxidase inhibitor	XDH	nephrology	hyperuricemia
fedratinib	Launched	FLT3 inhibitor|JAK inhibitor	BRD4|JAK1|JAK2|JAK3|TYK2	hematologic malignancy	myelofibrosis
felbamate	Launched	glutamate receptor antagonist	GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|GRIN3A|GRIN3B	neurology/psychiatry	epilepsy
felbinac	Launched	cyclooxygenase inhibitor	CTSL	rheumatology|neurology/psychiatry	rheumatoid arthritis|muscle pain
felbinac-ethyl	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2		
felodipine	Launched	calcium channel blocker	CFTR	cardiology	hypertension
felypressin	Preclinical	vasopressin receptor agonist			
fenaclon	Preclinical				
fenbendazole	Launched	tubulin polymerization inhibitor	TUBB	infectious disease	gastrointestinal parasites|gastrointestinal roundworms
fenbufen	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	neurology/psychiatry	pain relief
fenclonine-(+/-)	Preclinical	tryptophan hydroxylase inhibitor	PAH|TPH1|TPH2		
fendiline	Preclinical	calcium channel blocker	HTR2B		
fenebrutinib	Phase 2	Bruton's tyrosine kinase (BTK) inhibitor			
fenigam	Launched	benzodiazepine receptor agonist	GABBR1|GABBR2	neurology/psychiatry	posttraumatic stress disorder|anxiety|depression
fenipentol	Launched	choleretic agent		gastroenterology	bile stimulation
fenobam	Phase 2	glutamate receptor antagonist	GRM5		
fenofibrate	Launched	PPAR receptor agonist	MMP25|PPARA	endocrinology	hypercholesterolemia|hypertriglyceridemia
fenofibric-acid	Launched	cytochrome P450 inhibitor	CLCN1|PPARA	cardiology	dyslipidemia
fenoldopam	Launched	dopamine receptor agonist	DRD1|DRD4	cardiology	hypertension
fenoprofen	Launched	prostaglandin inhibitor	PTGS1|SLC5A8	rheumatology	rheumatoid arthritis|osteoarthritis
fenoterol	Withdrawn	adrenergic receptor agonist	ADRB2		
fenoverine	Launched	acetylcholine receptor antagonist		neurology/psychiatry	spasms
fenoxaprop-p-ethyl	Preclinical		NOS3		
fenretinide	Phase 3	apoptosis stimulant|retinoid receptor agonist	RARA		
fenspiride	Launched	bronchodilator		pulmonary|otolaryngology	asthma|otitis|sinusitis|rhinopharyngitis|laryngitis
fenthion	Launched	cholinesterase inhibitor			
fentiazac	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	neurology/psychiatry|rheumatology	muscle pain|joint pain
fenticonazole	Launched	bacterial cell wall synthesis inhibitor		infectious disease	vulvovaginal candidiasis
FERb-033	Preclinical	EGFR inhibitor	ERBB2		
ferroquine	Phase 2	antimalarial agent			
ferrostatin-1	Preclinical	ferroptosis inhibitor			
ferulic-acid	Phase 2	antioxidant	CA1|CA12|CA14|CA2|CA4|CA6|CA9		
fesoterodine	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5	urology	urinary incontinence
fevipiprant	Phase 2	prostaglandin inhibitor			
fexaramine	Preclinical	FXR agonist	NR1H4		
fexinidazole	Phase 3				
fexofenadine	Launched	histamine receptor antagonist	HRH1	allergy	allergic rhinitis|urticaria
fezolinetant	Phase 2	neurokinin receptor antagonist			
FG-2216	Phase 2	hypoxia inducible factor prolyl hydroxylase inhibitor	EGLN1|EGLN2|HIF1A		
FG-4592	Phase 3	hypoxia inducible factor prolyl hydroxylase inhibitor	EGLN1|EGLN2|EGLN3		
FG-7142	Preclinical	GABA benzodiazepine site receptor inverse agonist			
FGIN-1-27	Preclinical	inositol monophosphatase inhibitor	TSPO		
FGIN-1-43	Preclinical	benzodiazepine receptor agonist	TSPO		
FH-535	Preclinical	PPAR receptor antagonist|WNT signaling inhibitor	PPARD|PPARG		
FH1	Preclinical	hepatocyte function enhancer			
fiacitabine	Phase 2	DNA synthesis inhibitor			
fidarestat	Phase 3	aldose reductase inhibitor	AKR1B1		
fidaxomicin	Launched	RNA polymerase inhibitor		gastroenterology	diarrhea
filanesib	Phase 3	kinesin inhibitor|kinesin-like spindle protein inhibitor	KIF11		
filgotinib	Phase 3	JAK inhibitor	JAK1|JAK2|JAK3|TYK2		
fimasartan	Launched	angiotensin receptor antagonist	AGTR1	cardiology	hypertension|congestive heart failure
finafloxacin	Launched	bacterial DNA gyrase inhibitor		infectious disease|pulmonary	intra-abdominal infections|chronic obstructive pulmonary disease (COPD)|cystic fibrosis
finasteride	Launched	5 alpha reductase inhibitor	AKR1D1|SRD5A1|SRD5A2	endocrinology	androgenetic alopecia
fingolimod	Launched	immunosuppressant|sphingosine 1-phosphate receptor agonist	S1PR1|S1PR5	neurology/psychiatry	multiple sclerosis
fipexide	Withdrawn	psychoactive drug			
FIPI	Preclinical	phospholipase inhibitor	PLD1|PLD2		
fipronil	Launched	chloride channel blocker|GABA gated chloride channel blocker		infectious disease	flea control
firategrast	Phase 2	integrin antagonist	ITGA4		
firocoxib	Launched	cyclooxygenase inhibitor	PTGS2	rheumatology	osteoarthritis
firsocostat	Phase 2	acetyl-CoA carboxylase inhibitor			
fisetin	Preclinical	Aurora kinase inhibitor	CDK6|FASN		
fisogatinib	Phase 1	fibroblast growth factor inhibitor			
FIT	Preclinical	opioid receptor agonist	OPRD1		
FK-33-824	Phase 2	opioid receptor agonist	OPRM1		
FK-3311	Phase 2	cyclooxygenase inhibitor	PTGS2		
FK-409	Phase 2	guanylyl cyclase activator			
FK-866	Phase 2	niacinamide phosphoribosyltransferase inhibitor	NAMPT		
FK-888	Phase 2	tachykinin antagonist	TACR1|TACR2		
FK-962	Phase 2	somatostatin receptor agonist			
flavin-adenine-dinucleotide	Preclinical		ACAD8|ACADM|ACADS|ACOX1|AIFM1|CYB5R1|CYB5R3|DAO|DLD|DPYD|ERO1LB|FDXR|GCDH|GFER|GSR|IL4I1|IVD|MAOA|MAOB|NOS1|NQO1|NQO2|POR|TXNRD1|XDH		
flavoxate	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2	urology	urinary incontinence|interstitial cystitis (IC)|urethritis|prostatitis
flecainide	Launched	sodium channel blocker	KCNA5|KCNA7|SCN5A	cardiology	ventricular tachycardia (VT)|atrial fibrillation (AF)|ventricular arrhythmias
fleroxacin	Launched	topoisomerase inhibitor	TOP2A	infectious disease|gastroenterology	gonorrhea|enteritis|diarrhea|respiratory tract infections
FLI-06	Preclinical	notch signaling inhibitor			
flibanserin	Launched	serotonin receptor agonist	DRD4|HTR1A|HTR2A	neurology/psychiatry	hypoactive sexual desire disorder
flindokalner	Phase 3	potassium channel agonist	KCNMA1|KCNN4|KCNQ2|KCNQ4|KCNQ5		
floctafenine	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	neurology/psychiatry	pain relief
flopropione	Launched	serotonin receptor antagonist	HTR1A	neurology/psychiatry	spasms
florfenicol	Launched	protein synthesis inhibitor		pulmonary	bovine respiratory disease (BRD)
florifenine	Preclinical	anti-inflammatory agent			
flosequinan	Withdrawn	phosphodiesterase inhibitor			
floxuridine	Launched	DNA synthesis inhibitor	TYMS	oncology	colorectal cancer
FLT3-IN-1	Preclinical	FLT3 inhibitor			
flubendazole	Launched	tubulin polymerization inhibitor	TUBB	infectious disease	gastrointestinal parasites
flucloxacillin	Launched	bacterial cell wall synthesis inhibitor		infectious disease|otolaryngology|dermatology|gastroenterology	gram-positive bacterial infections|tonsillitis|sinusitis|pneumonia|eczema|endocarditis|meningitis|enteritis|bacterial septicemia
fluconazole	Launched	sterol demethylase inhibitor	CYP51A1	infectious disease	esophageal candidiasis|meningitis
flucytosine	Launched	other antifungal	DNMT1	infectious disease	bacterial septicemia|endocarditis|urinary tract infections|meningitis
fludarabine	Launched	ribonucleotide reductase inhibitor	ADA|DCK|POLA1|RRM1|RRM2	hematologic malignancy	chronic lymphocytic leukemia (CLL)
fludarabine-phosphate	Launched	ribonucleotide reductase inhibitor	POLA1|POLD1|POLE|RRM1|RRM2|RRM2B	hematologic malignancy	chronic lymphocytic leukemia (CLL)
fludrocortisone-acetate	Launched		NR3C2	endocrinology	Addison's disease|adrenogenital syndrome
fludroxycortide	Launched	glucocorticoid receptor agonist	NR3C1|SERPINA6	infectious disease|dermatology	skin infections|psoriasis
flufenamic-acid	Preclinical	chloride channel blocker	AKR1C3|ANO1|AR|GJA1|GJA10|GJA3|GJA4|GJA5|GJA8|GJA9|GJB1|GJB2|GJB3|GJB4|GJB5|GJB6|GJB7|GJC1|GJC2|GJC3|GJD2|GJD3|GJD4|GJE1|PANX1|PANX2|PANX3|PKD2L1|PTGS1|PTGS2|TRPC5|TRPM2|TRPM5		
flumatinib	Phase 3	Bcr-Abl kinase inhibitor	ABL1|PDGFRB		
flumazenil	Launched	benzodiazepine receptor antagonist	GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ	neurology/psychiatry	sedative
flumecinol	Launched				
flumequine	Launched	topoisomerase inhibitor		infectious disease	urinary tract infections
flumethasone	Launched	glucocorticoid receptor agonist	NR3C1|PLA2G1B	otolaryngology|infectious disease|dermatology	otitis|ear infections|corticosteroid-responsive dermatoses
flumethasone-pivalate	Launched	glucocorticoid receptor agonist	NR3C1|SERPINA6	allergy	allergic rhinitis
flumexadol	Preclinical				
flunarizine	Launched	calcium channel blocker	CACNA1G|CACNA1H|CACNA1I|CALM1|HRH1	neurology/psychiatry|cardiology	migraine headache|vertigo|peripheral artery disease (PAD)
flunisolide	Launched	cytochrome P450 inhibitor	NR3C1	allergy	allergic rhinitis
flunixin-meglumin	Launched	prostanoid receptor antagonist		pulmonary	bovine respiratory disease (BRD)
fluocinolone-acetonide	Launched	glucocorticoid receptor agonist	NR3C1|SERPINA6	dermatology	seborrheic dermatitis
fluocinonide	Launched	glucocorticoid receptor agonist	NR3C1|SERPINA6|SMO	dermatology	seborrheic dermatitis|eczema
fluorescein	Launched		SLC22A6	ophthalmology	ophthalmology diagnostic
fluorometholone	Launched	glucocorticoid receptor agonist	NR3C1	ophthalmology	eye inflammation
fluorometholone-acetate	Launched		NR3C1	ophthalmology	eye inflammation
fluoromethylcholine	Launched				
fluoxetine	Launched	selective serotonin reuptake inhibitor (SSRI)	ANO1|HTR2B|SLC6A4	neurology/psychiatry	depression|obsessive compulsive disorder (OCD)|bulimia nervosa|panic disorders|bipolar disorder
flupentixol	Launched	dopamine receptor antagonist	ADRA1A|CHRM1|DRD1|DRD2|DRD3|DRD5|HTR2A	neurology/psychiatry	schizophrenia|depression
fluphenazine	Launched	dopamine receptor antagonist	CALM1|DRD1|DRD2|DRD5|HRH1|HTR2A|HTR6|HTR7	neurology/psychiatry	schizophrenia
fluphenazine-decanoate	Launched	dopamine receptor antagonist	DRD2|HTR1B|HTR4	neurology/psychiatry	schizophrenia
flupirtine	Launched	glutamate receptor antagonist	ADRA2A|KCNQ1|KCNQ2	neurology/psychiatry	pain relief
fluprazine	Phase 1	serotonin receptor agonist	HTR1A|HTR1B		
fluralaner	Preclinical	GABA receptor antagonist			
flurbiprofen-(+/-)	Launched	cyclooxygenase inhibitor		rheumatology	rheumatoid arthritis|osteoarthritis
flurbiprofen-(S)-(+)	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	rheumatology	rheumatoid arthritis|osteoarthritis
flurbiprofen-axetil	Launched	analgesic agent			
flurizan	Phase 3	gamma secretase inhibitor	APH1B|BACE1|IKBKG|PSEN1|PSEN2|PTGS1|PTGS2		
flurofamide	Preclinical	urease inhibitor			
flurothyl	Preclinical				
fluroxene	Preclinical	local anesthetic			
fluspirilene	Launched	dopamine receptor antagonist	CACNG1|DRD2|HRH1|HTR1A|HTR1D|HTR1E|HTR2A	neurology/psychiatry	schizophrenia
flutamide	Launched	androgen receptor antagonist	AHR|AR	oncology	prostate cancer
fluticasone-propionate	Launched	glucocorticoid receptor agonist	NR3C1|NR3C2|PGR|PLA2G4A	dermatology	corticosteroid-responsive dermatoses
flutrimazole	Launched	sterol demethylase inhibitor		infectious disease	mycosis
fluvastatin	Launched	HMGCR inhibitor	HMGCR	endocrinology|cardiology	hypercholesterolemia|congenital heart defects
fluvoxamine	Launched	selective serotonin reuptake inhibitor (SSRI)	SLC6A4	neurology/psychiatry	obsessive compulsive disorder (OCD)
fmoc-L-leucine	Phase 2	PPAR receptor agonist			
FN-1501	Phase 1	tyrosine kinase inhibitor			
folic-acid	Launched	folate receptor ligand	FOLR2|FOLR3|SLC19A1|SLC46A1	hematology	megaloblastic anemia
fomepizole	Launched	alcohol dehydrogenase inhibitor	ADH1A|ADH1B|ADH1C|AKR1A1|CAT	critical care	poison antidote
fomocaine	Launched	voltage-gated sodium channel modulator		neurology/psychiatry	local anesthetic
fondaparinux	Launched	coagulation factor inhibitor	F10|SERPINC1	hematology	deep vein thrombosis (DVT)
foretinib	Phase 2	VEGFR inhibitor	FLT1|FLT4|KDR|MET		
formestane	Launched	aromatase inhibitor	CYP19A1	oncology	breast cancer
formononetin	Preclinical	alcohol dehydrogenase inhibitor	ADH1C|SLC5A2		
formoterol	Launched	adrenergic receptor agonist	ADRB2	pulmonary	asthma|chronic obstructive pulmonary disease (COPD)|bronchospasm
forodesine	Launched	purinergic receptor antagonist	PNP	hematologic malignancy	peripheral T-cell lymphoma (PTCL)
foropafant	Phase 3	platelet activating factor receptor antagonist	PTAFR		
forskolin	Launched	adenylyl cyclase activator	ADCY2|ADCY5|GNAS		
fosamprenavir	Launched	HIV protease inhibitor		infectious disease	human immunodeficiency virus (HIV-1)
fosaprepitant-dimeglumine	Launched	tachykinin antagonist	TACR1	gastroenterology	nausea|vomiting
fosbretabulin	Phase 3	tubulin polymerization inhibitor|VE-cadherin antagonist	CDH5		
foscarnet	Launched	DNA polymerase inhibitor		infectious disease	cytomegalovirus retinitis|acquired immunodeficiency syndrome (AIDS)|virus herpes simplex (HSV)
fosfestrol	Launched	synthetic estrogen	ESR1|ESR2	oncology	prostate cancer
fosfluconazole	Preclinical	other antifungal			
fosfomycin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	urinary tract infections
fosfosal	Launched	phosphodiesterase inhibitor	PTGS1|PTGS2	neurology/psychiatry	pain relief
fosfructose	Phase 3	fructose diphosphate stimulant			
fosinopril	Launched	angiotensin converting enzyme inhibitor	ACE	cardiology	hypertension|congestive heart failure
fosinoprilat	Launched	angiotensin converting enzyme inhibitor	ACE	cardiology	hypertension
fosphenytoin	Launched	sodium channel blocker	SCN5A	neurology/psychiatry	epilepsy|seizures
fostamatinib	Launched	SYK inhibitor	SYK	hematology	chronic immune thrombocytopenia (ITP)
fostemsavir	Phase 3	antiviral			
fotemustine	Launched	thioredoxin inhibitor		oncology	melanoma
foxy-5	Phase 2	WNT5a peptide mimetic	WNT5A		
FPA-124	Preclinical	AKT inhibitor			
FPH1-(BRD-6125)	Preclinical	hepatocyte function enhancer			
FPL-12495	Phase 1	glutamate receptor antagonist			
FPL-55712	Phase 1	leukotriene receptor antagonist			
FPL-62064	Phase 2	cyclooxygenase inhibitor|lipoxygenase inhibitor			
FPL-64176	Preclinical	calcium channel activator	CACNA1C|CACNA1S		
FPS-ZM1	Preclinical	RAGE receptor antagonist	AGER		
FR-122047	Preclinical	cyclooxygenase inhibitor			
FR-139317	Phase 1	endothelin receptor antagonist	EDNRA		
FR-180204	Preclinical	MAP kinase inhibitor	MAPK1|MAPK3		
FRAX486	Preclinical	serine/threonine kinase inhibitor	PAK1|PAK2|PAK3|PAK4		
frentizole	Phase 1	immunosuppressant			
freselestat	Preclinical	elastase inhibitor	CELA1|ELANE		
frovatriptan	Launched	serotonin receptor agonist	HTR1A|HTR1B|HTR1D	neurology/psychiatry	migraine headache
fruquintinib	Launched	VEGFR inhibitor	KDR	oncology	colorectal cancer
ftaxilide	Preclinical				
ftorafur	Launched	thymidylate synthase inhibitor	TYMS	oncology	colorectal cancer
FT011	Preclinical	TGF beta receptor inhibitor			
fucoxanthin	Phase 2	anticancer agent			
fudosteine	Launched	mucolytic agent		pulmonary	chest congestion
fulvestrant	Launched	estrogen receptor antagonist	ESR1|ESR2|GPER1	oncology	breast cancer
fumagillin	Launched	methionine aminopeptidase inhibitor	METAP2	infectious disease	microsporidiosis
fumonisin-B1	Preclinical		CERS1		
funapide	Preclinical	sodium channel blocker			
furagin	Preclinical	antibacterial			
furaltadone	Launched	bacterial DNA inhibitor		infectious disease	gram-negative bacterial infections
furamidine	Preclinical	protein arginine N-methyltransferase inhibitor	PRMT1		
furazolidone	Launched	bacterial DNA inhibitor		gastroenterology|infectious disease	diarrhea|enteritis|cholera
furegrelate	Phase 1	thromboxane synthase inhibitor	TBXAS1		
furosemide	Launched	diuretic	CA2|GPR35|SLC12A1|SLC12A2	cardiology|rheumatology	edema|hypertension|congestive heart failure|nephrotic syndrome
fursultiamine	Launched	vitamin B		metabolism	thiamine deficiency
furvina	Preclinical	quorum sensing signaling inhibitor			
fusidic-acid	Launched	bacterial 30S ribosomal subunit inhibitor		dermatology	acne vulgaris (AV)
futibatinib	Phase 3	FGFR inhibitor			
F351	Phase 2	TGF beta receptor inhibitor	TGFB1		
g-caryophyllene	Preclinical	acetylcholinesterase inhibitor	ACHE		
G-1	Preclinical	G protein-coupled receptor agonist	GPER1		
G-15	Preclinical	estrogen receptor antagonist	GPER1		
G-749	Preclinical	tyrosine kinase inhibitor			
GABA-linoleamide	Phase 2	benzodiazepine receptor agonist			
gabapentin	Launched	calcium channel blocker	ADORA1|CACNA1A|CACNA1B|CACNA1C|CACNA1D|CACNA1E|CACNA1F|CACNA1G|CACNA1H|CACNA1I|CACNA1S|CACNA2D1|CACNA2D2|CACNA2D3|CACNA2D4|CACNB1|CACNB2|CACNB3|CACNB4|CACNG1|CACNG2|CACNG3|CACNG4|CACNG5|CACNG6|CACNG7|CACNG8|GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|GRIN3A|GRIN3B	infectious disease|neurology/psychiatry	virus herpes simplex (HSV)|shingles|seizures|restless leg syndrome
gabapentin-enacarbil	Launched	adrenergic receptor agonist	CACNA1G	neurology/psychiatry	restless leg syndrome|postherpetic neuralgia
gabazine	Preclinical	GABA receptor antagonist	GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRG2		
gabexate	Launched	serine protease inhibitor	PRSS1|TPSAB1	gastroenterology	pancreatitis
gaboxadol	Phase 3	benzodiazepine receptor agonist	GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRD|GABRR1|GABRR2|GABRR3		
gadobutrol	Launched	radiopaque medium		radiology	MRI contrast agent
gadodiamide	Launched	radiopaque medium		radiology	MRI contrast agent
gadopentetic-acid	Launched	contrast agent	PGD	radiology	contrast agent
gadoterate-meglumine	Launched	radiopaque medium		radiology	MRI contrast agent
gadoteridol	Launched	radiopaque medium		radiology	MRI contrast agent
GAL-021	Preclinical	calcium channel blocker			
galantamine	Launched	acetylcholinesterase inhibitor	ACHE|BCHE|CHRNA1|CHRNA10|CHRNA2|CHRNA3|CHRNA4|CHRNA5|CHRNA6|CHRNA7|CHRNA9|CHRNB1|CHRNB2|CHRNB3|CHRNB4|CHRND|CHRNE|CHRNG	neurology/psychiatry	senile dementia
galeterone	Phase 3	androgen receptor modulator	AR|CYP17A1		
galidesivir	Phase 1	antiviral			
gallamine-triethiodide	Launched	acetylcholine receptor antagonist	CHRM2|CHRNA1	neurology/psychiatry	muscle relaxant
gallic-acid	Preclinical	beta amyloid protein neurotoxicity inhibitor|PPAR receptor agonist	CA1|CA12|CA14|CA2|CA4|CA6|CA9|SELP		
gallium-triquinolin-8-olate	Phase 1				
gallopamil	Launched	L-type calcium channel blocker	ATP2A2	cardiology	hypertension|cardiac arrythmia
gambogic-acid	Phase 2	caspase activator	BCL2		
gamithromycin	Preclinical	antibacterial 			
gamma-aminobutyric-acid	Preclinical	benzodiazepine receptor agonist	GABBR1|GABBR2|GABRA1|GABRA2|GABRA3|GABRA5|GABRB2|GABRG2|GATM|KCTD12|KCTD16|KCTD8|SLC6A1		
gamma-linolenic-acid	Phase 2	cyclooxygenase inhibitor|prostanoid receptor agonist	PTGS1|PTGS2		
ganaxolone	Phase 3	GABA receptor modulator	GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6		
ganciclovir	Launched	DNA polymerase inhibitor		infectious disease	cytomegalovirus (CMV)
ganetespib	Phase 3	HSP inhibitor	HSP90AA1		
ganoderic-acid-a	Preclinical	JAK inhibitor			
GANT-58	Preclinical	GLI antagonist	GLI1		
GANT-61	Preclinical	GLI antagonist	GLI1|GLI2		
garenoxacin	Launched	topoisomerase inhibitor	TOP2A	infectious disease	respiratory tract infections
gastrodin	Phase 2				
gatifloxacin	Withdrawn	bacterial DNA gyrase inhibitor			
gavestinel	Phase 3	glutamate receptor antagonist	GLRB|GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|GRIN3A|GRIN3B		
GBR-12783	Preclinical	dopamine reuptake inhibitor			
GBR-12935	Preclinical	dopamine reuptake inhibitor	AGTR1|SLC6A3		
GBR-13069	Preclinical	dopamine reuptake inhibitor	SLC6A3		
GDC-0068	Phase 3	AKT inhibitor	AKT1|AKT2|AKT3|PRKG1		
GDC-0077	Phase 1	PI3K inhibitor			
GDC-0084	Phase 2	mTOR inhibitor|PI3K inhibitor			
GDC-0152	Phase 1	XIAP inhibitor	BIRC2|BIRC3|BIRC7|XIAP		
GDC-0349	Phase 1	Pim kinase inhibitor	PIK3CA		
GDC-0575	Phase 1	CHK inhibitor			
GDC-0623	Phase 1	MEK inhibitor			
GDC-0810	Phase 2	selective estrogen receptor destabilizer	ESR1		
GDC-0834	Phase 1	Bruton's tyrosine kinase (BTK) inhibitor	BTK		
GDC-0879	Preclinical	RAF inhibitor	BRAF		
GDC-0927	Phase 1	estrogen receptor antagonist			
GDC-0941	Phase 2	PI3K inhibitor	PIK3CA|PIK3CB|PIK3CD|PIK3CG		
GDC-0980	Phase 2	mTOR inhibitor|PI3K inhibitor	FGR|MAP3K9|MTOR|PIK3CA|PIK3CB|PIK3CD|PIK3CG|SYK		
GDC-0994	Phase 1	MAP kinase inhibitor	MAPK1|MAPK3		
gedunin	Preclinical	HSP inhibitor	HSP90AA1		
gefapixant	Phase 3	purinergic receptor antagonist			
gefitinib	Launched	EGFR inhibitor	EGFR	oncology	non-small cell lung cancer (NSCLC)
geldanamycin	Preclinical	HSP inhibitor	HSP90AA1		
gemcadiol	Phase 2	antilipemic			
gemcitabine	Launched	ribonucleotide reductase inhibitor	CMPK1|RRM1|RRM2|TYMS	oncology	ovarian cancer|breast cancer|non-small cell lung cancer (NSCLC)|pancreatic cancer
gemcitabine-elaidate	Phase 1	apoptosis inhibitor|DNA synthesis inhibitor	CMPK1|RRM1|TYMS		
gemfibrozil	Launched	lipoprotein lipase activator	LPL|PPARA|SLCO1B1|SLCO1B3|SLCO2B1	endocrinology|cardiology	hyperlipidemia|coronary heart disease
gemifloxacin	Launched	bacterial DNA gyrase inhibitor		pulmonary|infectious disease	bronchitis|pneumonia
gemigliptin	Launched	dipeptidyl peptidase inhibitor			
genipin	Preclinical	choleretic agent			
geniposide	Preclinical	GLP receptor agonist	GLP1R		
geniposidic-acid	Preclinical	cyclooxygenase inhibitor			
genistein	Phase 2/Phase 3	tyrosine kinase inhibitor	CFTR|ESR1|ESR2|ESRRA|ESRRB|ESRRG|NCOA1|NCOA2|PPARG|PTK2B|TOP2A|TRPC5		
gentamycin	Launched	bacterial 50S ribosomal subunit inhibitor	HSPA8	infectious disease|critical care	bone and joint infections|endocarditis|pelvic inflammatory disease|meningitis|pneumonia|urinary tract infections|sepsis
gentiopicrin	Phase 3	glutamate receptor downregulator	GRIN2B		
genz-123346	Preclinical	glucosylceramidase inhibitor	UGCG		
genz-644282	Phase 1	topoisomerase inhibitor	TOP1		
gepefrine	Launched	adrenergic receptor agonist		cardiology	hypotension
gepon	Phase 1				
gepotidacin	Phase 2	topoisomerase inhibitor			
geranyl-farnesylacetate	Phase 2	mucin production enhancer			
gestodene	Launched	contraceptive agent		endocrinology	contraceptive
gestrinone	Launched	progesterone receptor antagonist	AR|ESR1|PGR	obstetrics/gynecology	endometriosis
GF109203X	Preclinical	PKC inhibitor	PDPK1|PIM1|PRKCI|PRKCZ		
GGsTop	Preclinical	gamma glutamyltransferase Inhibitor	GGT1		
GGTI-298	Preclinical	GGTase inhibitor	CDKN1A		
gilteritinib	Launched	FLT3 inhibitor	FLT3		
gimeracil	Launched	dihydropyrimidine dehydrogenase inhibitor	DPYD	oncology	gastric adenocarcinoma
ginkgolide-A	Preclinical	GABA receptor antagonist	GLRA1|GLRB		
ginkgolide-B	Phase 3	platelet activating factor receptor antagonist	GLRA1|GLRA2|GLRA3|GLRB|HTR3A|HTR3B		
ginsenoside-C-K	Phase 1	NFkB pathway inhibitor|nitric oxide synthase inhibitor	PTGS2		
ginsenoside-RD	Phase 3	calcium channel blocker			
ginsenoside-RE	Phase 1	anti-inflammatory agent			
ginsenoside-RE3	Launched	angiogenesis inhibitor|apoptosis stimulant	KCNH2		
givinostat	Phase 3	HDAC inhibitor	HDAC1|HDAC2|HDAC3|HDAC4|HDAC5|HDAC6|HDAC7|HDAC8|HDAC9		
GKA-50	Preclinical	glucokinase activator	GCK		
GKT137831	Phase 2	NADPH oxidase inhibitor	NOX1|NOX4		
GK921	Preclinical	transglutaminase inhibitor	TGM2		
glafenine	Withdrawn	DeltaF508-CFTR Correctors	CFTR		
glasdegib	Launched	hedgehog pathway inhibitor	SMO	hematologic malignancy	acute myeloid leukemia (AML)
glecaprevir	Launched	serine protease inhibitor		infectious disease	hepatitis C
glesatinib	Phase 2	tyrosine kinase inhibitor			
gliclazide	Launched	ATP channel blocker|insulin secretagogue		endocrinology	diabetes mellitus
glimepiride	Launched	insulin secretagogue	ABCC8|KCNJ1|KCNJ11	endocrinology	diabetes mellitus
glipizide	Launched	sulfonylurea	ABCC8|KCNJ10|KCNJ11|PPARG	endocrinology	diabetes mellitus|hyperglycemia
gliquidone	Launched	sulfonylurea	ABCC8|KCNJ10|KCNJ8	endocrinology	diabetes mellitus
Gln-1062	Preclinical	cholinesterase inhibitor			
GLPG0187	Phase 1	integrin antagonist			
GLPG0492	Phase 1	androgen receptor modulator	AR		
GLPG0492-R-enantiomer	Phase 1	androgen receptor modulator	AR		
GLPG1837	Phase 2	CFTR channel potentiator			
glucaric-acid	Phase 1				
gluconolactone	Launched		LCT		
glucosamine	Launched	glycosylated protein precursor	IL1B	neurology/psychiatry|rheumatology	muscle pain|rheumatoid arthritis|joint pain|backache
glutathione	Phase 3	antioxidant	ESD|GGT1|GLO1|GLRX|GLRX2|GPX1|GPX2|GPX3|GPX4|GPX5|GPX6|GPX7|GPX8|GSR|GSS|GSTA1|GSTA2|GSTA3|GSTA4|GSTA5|GSTK1|GSTM1|GSTM2|GSTM3|GSTM4|GSTM5|GSTO1|GSTO2|GSTP1|GSTT1|GSTZ1|HAGH|HPGDS|LTC4S|MGST1|MGST2|MGST3|TXNDC12		
glutathione-monoisopropyl-ester	Phase 2	lipid peroxidase inhibitor			
gly-gln	Phase 2				
glyburide	Launched	ATP channel blocker|insulin secretagogue|sulfonylurea	ABCA1|ABCB11|ABCC8|ABCC9|CFTR|CPT1A|KCNJ1|KCNJ11|KCNJ5|KCNJ8|SLCO2B1	endocrinology	diabetes mellitus|hyperglycemia
glycerol-monolaurate	Launched	beta lactamase inhibitor			
glycerol-phenylbutyrate	Phase 1	sigma receptor ligand			
glycitein	Phase 3	tumor necrosis factor release inhibitor	TNF		
glycopyrrolate	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5	gastroenterology	peptic ulcer disease (PUD)
GM-1485	Preclinical	immunophilin ligand	FKBP1A		
GMX1778	Phase 1/Phase 2	NAMPT inhibitor	NAMPT		
GNE-7915	Preclinical	leucine rich repeat kinase inhibitor			
GNF-2	Preclinical	Bcr-Abl kinase inhibitor	ABL1|BCR		
GNF-5	Preclinical	Bcr-Abl kinase inhibitor	ABL1|BCR		
GNF-5837	Preclinical	growth factor receptor inhibitor	NTRK1|NTRK2|NTRK3		
GNF-7	Preclinical	glucokinase inhibitor|protein kinase inhibitor	GCK|TNK2		
GNTI	Preclinical	opioid receptor antagonist	OPRK1|OPRM1		
go-6983	Preclinical	protein kinase inhibitor	PRKCA|PRKCB|PRKCD|PRKCG|PRKCZ		
golgicide-A	Preclinical	ARF inhibitor	GBF1		
golvatinib	Phase 2	VEGFR inhibitor	KDR|MET		
gonadorelin	Launched	gonadotropin releasing factor hormone receptor agonist	GNRHR	obstetrics/gynecology	cystic ovaries|reproductive synchrony
goserelin-acetate	Launched	gonadotropin releasing factor hormone receptor agonist	GNRHR|LHCGR	oncology|obstetrics/gynecology	prostate cancer|breast cancer|endometriosis
gossypol	Phase 2	BCL inhibitor|MCL1 inhibitor	BCL2		
GPBAR-A	Preclinical	G protein-coupled receptor agonist	GPBAR1		
GPI-1046	Preclinical	FKBP inhibitor	FKBP1A		
GPi-688	Preclinical	glycogen phosphorylase inhibitor			
GPP-78	Preclinical	NAMPT inhibitor	NAMPT		
GPR120-modulator-1	Preclinical	G protein-coupled receptor modulator	FFAR4		
GP1a	Preclinical	cannabinoid receptor agonist	CNR2		
GP2a	Preclinical	cannabinoid receptor agonist	CNR2		
GR-103691	Preclinical	dopamine receptor antagonist	DRD3		
GR-113808	Preclinical	serotonin receptor antagonist	HTR4		
GR-127935	Preclinical	serotonin receptor antagonist	HTR1A|HTR1B|HTR1D|HTR1E|HTR1F|HTR2A|HTR2B|HTR2C|HTR6		
GR-135531	Preclinical	melatonin receptor agonist			
GR-144053	Preclinical	integrin antagonist	ITGA2B|ITGB3		
GR-159897	Preclinical	tachykinin antagonist	TAC1|TACR2		
GR-235	Launched	estrogen receptor agonist|FXR antagonist|progesterone receptor agonist	NR1H4		
GR-79236	Phase 1	adenosine receptor agonist	ADORA1|ADORA2A		
gramicidin	Launched	bacterial permeability inducer		infectious disease	first-aid antibiotic
gramine	Preclinical	norepinephrine reputake inhibitor			
granisetron	Launched	serotonin receptor antagonist	HTR3A	gastroenterology	nausea|vomiting
grapiprant	Launched	prostaglandin inhibitor	PTGER4	rheumatology	osteoarthritis
grazoprevir	Launched	HCV inhibitor		infectious disease	hepatitis C
griseofulvin	Launched	tubulin polymerization inhibitor	KRT12	infectious disease	ringworm|tinea pedis
GR125487	Preclinical	serotonin receptor antagonist	HTR4		
GR46611	Preclinical	serotonin receptor agonist	HTR1D		
GS-143	Preclinical	ubiquitin ligase inhibitor	BTRC|NFKBIA		
GS-39783	Preclinical	GABA receptor modulator	GABBR1		
GS-6201	Phase 1	adenosine receptor antagonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
GS-9620	Phase 2	toll-like receptor agonist	TLR7		
GS-967	Preclinical	voltage-gated sodium channel blocker			
GS-9973	Phase 2	SYK inhibitor	SYK		
GSK-J1	Preclinical	histone demethylase inhibitor	KDM6B		
GSK-J2	Preclinical	histone demethylase inhibitor			
GSK-J4	Preclinical	histone lysine demethylase inhibitor	KDM6A|KDM6B		
GSK-J5	Preclinical	histone demethylase control			
GSK-LSD-1	Preclinical	histone lysine demethylase inhibitor	KDM1A		
GSK-3-inhibitor-IX	Preclinical	glycogen synthase kinase inhibitor|lipoxygenase inhibitor	GSK3A|GSK3B		
GSK0660	Preclinical	PPAR receptor antagonist	PPARD		
GSK1059615	Phase 1	PI3K inhibitor	PIK3CG		
GSK1070916	Phase 1	Aurora kinase inhibitor	AURKA|AURKB|AURKC|CYP2D6|CYP3A4		
GSK1292263	Phase 2	glucose dependent insulinotropic receptor agonist	GRPR		
GSK1562590	Preclinical	urotensin receptor antagonist	UTS2R		
GSK163090	Phase 2	serotonin receptor antagonist	HTR1A|HTR1B|HTR1D		
GSK1838705A	Preclinical	insulin growth factor receptor inhibitor	ALK|IGF1R|INSR|RPS6KA1		
GSK189254	Phase 2	histamine receptor antagonist			
GSK1904529A	Preclinical	IGF-1 inhibitor|insulin growth factor receptor inhibitor|insulin receptor ligand	IGF1R|INSR		
GSK2110183	Phase 2	AKT inhibitor	AKT1|AKT2|AKT3		
GSK2126458	Phase 1	mTOR inhibitor|PI3K inhibitor	MTOR|PIK3CA|PIK3CB|PIK3CD|PIK3CG		
GSK2190915	Phase 2	lipoxygenase inhibitor	ALOX5AP		
GSK2193874	Preclinical	transient receptor potential channel antagonist	TRPV4		
GSK2194069	Preclinical	fatty acid synthase inhibitor	FASN		
GSK2239633A	Preclinical	CC chemokine receptor antagonist			
GSK2256098	Phase 2	kinase inhibitor			
GSK2256294A	Phase 1	epoxide hydolase inhibitor	EPHX2		
GSK2330672	Phase 2	bile acid transporter inhibitor	SLC10A2		
GSK2334470	Preclinical	phosphoinositide dependent kinase inhibitor	AURKA|AURKB|PDPK1		
GSK239512	Preclinical	histamine receptor antagonist			
GSK256066	Phase 2	phosphodiesterase inhibitor	PDE4A		
GSK2578215A	Preclinical	leucine rich repeat kinase inhibitor	LRRK2		
GSK2606414	Preclinical	protein kinase inhibitor	EIF2AK3|MYLK2		
GSK2636771	Phase 2	PI3K inhibitor	PIK3CB		
GSK2656157	Preclinical	PERK inhibitor			
GSK269962	Preclinical	rho associated kinase inhibitor	ROCK1|ROCK2		
GSK2801	Preclinical	bromodomain inhibitor	BAZ2A|BAZ2B		
GSK2816126	Phase 1	histone lysine methyltransferase inhibitor	EZH2		
GSK2830371	Preclinical	protein phosphatase inhibitor	PPM1D		
GSK2837808A	Preclinical	lactate dehydrogenase inhibitor	LDHA		
GSK2838232	Phase 2	HIV gag inhibitor			
GSK2879552	Phase 1/Phase 2	histone lysine demethylase inhibitor	KDM1A		
GSK2881078	Phase 2	androgen receptor modulator			
GSK2981278	Phase 1/Phase 2	ROR modulator			
GSK2982772	Phase 2	RIPK inhibitor			
GSK3117391	Phase 1/Phase 2	HDAC inhibitor			
GSK3179106	Phase 1	RET tyrosine kinase inhibitor			
GSK3326595	Phase 1/Phase 2	protein arginine N-methyltransferase inhibitor			
GSK356278	Preclinical	phosphodiesterase inhibitor			
GSK369796	Phase 1	potassium channel antagonist			
GSK37647	Preclinical	free fatty acid receptor agonist	FFAR4		
GSK3787	Preclinical	PPAR receptor antagonist	PPARD		
GSK429286A	Preclinical	rho associated kinase inhibitor	ROCK1		
GSK461364	Phase 1	PLK inhibitor	PLK1		
GSK503	Preclinical	histone lysine methyltransferase inhibitor	EZH2		
GSK650394	Preclinical	serum/glucocorticoid regulated kinase inhibitor	SGK1|SGK2		
GSK656	Preclinical	leucyl-tRNA synthetase inhibitor			
GSK690693	Phase 1	AKT inhibitor	AKT1|AKT2|AKT3|PAK4|PAK6|PAK7|PRKCQ|PRKG1|PRKX		
GSK9027	Preclinical	glucocorticoid receptor agonist	NR3C1		
GSK923295	Phase 1	centromere associated protein inhibitor	CENPE		
GTP-14564	Preclinical	FLT3 inhibitor|tyrosine kinase inhibitor	CSF1R|FLT3|KIT|PDGFRB		
GTS21	Phase 1/Phase 2	cholinergic receptor agonist	CHRNA7		
guacetisal	Launched	immunosuppressant		pulmonary	cough suppressant
guadecitabine	Phase 3	DNA methyltransferase inhibitor			
guaiacol	Launched	local anesthetic	CA2	pulmonary	cough suppressant
guaifenesin	Launched	expectorant		pulmonary	cough suppressant
guanaben-acetate	Launched	adrenergic receptor agonist	ADRA2A|ADRA2B|ADRA2C	cardiology	hypertension
guanadrel	Launched	adrenergic inhibitor		cardiology	hypertension
guancydine	Preclinical	antihypertensive agent			
guanethidine	Launched	adrenergic inhibitor	SLC6A2	cardiology	hypertension
guanfacine	Launched	adrenergic receptor agonist	ADRA2A|ADRA2B|ADRA2C	cardiology	hypertension
guanidine	Launched	HSP inhibitor	ALDH2|DLG4|GAMT|RNASE1	neurology/psychiatry	Lambert-Eaton myasthenic syndrome (LEMS)
guanidinoethyldisulfide-bicarbonate	Phase 2	nitric oxide synthase inhibitor	NOS2		
guanidinopropionic-acid	Phase 2	creatine kinase inhibitor	CKM		
guanosine	Preclinical		PNP		
Gue-1654	Preclinical	oxoeicosanoid receptor modulator	OXER1		
guvacine	Preclinical	GABA uptake inhibitor	SLC6A1|SLC6A11|SLC6A12|SLC6A13		
GW-0742	Preclinical	PPAR receptor agonist	PPARD		
GW-1100	Preclinical	G protein-coupled receptor agonist	FFAR1		
GW-1929	Preclinical	PPAR receptor agonist	PPARG		
GW-2580	Preclinical	cFMS kinase inhibitor	CSF1R		
GW-311616	Phase 1	elastase inhibitor|leukocyte elastase inhibitor	ELANE		
GW-3965	Preclinical	LXR agonist	NR1H2|NR1H3		
GW-405833	Preclinical	cannabinoid receptor agonist	CNR2		
GW-4064	Preclinical	FXR agonist	NR1H4		
GW-438014A	Preclinical	neuropeptide receptor antagonist	NPY5R		
GW-441756	Preclinical	growth factor receptor inhibitor	NTRK1		
GW-501516	Phase 2	PPAR receptor agonist	PPARA|PPARD		
GW-5074	Phase 1/Phase 2	leucine rich repeat kinase inhibitor|RAF inhibitor	NTRK1|RAF1		
GW-542573X	Preclinical	calcium channel activator	KCNN1		
GW-583340	Preclinical	EGFR inhibitor	EGFR|ERBB2		
GW-627368	Preclinical	prostanoid receptor antagonist	PTGER4		
GW-6471	Preclinical	PPAR receptor antagonist	PPARA		
GW-7647	Preclinical	PPAR receptor agonist	PPARA		
GW-788388	Preclinical	ALK tyrosine kinase receptor inhibitor	LCK|MAPK14|TGFBR1		
GW-803430	Phase 1	melanin inhibitor	KCNH2|MCHR1		
GW-842166	Phase 2	cannabinoid receptor agonist	CNR2		
GW-843682X	Preclinical	PLK inhibitor	PLK1|PLK3		
GW-9508	Preclinical	free fatty acid receptor agonist|G protein-coupled receptor agonist	FFAR1|FFAR4		
GW-9662	Preclinical	PPAR receptor antagonist	NCOA2|PPARG|RXRA		
GW274150	Phase 2	nitric oxide synthase inhibitor			
GYKI-52466	Preclinical	glutamate receptor antagonist	GRIA1|GRIA2|GRIA3|GRIA4		
gynostemma-extract	Phase 2	calcium channel modulator			
GZD824	Preclinical	Bcr-Abl kinase inhibitor	ABL1|BCR		
G007-LK	Preclinical	tankyrase inhibitor	TNKS|TNKS2		
H-151	Preclinical	STING antagonist			
H-89	Preclinical	PKA inhibitor	GSG2|PKIA|PRKACA		
HA-1004	Phase 2	calcium channel blocker			
HA-130	Preclinical	autotaxin inhibitor	ENPP2		
HA-966-(R)-(+)	Preclinical	glutamate receptor agonist	GRIA1		
HA-966-(S)-(-)	Preclinical	glutamate receptor antagonist	GRIA1		
halazone	Launched			infectious disease	disinfectant
halcinonide	Launched	glucocorticoid receptor agonist	NR3C1	dermatology	corticosteroid-responsive dermatoses
halobetasol-propionate	Launched	glucocorticoid receptor agonist	NR3C1|PLA2G1B	dermatology	corticosteroid-responsive dermatoses
halofantrine	Launched	antimalarial agent	KCNN4	infectious disease	malaria
halofuginone	Launched	collagenase inhibitor	COL1A1|MMP2	rheumatology	scleroderma
halopemide	Phase 2	phospholipase inhibitor	PLD1|PLD2		
haloperidol	Launched	dopamine receptor antagonist	DRD1|DRD2|DRD3|DRD4|DRD5|GRIN2B|HRH1|HTR1A|HTR1D|HTR2A|HTR2B|HTR7|KCNH1	neurology/psychiatry	schizophrenia|Tourette's disorder
haloperidol-decanoate	Launched	psychoactive drug	DRD2|DRD3|DRD4|HTR2A	neurology/psychiatry	schizophrenia
haloprogin	Launched	other antifungal		infectious disease	tinea pedis
halothane	Launched	glutamate receptor antagonist	GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ|GLRA1|GLRB|KCNK10|KCNK12|KCNK13|KCNK15|KCNK18|KCNK2|KCNK3|KCNK9	neurology/psychiatry	general anaesthetic
harmane	Preclinical	monoamine oxidase inhibitor	MAOA|MAOB		
harringtonine	Phase 3	protein synthesis inhibitor			
HA14-1	Preclinical	BCL inhibitor	BCL2		
HBED	Phase 3	chelating agent			
HC-030031	Phase 1	TRPA1 channel blocker	TRPA1		
HC-067047	Preclinical	transient receptor potential channel antagonist	TRPV4		
HC-070	Preclinical	transient receptor potential channel antagonist			
heclin	Preclinical	ubiquitin ligase inhibitor	NEDD4|SMURF2|WWP1		
HEMADO	Preclinical	adenosine receptor agonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
hematoporphyrin	Launched			neurology/psychiatry	depression|psychosis
hematoxylin	Preclinical				
hemin	Launched	enzyme inducer		hematology|cardiology	acute intermittent porphyria (AIP)|hypertension|ventricular tachycardia (VT)
hemomex-s	Launched		PPARG		
hepsulfam	Preclinical	DNA cross-linking			
heptaminol	Launched	vasoconstrictor		cardiology	hypotension
HER2-Inhibitor-1	Preclinical	EGFR inhibitor			
hesperadin	Preclinical	Aurora kinase inhibitor	AURKB		
hesperetin	Launched	ACAT inhibitor	DGAT1|MTTP|SOAT1|SOAT2		
hesperidin	Launched	flavanone glycoside	AURKB|CACNA1B		
hetacillin	Launched	bacterial cell wall synthesis inhibitor		obstetrics/gynecology	mastitis
hexachlorophene	Launched	potassium channel activator	GLUD1|SDHD	infectious disease	gram-positive bacterial infections
hexamethonium	Preclinical	cholinergic receptor antagonist	CHRNA2|CHRNA3|CHRNA4|CHRNA6		
hexamethylenebisacetamide	Phase 2	AKT inhibitor|differentiation inducer|NFKB pathway inhibitor	AKT1		
hexaminolevulinate	Launched			radiology	diagnostic agent
hexasodium-phytate	Phase 2				
hexestrol	Launched	synthetic estrogen	AKR1C1|ESR1|ESR2	endocrinology	hypoestrogenism
hexetidine	Launched	local anesthetic		otolaryngology|infectious disease|dental|gastroenterology	pharyngitis|meningitis|laryngitis|gingivitis|ulcerative colitis
hexonic-acid	Preclinical				
hexoprenaline	Launched	adrenergic receptor agonist	ADRB2	pulmonary	asthma
hexylcaine	Launched	sodium channel blocker	SCN5A	neurology/psychiatry	local anesthetic
hexylene-glycol	Preclinical		AKR1C3|CTPS1|DLG4|HSP90AA1|NOS3|PGF|PLA2G1B|PTPN1|SELP		
hexylresorcinol	Launched	local anesthetic	TYR	infectious disease	skin infections|first-aid antiseptic
higenamine	Phase 1	adrenergic receptor agonist	ADRB2		
hippuric-acid	Preclinical				
histamine	Launched	histamine receptor agonist	HRH1|HRH2|HRH3|HRH4	allergy	allergic rhinitis
HJC-0350	Preclinical	GTPase inhibitor	RAPGEF4		
HKI-357	Phase 1	EGFR inhibitor	EGFR		
HLCL-61	Preclinical	protein arginine N-methyltransferase inhibitor	PRMT5		
HM-30181	Phase 1	P glycoprotein inhibitor			
HMN-214	Phase 1	PLK inhibitor	PLK1		
HOKU-81	Preclinical	bronchodilator			
homatropine	Launched	acetylcholine receptor antagonist	CHRM1	ophthalmology	uveal tract inflammation|pupil dilation
homatropine-methylbromide	Launched	acetylcholine receptor antagonist	CHRM5	ophthalmology	uveal tract inflammation
homidium	Preclinical				
homochlorcyclizine	Launched	antihistamine	HRH1	allergy	allergic rhinitis
homoharringtonine	Launched	protein synthesis inhibitor	RPL3	hematologic malignancy	chronic myeloid leukemia (CML)
homoquinolinic-acid	Preclinical	glutamate receptor agonist	GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D		
homosalate	Preclinical	HSP inducer			
homoveratrylamine	Preclinical	monoamine oxidase inhibitor			
honokiol	Phase 3	AKT inhibitor	ALOX5|PTGS1|PTGS2		
hordenine	Preclinical				
HP-228	Preclinical	nitric oxide synthase inhibitor			
hPGDS-IN-1	Preclinical	prostaglandin inhibitor			
HPPH	Phase 2	photosensitizing agent			
HQK-1001	Phase 2				
HSR6071	Preclinical	antiallergic agent			
HT-2157	Phase 1/Phase 2	galanin receptor 3 antagonist			
HTH-01-015	Preclinical	protein kinase inhibitor	NUAK1		
HTHQ	Preclinical	antioxidant			
HTMT	Preclinical	histamine receptor agonist	HRH4		
huperzine-A	Phase 2	acetylcholinesterase inhibitor	ACHE		
hyaluronic-acid	Launched		C1QBP|CD44|HABP2|HAPLN1|HAPLN3|HAPLN4|HMMR|ICAM1|NCAN|VCAN	rheumatology|urology	osteoarthritis|interstitial cystitis (IC)
hycanthone	Launched	RNA synthesis inhibitor		infectious disease	schistosomiasis
hydralazine	Launched	vasodilator		cardiology	hypertension
"hydrastine-(1R,9S)"	Preclinical	tyrosine hydroxylase inhibitor			
hydrastinine	Preclinical	hemostatic agent			
hydrochlorothiazide	Launched	thiazide diuretic	CA1|CA12|CA2|CA4|CA9|KCNMA1|SLC12A3	cardiology	hypertension|congestive heart failure
hydrocortisone	Launched	glucocorticoid receptor agonist	ANXA1|NOS2|NR3C1|NR3C2	dermatology|neurology/psychiatry	eczema|psoriasis|seborrheic dermatitis|itching
hydrocortisone-acetate	Launched	glucocorticoid receptor agonist	NR3C1	dermatology	corticosteroid-responsive dermatoses
hydrocortisone-butyrate	Launched	glucocorticoid receptor agonist	NR3C1	dermatology	corticosteroid-responsive dermatoses|eczema
hydrocortisone-hemisuccinate	Phase 2/Phase 3				
hydrocortisone-phosphate	Launched			pulmonary|gastroenterology|hematologic malignancy|ophthalmology	asthma|nausea|vomiting|multiple myeloma|contact dermatitis|enteritis|colitis
hydrocortisone-valerate	Launched	glucocorticoid receptor agonist	NR3C1	dermatology	corticosteroid-responsive dermatoses
hydroflumethiazide	Launched	sodium/potassium/chloride transporter inhibitor	ATP1A1|CA1|CA12|CA2|CA4|CA9|KCNMA1|SLC12A1|SLC12A3	cardiology|gastroenterology|rheumatology|nephrology	edema|congestive heart failure|hepatic cirrhosis|nephrotic syndrome|chronic renal failure|acute glomerulonephritis (AGN)|hypertension
hydroquinidine	Launched	antiarrhythmic		cardiology	cardiac arrythmia
hydroquinone	Launched	melanin inhibitor	TYR	dermatology	dyschromia
hydroxocobalamin	Launched	vitamin B			
hydroxyamphetamine	Launched	trace amine associated receptor agonist	TAAR1	ophthalmology	mydriasis
hydroxychloroquine	Launched	antimalarial agent	TLR7|TLR9	infectious disease	malaria
hydroxyfasudil	Preclinical	rho associated kinase inhibitor	PKIA|PRKACA|ROCK1		
hydroxyprogesterone	Launched	progesterone receptor agonist	PGR	obstetrics/gynecology	spontaneous preterm birth
hydroxyprogesterone-acetate	Launched	progesterone receptor agonist	PGR		
hydroxypropyl-beta-cyclodextrin	Phase 2/Phase 3				
hydroxysafflor-yellow-A	Preclinical	antitumor agent			
hydroxystilbamidine	Launched				
"hydroxytacrine-maleate-(R,S)"	Preclinical	cholinesterase inhibitor	ACHE		
hydroxytoluic-acid	Preclinical				
hydroxyurea	Launched	ribonucleotide reductase inhibitor	RRM1|RRM2|RRM2B	hematologic malignancy|oncology	chronic myeloid leukemia (CML)|head and neck squamous cell carcinoma (HNSCC)
hydroxyzine	Launched	antihistamine	HRH1	neurology/psychiatry|allergy|dermatology	anxiety|urticaria|itching|dermatosis
hygromycin-B	Preclinical	polypeptide synthesis inhibitor			
hymecromone	Phase 2	monoamine oxidase inhibitor	MAOA|MAOB		
hyodeoxycholic-acid	Phase 1	atherosclerosis formation inhibitor			
hyoscyamine	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4	gastroenterology|urology|neurology/psychiatry|allergy	peptic ulcer disease (PUD)|acute abdominal visceral spasm|ulcerative colitis|interstitial cystitis (IC)|enterocolitis|irritable bowel syndrome|tremors|allergic rhinitis
hypericin	Phase 3	tyrosine kinase inhibitor			
hyperin	Preclinical	aldose reductase inhibitor	ACE|AKR1B1		
hypoestoxide	Phase 1	IKK inhibitor	IKBKB|IL1B|TNF		
hypoxanthine	Preclinical	PARP inhibitor	PNP		
H2L-5765834	Preclinical	lysophosphatidic acid receptor antagonist	LPAR1|LPAR3		
I-BET-762	Phase 2	bromodomain inhibitor	BRD2|BRD3|BRD4		
I-BET151	Preclinical	bromodomain inhibitor	BRD2|BRD3|BRD4		
I-BRD9	Preclinical	bromodomain inhibitor	BRD9		
I-BZA	Phase 2				
I-BZA2	Phase 3				
I-CBP-112	Preclinical	bromodomain inhibitor	CREBBP|EP300		
IACS-10759	Preclinical	mitochondrial complex I inhibitor			
IB-MECA	Phase 3	adenosine receptor agonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
ibandronate	Launched	bone resorption inhibitor	FDPS	orthopedics	osteoporosis
IBC-293	Preclinical	hydroxycarboxylic acid receptor agonist	HCAR3		
iberdomide	Preclinical	cereblon modulator			
ibiglustat	Preclinical	glucosylceramidase inhibitor			
IBMX	Preclinical	phosphodiesterase inhibitor	ADORA1|PDE2A|PDE3B|PDE4D|PDE5A|PDE6G|PDE7A|PDE8A|PDE9A		
ibotenic-acid	Preclinical	glutamate receptor agonist	GRIN1		
ibrolipim	Phase 2	lipoprotein lipase activator	LPL		
ibrutinib	Launched	Bruton's tyrosine kinase (BTK) inhibitor	BLK|BMX|BTK	hematologic malignancy	chronic lymphocytic leukemia (CLL)|mantle cell lymphoma (MCL)|Waldenstrom's macroglobulinemia (WM)
ibudilast	Launched	leukotriene receptor antagonist|phosphodiesterase inhibitor	IL1B|IL6|PDE3A|PDE4A|PDE4B|PDE4C|PDE4D|PDE5A	pulmonary|neurology/psychiatry	asthma|stroke
ibuprofen	Launched	cyclooxygenase inhibitor		neurology/psychiatry|rheumatology|otolaryngology|obstetrics/gynecology|endocrinology|dental	headache|muscle pain|rheumatoid arthritis|backache|common cold|menstrual pain|fever|toothache
ibuprofen-(S)	Launched	cyclooxygenase inhibitor	ASIC1|PTGS1|PTGS2|SLC5A8	neurology/psychiatry	pain relief
ibuprofen-lysine	Launched	cyclooxygenase inhibitor		cardiology	patent ductus arteriosus (PDA)
ibuprofen-piconol	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	neurology/psychiatry	pain relief
ibuproxam	Launched	cyclooxygenase inhibitor|prostaglandin inhibitor	ALOX5	endocrinology|rheumatology|neurology/psychiatry	fever|joint inflammation|pain relief
ibutamoren	Phase 2	growth hormone secretagogue receptor agonist	GHR|GHSR		
ibutilide	Launched	potassium channel blocker	CACNA1C|KCNH2	cardiology	atrial fibrillation (AF)
ICA-069673	Preclinical	voltage-gated potassium channel activator	KCNQ2|KCNQ3		
ICA-110381	Preclinical	voltage-gated potassium channel activator	KCNQ2		
ICA-121431	Preclinical	sodium channel blocker	SCN1A|SCN3A		
icariin	Phase 3	phosphodiesterase inhibitor	PDE5A		
icaritin	Phase 3	PPAR receptor antagonist	PDE5A		
icatibant-acetate	Launched	bradykinin receptor antagonist	BDKRB2	cardiology	angioedema
ICG-001	Preclinical	beta-catenin inhibitor	CTNNB1		
"ICI-118,551"	Phase 2	adrenergic receptor antagonist	ADRB2|ADRB3		
ICI-162846	Phase 1	histamine receptor antagonist	HRH2		
ICI-169369	Phase 2	serotonin receptor antagonist			
"ICI-185,282"	Phase 1	thromboxane receptor antagonist			
ICI-192605	Phase 2	thromboxane receptor antagonist	TBXA2R		
ICI-199441	Preclinical	opioid receptor agonist	CYP2D6|OPRD1|OPRK1|OPRM1|UTS2R		
"ICI-215,001"	Preclinical	adrenergic receptor agonist	ADRB3		
ICI-63197	Preclinical	phosphodiesterase inhibitor			
ICI-89406	Phase 1	adrenergic receptor antagonist	ADRB1|ADRB2		
icilin	Phase 1	TRPV agonist	TRPA1|TRPM8		
iclaprim	Phase 3	dihydrofolate reductase inhibitor			
icomucret	Phase 3	mucin production enhancer	LTB4R2		
icosapent	Launched	platelet aggregation inhibitor	ACSL3|ACSL4|FADS1|FFAR1|PPARD|PPARG|PTGS1|PTGS2|SLC8A1|TRPV1	endocrinology	hypertriglyceridemia
icotinib	Launched	EGFR inhibitor	EGFR	oncology	non-small cell lung cancer (NSCLC)
iCRT-14	Preclinical	beta catenin inhibitor|WNT signaling inhibitor	CTNNB1|TCF4		
IC261	Preclinical	casein kinase inhibitor	CSNK1A1|CSNK1D|CSNK1E|CSNK1G2		
ID-1101	Phase 1	insulin sensitizer	INS		
ID-8	Preclinical				
idalopirdine	Phase 3	serotonin receptor antagonist	HTR6		
idarubicin	Launched	topoisomerase inhibitor	TOP2A	hematologic malignancy	acute myeloid leukemia (AML)
idasanutlin	Phase 3	MDM inhibitor	MDM2|TP53		
idazoxan	Phase 3	adrenergic receptor antagonist	ADRA2A|PTGS2		
idebenone	Launched	calcium channel modulator		neurology/psychiatry|ophthalmology	Alzheimer's disease|Friedreich's ataxia|Leber hereditary optic neuropathy (LHON)
idelalisib	Launched	PI3K inhibitor	PIK3CA|PIK3CB|PIK3CD|PIK3CG	hematologic malignancy	chronic lymphocytic leukemia (CLL)
IDF-11774	Preclinical	hypoxia inducible factor inhibitor			
IDH-305	Phase 2	isocitrate dehydrogenase inhibitor			
idoxuridine	Launched	DNA directed DNA polymerase inhibitor|DNA synthesis inhibitor		infectious disease	virus herpes simplex (HSV)
IDO5L	Preclinical	"indoleamine 2,3-dioxygenase inhibitor"	IDO1		
IDRA-21	Preclinical	glutamate receptor positive allosteric modulator	GRIA1|GRIA2|GRIA3|GRIA4		
idramantone	Preclinical				
idronoxil	Phase 3	XIAP inhibitor	ENOX2|SPHK1		
IEM1460	Preclinical	glutamate receptor antagonist	GRIA2		
IEM1754	Preclinical	glutamate receptor antagonist	GRIA1		
ifenprodil	Launched	adrenergic receptor antagonist|glutamate receptor antagonist	GRIN2B		
ifosfamide	Launched	DNA alkylating agent	CYP2A6|CYP2B6|CYP2C18|CYP2C19|CYP2C8|CYP2C9|CYP3A4|CYP3A5|CYP3A7|PTGS1	oncology|urology	testicular carcinoma|hemorrhagic cystitis
igmesine	Phase 2	sigma receptor agonist	SIGMAR1		
iguratimod	Launched	cyclooxygenase inhibitor|NFkB pathway inhibitor	PTGS2	rheumatology	rheumatoid arthritis
IKK-16	Preclinical	IKK inhibitor	IKBKB		
IKK-2-inhibitor	Preclinical	IKK inhibitor|SYK inhibitor	IKBKB		
IKK-2-inhibitor-V	Phase 1	IKK inhibitor|NFkB pathway inhibitor	IKBKB		
ilaprazole	Launched	proton pump inhibitor		gastroenterology	gastroesophageal reflux disease (GERD)
ilepcimide	Phase 3	anticonvulsant			
ilomastat	Phase 3	matrix metalloprotease inhibitor	ACAN|ADAM28|MMP1|MMP12|MMP13|MMP14|MMP2|MMP3|MMP8|MMP9		
iloperidone	Launched	dopamine receptor antagonist|serotonin receptor antagonist	ADRA1A|ADRA2C|DRD1|DRD2|DRD3|DRD4|HRH1|HTR1A|HTR2A|HTR6|HTR7	neurology/psychiatry	schizophrenia
iloprost	Launched	platelet aggregation inhibitor|prostanoid receptor agonist	PTGDR|PTGER1|PTGER2|PTGER3|PTGER4|PTGFR|PTGIR|TBXA2R	pulmonary	pulmonary arterial hypertension (PAH)
imatinib	Launched	Bcr-Abl kinase inhibitor|KIT inhibitor|PDGFR tyrosine kinase receptor inhibitor	ABL1|CSF1R|DDR1|KIT|NTRK1|PDGFRA|PDGFRB|RET	hematologic malignancy|oncology	chronic myeloid leukemia (CML)|acute lymphoblastic leukemia (ALL)|myelodysplastic diseases (MDS)|aggressive systemic mastocytosis (ASM)|hypereosinophilic syndrome (HES)|chronic eosinophilic leukemia (CEL)|dermatofibrosarcoma protuberans (DFSP)|gastrointestinal stromal tumors (GIST)
Imazodan	Phase 1	phosphodiesterase inhibitor			
imeglimin	Phase 2	gluconeogenesis inhibitor			
imetit	Preclinical	histamine receptor agonist	HRH3|HRH4		
imexon	Phase 2	apoptosis stimulant|ribonucleotide reductase inhibitor			
imidacloprid	Launched	acetylcholine receptor antagonist			
imidafenacin	Launched	acetylcholine receptor antagonist	CHRM1|CHRM3	neurology/psychiatry	spasms
imidapril	Launched	angiotensin converting enzyme inhibitor	ACE	cardiology	hypertension|congestive heart failure
imidazoacridinone	Preclinical	anticancer agent			
imidurea	Preclinical	other antibiotic			
imiloxan	Phase 1	adrenergic receptor antagonist	ADRA2A|ADRA2B		
imipenem	Launched	bacterial cell wall synthesis inhibitor		infectious disease	pneumonia|urinary tract infections|intra-abdominal infections|gynecologic infections|bacterial septicemia|bone and joint infections|skin infections|endocarditis
imipramine	Launched	norepinephrine reputake inhibitor|serotonin reuptake inhibitor	ADRA1A|ADRA1B|ADRA1D|CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|DRD1|DRD2|DRD5|HRH1|HTR1A|HTR2A|HTR2C|HTR6|HTR7|KCND2|KCND3|KCNH1|KCNH2|SLC6A2|SLC6A3|SLC6A4	neurology/psychiatry|urology	depression|nocturnal enuresis
imiquimod	Launched	interferon inducer|toll-like receptor agonist	TLR7|TLR8	dermatology|infectious disease|oncology	actinic keratosis (AK)|genital warts|basal cell carcinoma (BCC)
imirestat	Preclinical	aldose reductase inhibitor			
imisopasem-manganese	Preclinical	superoxide dismutase mimetic			
immepip	Preclinical	histamine receptor agonist	HRH3|HRH4		
immethridine	Phase 1	histamine receptor agonist	HRH3		
impentamine	Preclinical	histamine receptor antagonist	HRH3		
IMREG-1	Phase 3				
inarigivir	Phase 2	antiviral			
inarigivir-soproxil	Phase 2	antiviral			
INC-280	Phase 3	c-Met inhibitor	MET		
INCA-6	Preclinical	calcineurin inhibitor	NFATC1		
INCB-003284	Phase 2	CC chemokine receptor antagonist			
INCB-057643	Phase 1/Phase 2	bromodomain inhibitor			
INCB-3284	Phase 2	CC chemokine receptor antagonist	CCR2		
incyclinide	Phase 2	matrix metalloprotease inhibitor			
indacaterol	Launched	adrenergic receptor agonist	ADRB1|ADRB2	pulmonary	chronic obstructive pulmonary disease (COPD)
indalpine	Withdrawn	selective serotonin reuptake inhibitor (SSRI)	SLC6A4		
indapamide	Launched	thiazide diuretic	CA2|HTR3A|KCNQ1	cardiology	hypertension|congestive heart failure
indatraline	Preclinical	norepinephrine transporter inhibitor	MAOA|MAOB		
indeglitazar	Phase 2	PPAR receptor agonist	NCOA1|PPARA|PPARD|PPARG		
indeloxazine	Withdrawn	norepinephrine reuptake inhibitor|serotonin reuptake inhibitor			
indibulin	Phase 1/Phase 2	tubulin polymerization inhibitor			
indinavir	Launched	HIV protease inhibitor	CYP3A4|CYP3A5|CYP3A7	infectious disease	human immunodeficiency virus (HIV-1)
indiplon	Phase 3	benzodiazepine receptor agonist	GABRA1		
indirubin	Phase 2/Phase 3	CDK inhibitor|glycogen synthase kinase inhibitor	CDK1|CDK5|GSK3A		
indirubin-3-monoxime	Preclinical	CDK inhibitor|glycogen synthase kinase inhibitor	CDK1|CDK2|CDK5|CDK5R1|GSK3B		
indisulam	Phase 2	CDK inhibitor	CA1|CA12|CA14|CA2|CA6|CA7|CA9		
indium(III)-isopropoxide	Preclinical				
indium-tri(2-propanolate)	Preclinical				
indobufen	Launched	cyclooxygenase inhibitor|platelet aggregation inhibitor	PTGS1|PTGS2	hematology	thrombosis
indocyanine-green	Launched	contrast agent	SLCO1B1	cardiology	vascular imaging agent
indole-3-carbinol	Phase 2/Phase 3	"aryl hydrocarbon receptor agonist|indoleamine 2,3-dioxygenase inhibitor"	AHR		
indole-3-pyrubate	Phase 2	melatonin receptor agonist			
indomethacin	Launched	cyclooxygenase inhibitor	GLO1|PLA2G2A|PPARA|PPARG|PTGDR2|PTGR2|PTGS1|PTGS2|SLC46A1	rheumatology|orthopedics	rheumatoid arthritis|ankylosing spondylitis|osteoarthritis|bursitis|tendinitis
indoprofen	Withdrawn	cyclooxygenase inhibitor|prostanoid receptor antagonist	CXCR1|CXCR2|PTGS1|PTGS2		
indoramin	Launched	adrenergic receptor antagonist	ADRA1A|ADRA1B|ADRA1D|ADRA2B|ADRA2C	urology|cardiology	benign prostatic hyperplasia (BPH)|hypertension
indoximod	Phase 2	"indoleamine 2,3-dioxygenase inhibitor"	IDO1		
ingenol	Launched	PKC activator	PRKCD|PRKCE	dermatology	keratosis
ingenol-mebutate	Launched	PKC activator	PRKCA|PRKCB|PRKCD|PRKCE|PRKCG	dermatology	actinic keratosis (AK)
INH1	Preclinical	Hec1 inhibitor	NDC80		
inimur	Launched	other antifungal			
iniparib	Phase 3	PARP inhibitor	PARP1		
inosine	Launched	neurotrophic agent	PARP1|PNP		
inositol	Launched	insulin sensitizer	CDIPT	obstetrics/gynecology	polycystic ovary syndrom (PCOS)
inositol-hexanicotinate	Launched			dermatology|cardiology|rheumatology|neurology/psychiatry	statis dermatitis|claudication|Raynaud's disease|hypertension|insomnia|atherosclerosis|restless leg syndrome|schizophrenia|psoriasis|acne vulgaris (AV)
INS316	Phase 2	purinergic receptor antagonist			
INT-747	Phase 3	FXR agonist			
INT-767	Phase 1	FXR agonist	GPBAR1		
integrin-antagonist-1	Phase 1	integrin antagonist	ITGAV|ITGB6		
INX-08189	Phase 2	antiviral			
iobenguane	Launched	antineoplastic agent		oncology|cardiology|endocrinology	neuroblastoma|congestive heart failure|pheochromocytoma
iocetamic-acid	Launched	radiopaque medium		radiology	contrast agent
iodipamide	Launched	radiopaque medium	ALB	radiology	contrast agent
iodixanol	Launched	radiopaque medium		radiology	contrast agent
iodoantipyrine	Preclinical				
iododexetimide	Phase 2	acetylcholine receptor antagonist			
iodophenpropit	Preclinical	histamine receptor antagonist	HRH3|HRH4		
iodoquinol	Launched	antiseptic		infectious disease	amebiasis
iohexol	Launched	radiopaque medium		radiology	contrast agent
iopamidol	Launched	radiopaque medium		radiology	contrast agent
iopanic-acid	Withdrawn	thyroid hormone inhibitor			
iopodic-acid	Launched			radiology	contrast agent
iopromide	Launched	radiopaque medium		radiology	contrast agent
iothalamic-acid-d3	Preclinical	radiopaque medium			
ioversol	Launched	radiopaque medium		radiology	contrast agent
IOWH032	Phase 2	CFTR channel antagonist	CFTR		
ioxaglic-acid	Launched	radiopaque medium		radiology	contrast agent
ioxilan	Launched	radiopaque medium		radiology	angiography
IOX1	Preclinical	histone demethylase inhibitor	EGLN1|KDM3A|KDM4C|KDM6B		
IOX2	Preclinical	hypoxia inducible factor inhibitor	EGLN1|KDM2A|KDM5C		
IPA-3	Preclinical	p21 activated kinase inhibitor	PAK1		
IPAG	Preclinical				
ipidacrine	Phase 3	acetylcholinesterase inhibitor	ACHE		
IPI549	Phase 2	PI3K inhibitor			
ipragliflozin-L-proline	Launched	sodium/glucose cotransporter inhibitor	SLC5A2	endocrinology	diabetes mellitus
ipratropium	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5	pulmonary	bronchospasm|chronic obstructive pulmonary disease (COPD)|bronchitis|emphysema
ipriflavone	Launched	bone resorption inhibitor		orthopedics	osteoporosis
iproniazid	Withdrawn	monoamine oxidase inhibitor	MAOA|MAOB		
ipsapirone	Phase 3	serotonin receptor agonist	HTR1A		
irbesartan	Launched	angiotensin receptor antagonist	AGTR1|JUN|SLC10A1	cardiology|nephrology	hypertension|diabetic nephropathy
irganox-1010	Preclinical	antioxidant			
iRGD-peptide	Preclinical	integrin signaling activator			
irinotecan	Launched	topoisomerase inhibitor	TOP1|TOP1MT	oncology	colorectal cancer
IRL-2500	Preclinical	endothelin receptor antagonist	EDNRB		
irosustat	Phase 2	steroid sulfatase inhibitor	CA2|STS		
irsogladine	Launched	phosphodiesterase inhibitor	PDE4A	gastroenterology	peptic ulcer disease (PUD)
isamoltane	Phase 1	adrenergic receptor antagonist	HTR1A|HTR1B		
isavuconazole	Phase 3	cytochrome P450 inhibitor	CYP3A4		
isaxonine	Withdrawn	nerve growth factor agonist			
isbufylline	Phase 2	phosphodiesterase inhibitor			
isepamicin	Launched	protein synthesis inhibitor		infectious disease	pneumonia|peritonitis
ISO-1	Preclinical	macrophage migration inhibiting factor inhibitor	MIF		
isobutamben	Preclinical	local anesthetic			
isobutyramide	Phase 2	gene expression stimulant	HBE1|HBG1		
isocarboxazid	Launched	monoamine oxidase inhibitor	MAOA|MAOB	neurology/psychiatry	depression
isoconazole	Launched	fungal lanosterol demethylase inhibitor	CYP17A1	infectious disease	gram-positive bacterial infections
isodibut	Phase 2	aldehyde reductase inhibitor			
isoetharine	Launched	adrenergic receptor agonist		pulmonary	bronchospasm|asthma
isofloxythepin	Phase 2	dopamine receptor antagonist			
isoflupredone-acetate	Preclinical		NR3C1		
isoflurane	Launched	inhaled anaesthetic	GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ|GLRA1|GLRB|KCNK10|KCNK18|KCNK2|KCNK3|KCNK9	neurology/psychiatry	general anaesthetic
isoflurophate	Launched	cholinesterase inhibitor	ACHE|BCHE	ophthalmology	glaucoma
isoguvacine	Preclinical	benzodiazepine receptor agonist	GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRR1|GABRR2|GABRR3		
isoleucine	Launched				
isoliquiritigenin	Preclinical	guanylate cyclase activator	GABBR1		
isometheptene-mucate	Launched			neurology/psychiatry	headache
isoniazid	Launched	FABI inhibitor	CYP1A2|CYP2C19|CYP2C8|CYP2E1|CYP3A4	infectious disease	tuberculosis
isopentyl-4-methoxycinnamate	Launched			dermatology	sunscreen lotion
isoprenaline	Launched	adrenergic receptor agonist	ADRB1|ADRB2|ADRB3	cardiology|pulmonary	bradycardia|heart block|asthma
isopropamide-iodide	Launched	acetylcholine receptor antagonist	CHRM3|CHRM4	gastroenterology	peptic ulcer disease (PUD)|gastrointestinal acidosis
isopropyl-myristate	Launched			dermatology	cosmetic
isopropyl-palmitate	Launched	cosmetic moisturizer		dermatology	cosmetic
isoquercitrin	Phase 2/Phase 3	antioxidant			
"Isoquinoline,-6,7-dimethoxy-1-methyl-1,2,3,4-tetrahydro,"	Preclinical				
isosorbide	Launched	nitric oxide stimulant		cardiology	angina pectoris|coronary artery disease (CAD)
isosorbide-dinitrate	Launched	nitric oxide stimulant	GUCY1A2|GUCY1A3|GUCY1B2|GUCY1B3|NPR1	cardiology	angina pectoris|coronary artery disease (CAD)
isosorbide-mononitrate	Launched	nitric oxide stimulant	GUCY1A2|GUCY1A3|GUCY1B2|GUCY1B3	cardiology	angina pectoris|coronary artery disease (CAD)
isosteviol	Phase 2				
isotiquimide	Phase 1				
isotretinoin	Launched	retinoid receptor agonist	RARA|RARB|RARG	dermatology	acne vulgaris (AV)
isovaleramide	Phase 2	alcohol dehydrogenase inhibitor			
isoxepac	Phase 2	anti-inflammatory agent			
isoxicam	Withdrawn	cyclooxygenase inhibitor	PTGS1|PTGS2		
isoxsuprine	Launched	adrenergic receptor agonist	ADRB2	rheumatology|cardiology	Raynaud's disease|arteriosclerosis|Buerger's disease
ispinesib	Phase 2	kinesin inhibitor	KIF11		
isradipine	Launched	calcium channel blocker	CACNA1D|CACNA1F|CACNA2D1	cardiology	hypertension
ISRIB	Preclinical	eukaryotic translation initiation factor inhibitor|PERK inhibitor	EIF2A|EIF2AK3		
istaroxime	Phase 2	ATPase inhibitor	ATP1A1		
istradefylline	Launched	adenosine receptor antagonist	ADORA1|ADORA2A|ADORA2B|ADORA3	neurology/psychiatry	Parkinson's Disease|dyskinesia
ISX-9	Preclinical	neural stem cell inducer	NEUROD1		
itacitinib	Phase 3	JAK inhibitor	JAK1		
ITD-1	Preclinical	TGF beta receptor inhibitor	TGFBR2		
ITE	Preclinical	aryl hydrocarbon receptor agonist	AHR		
ITI214	Phase 1/Phase 2	phosphodiesterase inhibitor	PDE1A		
itopride	Launched	dopamine receptor antagonist	CHRM3|DRD2	gastroenterology|neurology/psychiatry	dyspepsia|gastroparesis|heartburn|nausea|vomiting|anorexia
itraconazole	Launched	cytochrome P450 inhibitor		infectious disease	onychomycosis|histoplasmosis|blastomycosis|aspergillosis
ITX3	Preclinical	GEF inhibitor	TRIO		
ITX5061	Phase 1	SR-BI inhibitor			
IT1t	Preclinical	CC chemokine receptor antagonist	CXCR4		
IU1	Preclinical	ubiquitin C-terminal hydrolase inhibitor	USP14		
ivabradine	Launched	HCN channel blocker|potassium channel blocker|sodium channel blocker	HCN1|HCN3|HCN4	cardiology	angina pectoris
ivacaftor	Launched	CFTR channel potentiator	CFTR	pulmonary	cystic fibrosis
ivermectin	Launched	benzodiazepine receptor agonist	CHRNA7|P2RX7	infectious disease	gastrointestinal roundworms|lungworms|cattle grubs|mites|lice|horn flies
ivosidenib	Launched	isocitrate dehydrogenase inhibitor	IDH1	hematologic malignancy	acute myeloid leukemia (AML)
IWP-L6	Preclinical	porcupine inhibitor	PORCN		
ixabepilone	Launched	microtubule stabilizing agent	TUBB	oncology	breast cancer
ixazomib	Launched	proteasome inhibitor		hematologic malignancy	multiple myeloma
ixazomib-citrate	Launched	proteasome inhibitor		hematologic malignancy	multiple myeloma
JAK3-inhibitor-V	Preclinical	JAK inhibitor	JAK3		
JD-5037	Preclinical	cannabinoid receptor antagonist			
JDTic	Phase 1	opioid receptor antagonist	OPRK1		
JHW-007	Preclinical	dopamine reuptake inhibitor	SLC6A3		
JI-101	Phase 1/Phase 2	kinase inhibitor			
JIB04	Preclinical	histone lysine demethylase inhibitor	KDM4E		
JK-184	Preclinical	hedgehog pathway inhibitor			
JLK-6	Preclinical	gamma secretase inhibitor	PSEN1		
JNJ-10191584	Preclinical	histamine receptor antagonist	HRH4		
JNJ-10397049	Preclinical	orexin receptor antagonist	HCRTR1|HCRTR2		
JNJ-16259685	Preclinical	glutamate receptor antagonist	GRM1		
JNJ-1661010	Preclinical	FAAH inhibitor	FAAH		
JNJ-17203212	Preclinical	TRPV antagonist	TRPV1		
JNJ-26481585	Phase 2	HDAC inhibitor	HDAC1|HDAC10|HDAC11|HDAC2|HDAC3|HDAC4|HDAC5|HDAC6|HDAC7|HDAC8|HDAC9|MDM2		
JNJ-26990990	Phase 2	anticonvulsant			
JNJ-27141491	Preclinical	CC chemokine receptor antagonist	CCR2		
JNJ-37822681	Phase 2	dopamine receptor antagonist	DRD2		
JNJ-38877605	Phase 1	tyrosine kinase inhibitor	MET		
JNJ-38877618	Phase 1	c-Met inhibitor			
JNJ-39758979	Phase 2	histamine receptor antagonist			
JNJ-40411813	Phase 2	glutamate receptor positive allosteric modulator	GRM2		
JNJ-42041935	Preclinical	hypoxia inducible factor prolyl hydroxylase inhibitor	PDK2		
JNJ-42165279	Phase 2	FAAH inhibitor	FAAH		
JNJ-47965567	Preclinical	purinergic receptor antagonist	P2RX7		
JNJ-54175446	Phase 1	purinergic receptor antagonist			
JNJ-63533054	Preclinical	G protein-coupled receptor agonist	GPR139		
JNJ-64619178	Phase 1	protein arginine N-methyltransferase inhibitor			
JNJ-678	Phase 1	RSV fusion inhibitor			
JNJ-7706621	Preclinical	CDK inhibitor	AURKA|AURKB|CDK1|CDK2		
JNJ-7777120	Preclinical	histamine receptor antagonist	HRH4		
josamycin	Launched	bacterial 50S ribosomal subunit inhibitor		pulmonary	bronchitis
JPH203	Preclinical	solute carrier family member inhibitor			
JQ1-(+)	Preclinical	bromodomain inhibitor	BRD4|BRDT		
JTC-801	Phase 2	opioid receptor antagonist	OPRL1		
JTE-013	Preclinical	lysophospholipid receptor antagonist	P2RY10|S1PR2		
JTE-607	Phase 2	cytokine production inhibitor	IL10|IL1B|IL6|TNF		
JTE-907	Phase 1	cannabinoid receptor inverse agonist	CNR2		
JW-55	Preclinical	tankyrase inhibitor	TNKS|TNKS2		
JW-642	Preclinical	monoacylglycerol lipase inhibitor	MGLL		
JW-67	Preclinical	WNT pathway inhibitor	APC|AXIN1|GSK3B		
JW-74	Preclinical	tankyrase inhibitor|WNT signaling inhibitor	TNKS|TNKS2		
JX-401	Preclinical	p38 MAPK inhibitor	MAPK14		
JZL-184	Preclinical	monoacylglucerol lipase inhibitor	MGLL		
JZL-195	Preclinical	FAAH inhibitor|monoacylglycerol lipase inhibitor	FAAH|MGLL		
J147	Phase 1	BDNF inducer			
K-MAP	Phase 2				
K-Ras(G12C)-inhibitor-12	Preclinical	K-Ras inhibitor	KRAS		
K-Ras(G12C)-inhibitor-6	Preclinical	K-Ras inhibitor			
K-strophanthidin	Phase 2	ATPase inhibitor	ATP1A1		
K-247	Phase 1				
K-858	Preclinical	kinesin-like spindle protein inhibitor	KIF11		
kaempferol	Preclinical	bone resorption inhibitor|estrogen-related receptor inverse agonist	AKR1B1|ALOX15B|ALOX5|AR|CYP1B1|GLO1|HSD17B1|UGT3A1		
KAF-156	Preclinical	antimalarial agent			
kainic-acid	Preclinical	kainate receptor agonist	GRIA1|GRIK1|GRIK2|GRIK3|GRIK4|GRIK5		
kakonein	Phase 2	GABA receptor antagonist|serotonin receptor antagonist			
kanamycin	Launched	bacterial 30S ribosomal subunit inhibitor		infectious disease	gram-negative bacterial infections
karenitecin	Phase 3	topoisomerase inhibitor	TOP1		
kartogenin	Preclinical	chondrocyte differentiation stimulator	FLNA		
kasugamycin	Preclinical	bacterial 30S ribosomal subunit inhibitor			
KB-R7943	Preclinical	sodium/calcium exchange inhibitor	SLC8A1|TRPC3|TRPC5|TRPC6		
KB-SRC-4	Preclinical	SRC inhibitor	SRC		
KBG	Phase 2	neprilysin inhibitor	MME		
KD-023	Phase 2	ACAT inhibitor	ACACA|ACACB		
KD025	Phase 2	rho associated kinase inhibitor	ROCK2		
kenpaullone	Preclinical	CDK inhibitor|glycogen synthase kinase inhibitor	CCNB1|CDK1|CDK5|GSK3B		
ketanserin	Launched	serotonin receptor antagonist	ADRA1A|ADRA1B|ADRA1D|DRD1|DRD5|HTR1A|HTR1B|HTR1D|HTR2A|HTR2B|HTR2C|HTR5A|HTR7|SLC18A1|SLC18A2	cardiology	hypertension
ketoconazole	Launched	sterol demethylase inhibitor	KCNA10	dermatology	seborrheic dermatitis
ketohexokinase-inhibitor-1	Preclinical	kinase inhibitor			
ketoprofen	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2|SLC5A8	rheumatology	rheumatoid arthritis|osteoarthritis
ketorolac	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	neurology/psychiatry	pain relief
ketotifen	Launched	histamine receptor agonist|leukotriene receptor antagonist|phosphodiesterase inhibitor	HRH1	neurology/psychiatry	itching
kevetrin	Phase 1	p53 activator			
KF-38789	Preclinical	P selectin inhibitor	SELP		
KG-5	Preclinical	RAF inhibitor	BRAF|FLT3|KIT|PDGFRB		
KH-CB19	Preclinical	CDC inhibitor	CLK1|CLK3|DYRK1A		
khellin	Phase 2	vasodilator			
KHK-IN-1	Preclinical	hexokinase inhibitor	KHK		
KHS-101	Preclinical	neural stem cell inducer	TACC3		
KI-16425	Preclinical	lysophosphatidic acid receptor antagonist	LPAR1|LPAR3		
KI-20227	Preclinical	c-Fms inhibitor	CSF1R|KDR|KIT|PDGFRB		
KI-8751	Preclinical	KIT inhibitor|PDGFR tyrosine kinase receptor inhibitor|VEGFR inhibitor	KDR		
kifunensine	Phase 1	mannosidase inhibitor	MAN1B1|MAN2A1		
kinetin	Launched	cell division inducer		dermatology	sunburn
ki16198	Preclinical	lipoprotein antagonist	LPA		
KL-001	Preclinical	proteasome inhibitor	CRY1|CRY2		
KM-0118	Phase 1	anticancer agent			
KME-4	Preclinical	prostaglandin inhibitor			
KML29	Preclinical	monoacylglucerol lipase inhibitor	MGLL		
KN-62	Preclinical	calcium/calmodulin dependent protein kinase inhibitor|purinergic receptor antagonist	AKT1|CAMK2A|CHEK1|LCK|MAPK1|MAPK11|MAPK12|MAPK14|MAPK8|P2RX7|PRKCA|ROCK1|RPS6KB1|SGK1		
KN-93	Preclinical	calcium/calmodulin dependent protein kinase inhibitor	CAMK2A		
Ko143	Preclinical	BCRP inhibitor	ABCB1|ABCC1		
KP-1212	Phase 2				
KPT-185	Preclinical	exportin antagonist	XPO1		
KPT-276	Preclinical	exportin antagonist	XPO1		
KPT-9274	Phase 1	NAMPT inhibitor			
KR-33494	Preclinical	cell death inhibitor 			
KRCA-0008	Preclinical	ALK inihibitor	ALK		
KRN-633	Preclinical	VEGFR inhibitor	FLT1|FLT4|KDR		
KS-176	Preclinical	BCRP inhibitor	ABCG2		
KT-433	Phase 2	uricosuric agent			
KU-0063794	Preclinical	mTOR inhibitor	MTOR		
KU-55933	Preclinical	ATM kinase inhibitor	ATM|PRKDC		
KU-60019	Preclinical	ATM kinase inhibitor	ATM		
kuromanin	Preclinical	ribosyl cyclase inhibitor	CD38		
KU14R	Preclinical	imidazoline receptor antagonist			
KW-2449	Phase 1	Abl kinase inhibitor|Aurora kinase inhibitor|FLT3 inhibitor	ABL1|AURKA|AURKB|FLT3		
KW-2478	Phase 1/Phase 2	HSP inhibitor			
KW-3902	Phase 3	adenosine receptor antagonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
KX2-391	Phase 3	SRC inhibitor|tubulin polymerization inhibitor	SRC		
kynurenic-acid	Phase 1	glutamate receptor antagonist	GPR35|GRIN1|GRIN2A|GRIN2B		
KY02111	Preclinical	WNT pathway inhibitor	DKK1		
K02288	Preclinical	bone morphogenic protein inhibitor	BMP1		
K145	Preclinical	sphingosine kinase inhibitor	SPHK2		
L-(+)-rhamnose-monohydrate	Preclinical				
L-alanine	Launched		AARS|AARS2|ABAT|AGXT|AGXT2|GPRC6A|GPT|GPT2|KYNU|NFS1|PHYKPL|SLC1A4|SLC36A1|SLC7A8		
L-arginine	Launched	nitric oxide precursor	ARG2|ASL|ASS1|AZIN2|GPRC6A|NOS2|NOS3|SLC7A1|SLC7A3|SLC7A4	cardiology|neurology/psychiatry|urology|obstetrics/gynecology|otolaryngology	congestive heart failure|hypertension|coronary artery disease (CAD)|claudication|senile dementia|erectile dysfunction|infertility|common cold
L-ascorbyl-6-palmitate	Preclinical				
L-asparagine	Phase 3		ASNS|ASRGL1|NARS|NARS2|SLC1A5|SLC38A3		
L-asparagine-N-hydroxy	Preclinical				
L-aspartic-acid	Launched	metallic radical formation stimulant	ACY1|ACY3|ADSS|ADSSL1|ASNS|ASPA|ASPH|ASRGL1|ASS1|CAD|DARS|DARS2|GOT1|GOT2|GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|LYZ|PAICS|RNASE1|SLC1A1|SLC25A12|SLC25A13		
L-citrulline	Launched	nitric oxide stimulant	ASS1|DDAH1|DDAH2|GPRC6A|NOS1|NOS2|NOS3|OTC|PADI1|PADI2|PADI3|PADI4|PADI6	cardiology|urology	hypertension|erectile dysfunction
L-cysteine	Launched		CARS|CARS2|CBS|CDO-1|CDO1|CSAD|CTH|GCLC|GCLM|GOT1|GSS|MGMT|NFS1|SLC19A3	rheumatology	osteoarthritis|rheumatoid arthritis
L-cysteinesulfinic-acid	Preclinical	glutamate receptor agonist	GRM1|GRM5|GSR|HMGCS2|PAPOLA|PRDX2		
L-cystine	Launched		CTNS|SLC3A1|SLC7A11|SLC7A9		
L-ergothioneine	Phase 3	free radical scavenger			
L-glutamic-acid	Launched	glutamate receptor agonist	AADAT|AASS|ABAT|ALDH18A1|ASNS|BCAT1|BCAT2|CCBL2|DNPEP|EARS2|ENPEP|EPRS|FOLH1|FPGS|FTCD|GAD1|GAD2|GATB|GCLC|GCLM|GGCX|GLS|GLS2|GLUD1|GLUD2|GLUL|GMPS|GOT1|GOT2|GPT|GPT2|GRIA1|GRIA2|GRIA3|GRIA4|GRID1|GRID2|GRIK1|GRIK2|GRIK3|GRIK4|GRIK5|GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D|GRIN3A|GRIN3B|GRM1|GRM2|GRM3|GRM4|GRM6|GRM7|GRM8|LGSN|NADSYN1|NAGS|OPLAH|PFAS|PGCP|PSAT1|SLC1A1|SLC1A2|SLC1A3|SLC1A6|SLC1A7|SLC25A18|SLC25A22|SLC7A11|TAT		
L-glutamine	Launched		CTPS1|GLUL|GPRC6A|PPAT	gastroenterology|dental|neurology/psychiatry|rheumatology	diarrhea|mucositis|muscle pain|joint pain|peptic ulcer disease (PUD)|ulcerative colitis|Crohn's disease|anxiety|insomnia
L-hydroxyproline	Launched				
L-kynurenine	Phase 1	aryl hydrocarbon receptor agonist			
L-leucine	Phase 3		BCAT1|BCAT2|LARS|LARS2|LCMT1|LCMT2		
L-lysine	Phase 2	serotonin receptor agonist	GPRC6A|KARS|SLC7A1|SLC7A2|SLC7A3|SLC7A4		
L-methionine	Launched	voltage-gated calcium channel ligand	BHMT|BHMT2|METAP2|MTR|MTRR	pulmonary|allergy|neurology/psychiatry	asthma|allergic rhinitis|depression|Parkinson's Disease|schizophrenia
L-mimosine	Preclinical	dopamine beta hydroxylase inhibitor|eukaryotic translation initiation factor inhibitor	DBH|EIF5A		
L-monomethylarginine	Phase 3	nitric oxide synthase inhibitor	NOS1|NOS2		
L-NAME	Phase 2/Phase 3	nitric oxide synthase inhibitor	NOS3		
L-NIL	Preclinical	nitric oxide synthase inhibitor	NOS1|NOS2|NOS3		
L-phenylisopropyladenosine	Preclinical				
L-proline	Launched	glutamate receptor agonist	EPRS|L3HYPDH|P3H1|P3H2|P3H3|P4HA1|P4HA2|PARS2|PPIA|PPIB|PPIC|PPIF|PPIG|PPIH|PRODH|PROSC|PYCR1|PYCR2|PYCRL|SLC6A14|SLC6A7		
L-quisqualic-acid	Preclinical	glutamate receptor agonist	FOLH1|GRIA2|GRIK1|GRIK2|GRM1|GRM2|GRM3|GRM5|GRM7|GRM8		
L-theanine	Launched	glutamate receptor antagonist			
L-threonine	Phase 2		TARS|TARS2|THNSL1		
L-valine	Phase 2				
L-152804	Preclinical	neuropeptide receptor antagonist	NPY5R		
L-161982	Preclinical	prostanoid receptor antagonist	PTGER4		
L-165041	Preclinical	PPAR receptor agonist	PPARD		
L-168049	Preclinical	glucagon receptor antagonist	GCGR		
L-365260	Phase 2	CCK receptor antagonist	CCKAR|CCKBR|KCNQ1		
L-368899	Phase 1	oxytocin receptor antagonist	AVPR1A|AVPR2|OXTR		
"L-655,708"	Preclinical	GABA receptor inverse agonist	GABRA1|GABRA2|GABRA3|GABRA5|GABRG2		
L-655240	Phase 1	thromboxane receptor antagonist	PTGES		
L-670596	Preclinical	prostanoid receptor antagonist			
L-689560	Preclinical	glutamate receptor antagonist	GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D		
L-690330	Preclinical	inositol monophosphatase inhibitor	IMPA1		
L-693403	Preclinical	sigma receptor agonist|sigma receptor antagonist	DRD2|SIGMAR1		
L-694247	Preclinical	serotonin receptor agonist	HTR1A|HTR1B|HTR1D		
L-701252	Preclinical	glutamate receptor antagonist	GRIN1		
L-701324	Preclinical	glutamate receptor antagonist	GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D		
"L-732,138"	Preclinical	tachykinin antagonist	TACR1|TACR2		
L-733060	Preclinical	tachykinin antagonist	TACR1		
L-741742	Preclinical	dopamine receptor antagonist	DRD3|DRD4|SCN1A|SCN3A		
L-745870	Preclinical	dopamine receptor antagonist	DRD1|DRD2|DRD3|DRD4|HTR1A|HTR2A|HTR6|HTR7		
L-755507	Preclinical	adrenergic receptor agonist	ADRB1|ADRB2|ADRB3		
L-760735	Preclinical	tachykinin antagonist	TACR1		
L-778123	Phase 1	farnesyltransferase inhibitor	FNTA|FNTB|PGGT1B		
L-798106	Preclinical	prostanoid receptor antagonist	PTGER3		
L-838417	Preclinical	GABA receptor partial agonist	GABRA1|GABRA2|GABRA3|GABRA5		
labetalol	Launched	adrenergic receptor antagonist	ADRA1D|ADRB1|ADRB2	cardiology	hypertension
lacidipine	Launched	calcium channel blocker	CACNA1C	cardiology	hypertension
lacitol	Launched	laxative		gastroenterology	constipation
lactulose	Launched	laxative		gastroenterology	portal-systemic encephalopathy (PSE)
lafutidine	Launched	histamine receptor antagonist	HRH2	gastroenterology	duodenal ulcer disease|peptic ulcer disease (PUD)
lamivudine	Launched	nucleoside reverse transcriptase inhibitor		infectious disease	human immunodeficiency virus (HIV-1)|acquired immunodeficiency syndrome (AIDS)|hepatitis B
lamotrigine	Launched	serotonin receptor antagonist|sodium channel blocker	SCN10A|SCN11A|SCN1A|SCN2A|SCN3A|SCN4A|SCN5A|SCN7A|SCN8A|SCN9A	neurology/psychiatry	epilepsy|bipolar disorder
lanabecestat	Phase 3	beta secretase inhibitor			
lanatoside-C	Preclinical	cardiac glycoside			
landiolol	Launched	adrenergic receptor antagonist	ADRB1	cardiology	cardiac arrythmia
lanifibranor	Phase 2	PPAR receptor agonist			
lanoconazole	Launched	sterol demethylase inhibitor		infectious disease	fungal infection
lansoprazole	Launched	ATPase inhibitor	ATP4A|ATP4B	gastroenterology	heartburn
lapatinib	Launched	EGFR inhibitor	EGFR|ERBB2	oncology	breast cancer
lappaconite	Phase 2	sodium channel blocker			
laquinimod	Phase 3	immunosuppressant	CXCL2		
larazotide-acetate	Phase 2	tight junction regulator			
laropiprant	Launched	prostanoid receptor antagonist	PTGDR|PTGDR2|PTGER1|PTGER2|PTGER3|PTGFR|PTGIR|TBXA2R	cardiology	cholesterol
larotrectinib	Launched	tropomyosin receptor kinase inhibitor	NTRK1|NTRK2|NTRK3		
lasalocid	Launched	bacterial permeability inducer		infectious disease	coccidiosis
lasmiditan	Launched	serotonin receptor agonist			
lasofoxifene	Launched	selective estrogen receptor modulator (SERM)	ESR1|ESR2	orthopedics|oncology	osteoporosis|breast cancer
latanoprost	Launched	prostanoid receptor agonist	PTGFR	ophthalmology	ocular hypertension|glaucoma
latrepirdine	Phase 3	glutamate receptor antagonist	HRH1|HTR6		
latrunculin-B	Phase 1	actin polymerization inhibitor	ACTA1|MKL1|SPIRE2		
lauric-acid	Phase 3	bacterial permeability inducer	GPR84|HNF4A|LTF|LY96|PLA2G2A|TLR4		
lauric-diethanolamide	Preclinical				
laurocapram	Phase 3				
lazabemide	Phase 3	monoamine oxidase inhibitor	MAOB		
lazertinib	Phase 1/Phase 2	tyrosine kinase inhibitor			
LB-100	Phase 2	protein phosphatase inhibitor			
LB42708	Preclinical	farnesyltransferase inhibitor			
LCL-161	Phase 2	XIAP inhibitor	BIRC2|XIAP		
LCQ908	Phase 3	diacylglycerol O acyltransferase inhibitor	DGAT1		
LCZ696	Launched	angiotensin receptor antagonist		cardiology	angioedema|hypotension
LDC1267	Preclinical	protein tyrosine kinase inhibitor	AXL|MERTK|TYRO3		
LDN-209929	Preclinical	haspin kinase inhibitor	GSG2		
LDN-212854	Preclinical	bone morphogenic protein inhibitor	ABL1|ACVR1|RIPK2		
LDN-27219	Preclinical	tissue transglutaminase inhibitor	TGM2		
LDN-57444	Preclinical	ubiquitin C-terminal hydrolase inhibitor			
LDN193189	Preclinical	bone morphogenic protein inhibitor	ACVR1|BMPR1A		
LE-135	Preclinical	retinoid receptor agonist	RARB		
ledipasvir	Launched	HCV inhibitor		infectious disease	hepatitis C
leflunomide	Launched	dihydroorotate dehydrogenase inhibitor|PDGFR tyrosine kinase receptor inhibitor	AHR|DHODH|PTK2B	rheumatology	rheumatoid arthritis
lemborexant	Launched	orexin receptor antagonist	HCRTR1|HCRTR2		
lenalidomide	Launched	anticancer agent	TNF	hematologic malignancy	multiple myeloma|mantle cell lymphoma (MCL)|myelodysplastic diseases (MDS)
leniolisib	Phase 2/Phase 3	PI3K inhibitor			
lenvatinib	Launched	FGFR inhibitor|KIT inhibitor|PDGFR tyrosine kinase receptor inhibitor|VEGFR inhibitor	FLT4|KDR	oncology	thyroid cancer
leonurine	Preclinical	anti-inflammatory agent			
LEQ506	Phase 1	G protein signaling inhibitor			
lercanidipine	Launched	calcium channel blocker	CACNA2D1	cardiology	hypertension
lerisetron	Phase 3	serotonin receptor antagonist	HTR3A		
lersivirine	Phase 2	non-nucleoside reverse transcriptase inhibitor			
lesinurad	Launched	uric acid diuretic	SLC22A12	rheumatology	gout
lestaurtinib	Phase 3	FLT3 inhibitor|growth factor receptor inhibitor|JAK inhibitor	FLT3|NTRK1		
leteprinim	Phase 2	nerve growth factor agonist			
letermovir	Launched	CMV terminase inhibitor		infectious disease	cytomegalovirus (CMV)
letosteine	Launched	mucolytic agent		pulmonary|infectious disease	bronchitis|pneumonia
letrazuril	Phase 1	antiinfective drug			
letrozole	Launched	aromatase inhibitor	CYP19A1	oncology	breast cancer
leucomethylene-blue	Phase 3	nitric oxide production inhibitor|tau aggregation inhibitor	MAPT		
leucovorin	Launched	folate receptor ligand		oncology	osteosarcoma
leucylleucine-methyl-ester	Phase 2				
leuprolide	Launched	gonadotropin releasing factor hormone receptor agonist	GNRHR	oncology	prostate cancer
levalbuterol	Launched	adrenergic receptor agonist	ADRB2	pulmonary	bronchospasm
levallorphan	Launched	opioid receptor antagonist	CHRNA2|OPRM1	pulmonary	respiratory depression
levamisole	Withdrawn	acetylcholine receptor agonist	ALPL		
levamlodipine	Launched	calcium channel blocker		cardiology	hypertension
levcromakalim	Phase 3	potassium channel activator	KCNJ5		
levetiracetam	Launched	calcium channel blocker	CACNA1B|SCN1A|SV2A	neurology/psychiatry	seizures
levo-phencynonate	Launched	acetylcholine receptor antagonist	CHRM1		
levobetaxolol	Launched	adrenergic receptor antagonist	ADRB1|ADRB2	ophthalmology	intraocular pressure|glaucoma
levobunolol	Launched	adrenergic receptor antagonist	ADRB1|ADRB2|ADRB3	ophthalmology	glaucoma|ocular hypertension
levobunolol-(+)	Preclinical	adrenergic receptor antagonist			
levobunolol-(+/-)	Preclinical	adrenergic receptor antagonist			
levocabastine	Launched	histamine receptor antagonist	HRH1|NTSR2	ophthalmology	conjunctivitis
levocarnitine	Launched		CRAT|CROT	endocrinology	carnitine deficiency
levocarnitine-propionate	Launched	carnitine palmitoyltransferase inhibitor	CRAT	neurology/psychiatry|endocrinology	peripheral neuropathy|carnitine deficiency
levocetirizine	Launched	histamine receptor antagonist	HRH1	allergy	allergic rhinitis|urticaria
levodopa	Launched	dopamine precursor	DRD1|DRD2|DRD3|DRD4|DRD5|GPR143	neurology/psychiatry	Parkinson's Disease
levodropropizine	Launched	antitussive		pulmonary	cough suppressant
levofloxacin	Launched	bacterial DNA gyrase inhibitor	TOP2A	infectious disease|otolaryngology|pulmonary|urology	pneumonia|sinusitis|bronchitis|skin infections|prostatitis|urinary tract infections|pyelonephritis|anthrax|plague
levomenol	Launched			neurology/psychiatry|infectious disease	spasms|skin infections
levomenthol	Launched		OPRK1|TRPA1|TRPM8|TRPV3	neurology/psychiatry	pain relief
levomepromazine	Launched	dopamine receptor antagonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|DRD1|DRD2|DRD3|DRD4|DRD5|HRH1|HTR2A|HTR2C	neurology/psychiatry|gastroenterology	psychosis|schizophrenia|bipolar disorder|nausea|insomnia
levomequitazine	Phase 2	histamine receptor antagonist	HRH1		
levonordefrin	Launched	vasodilator	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|SLC6A2	hematology	hemorrhage
levonorgestrel	Launched	estrogen receptor agonist|glucocorticoid receptor antagonist|progesterone receptor agonist|progesterone receptor antagonist	PGR	endocrinology	contraceptive
levopropoxyphene	Launched	antitussive		pulmonary	cough suppressant
levosimendan	Launched	calcium sensitizer	KCNJ11|KCNJ8|PDE3A|TNNC1	cardiology	congestive heart failure
levosulpiride	Launched	dopamine receptor antagonist	CA1|CA12|CA7|DRD2|DRD3	neurology/psychiatry|gastroenterology|urology	schizophrenia|psychosis|anxiety|vertigo|dyspepsia|irritable bowel syndrome|premature ejaculation (PE)
levothyroxine	Launched	thyroid hormone stimulant	THRA|THRB	endocrinology	myxedema coma
LFM-A13	Preclinical	Bruton's tyrosine kinase (BTK) inhibitor	BTK		
LGD-6972	Phase 2	glucagon receptor antagonist			
LGK-974	Phase 2	porcupine inhibitor	PORCN		
LH846	Preclinical	casein kinase inhibitor	CSNK1D		
liarozole	Phase 2/Phase 3	cytochrome P450 inhibitor	CYP19A1|CYP26A1		
licarbazepine	Phase 3	voltage-gated sodium channel blocker	SCN5A		
licochalcone-A	Phase 3	topoisomerase inhibitor	PTPN1		
licofelone	Phase 3	cyclooxygenase inhibitor|lipoxygenase inhibitor	ALOX5|PLA2G2E|PTGS2		
licogliflozin	Preclinical	sodium/glucose cotransporter inhibitor			
licostinel	Phase 1	NMDA receptor antagonist 			
lidamidine	Launched	adrenergic receptor agonist		gastroenterology	diarrhea
lidocaine	Launched	histamine receptor agonist	EGFR|SCN10A|SCN5A|SCN9A	neurology/psychiatry|dermatology|hematology	itching|eczema|hemorrhage
lidoflazine	Launched	calcium channel blocker	SCN1A|SCN3A|SLC29A1	cardiology	coronary artery disease (CAD)
lifirafenib	Phase 1/Phase 2	RAF inhibitor			
lifitegrast	Launched	lymphocyte function-associated antigen negative modulator		ophthalmology	dry eye syndrome
ligustilide	Preclinical	tumor necrosis factor production inhibitor	TNF		
limaprost-alfadex	Launched	prostanoid receptor agonist	PTGER1	cardiology	claudication
LIMKi-3	Preclinical	LIM kinase inhibitor	LIMK1		
limonin	Preclinical	HIV protease inhibitor			
linaclotide	Launched	guanylate cyclase activator	GUCY2C	gastroenterology	irritable bowel syndrome|constipation
linagliptin	Launched	dipeptidyl peptidase inhibitor	DPP4	endocrinology	diabetes mellitus
linalool	Phase 1	anticonvulsant			
linaprazan	Preclinical	ATP-sensitive potassium channel inhibitor			
lincomycin	Launched	bacterial 30S ribosomal subunit inhibitor		gastroenterology	enteritis
lindane	Launched		GABRB1|GLRA1|GLRA2|GLRA3|GLRB	infectious disease	scabies
linezolid	Launched	bacterial 50S ribosomal subunit inhibitor	MAOA|MAOB	infectious disease	pneumonia|skin infections
linifanib	Phase 3	PDGFR tyrosine kinase receptor inhibitor|VEGFR inhibitor	CSF1|CSF1R|FLT1|FLT3|FLT4|KDR|KIT|PDGFRB|RET|TEK		
linoleic-acid	Phase 3	oxidative stress inducer	FABP4|FFAR1|FFAR4|HNF4A|KCNB1|PPARG|TRPM8		
linopirdine	Phase 3	potassium channel blocker	KCNQ2|KCNQ3|KCNQ4|KCNQ5		
linsidomine	Launched	nitric oxide donor		urology	erectile dysfunction
linsitinib	Phase 3	IGF-1 inhibitor	IGF1R|INSR|INSRR		
lintopride	Preclinical	serotonin receptor antagonist			
liothyronine	Launched	thyroid hormone stimulant	THRA|THRB	endocrinology	hypothyroidism|myxedema coma
liothyronine-(isomer)	Preclinical				
lipoamide	Preclinical				
liquiritin	Preclinical	antioxidant			
liraglutide	Launched	GLP receptor agonist	GLP1R	endocrinology	weight-loss aid|diabetes mellitus
liranaftate	Launched	fungal squalene epoxidase inhibitor		infectious disease	fungal infection
lirimilast	Phase 2	phosphodiesterase inhibitor			
lisadimate	Launched	topical sunscreen agent		dermatology	sunscreen lotion
lisinopril	Launched	angiotensin converting enzyme inhibitor	ACE|ACE2	cardiology|endocrinology	hypertension|congestive heart failure|diabetes mellitus
lisofylline	Phase 2	interleukin receptor antagonist|STAT inhibitor			
lisuride	Launched	dopamine receptor agonist	ADRA1A|ADRA2A|ADRA2B|ADRA2C|DRD1|DRD2|DRD3|DRD4|DRD5|HTR1A|HTR1B|HTR1D|HTR2A|HTR2B|HTR2C|HTR6	neurology/psychiatry	Parkinson's Disease
lithium-acetoacetate	Preclinical		FAH		
lithium-citrate	Launched			neurology/psychiatry	bipolar disorder|depression
lithocholic-acid	Preclinical	FXR antagonist|vitamin D receptor agonist	GPBAR1|NR1H4|NR1I2|VDR		
litronesib	Phase 2	kinesin-like spindle protein inhibitor	KIF11		
lixivaptan	Phase 3	vasopressin receptor antagonist	AVPR2		
LM-22A4	Preclinical	tropomyosin receptor kinase inhibitor	NTRK2		
LMI070	Phase 1/Phase 2	survival motor neuron protein modulator	SMN1		
LMK-235	Preclinical	HDAC inhibitor	HDAC4|HDAC5		
LM11A-31	Phase 1	neurotrophic agent	NGFR		
lobeline	Launched	acetylcholine receptor antagonist	CHRNA10|CHRNA9|SLC18A2	neurology/psychiatry	smoking cessation
lobendazole	Preclinical	anthelmintic agent			
lobenzarit	Launched	immunosuppressant		rheumatology	rheumatoid arthritis
lodenosine	Phase 2	antiretroviral 			
lodoxamide	Launched	histamine receptor antagonist		ophthalmology	vernal keratoconjunctivitis (VKC)
lofemizole	Phase 3	cyclooxygenase inhibitor			
lofepramine	Launched	norepinephrine reuptake inhibitor|serotonin–norepinephrine reuptake inhibitor (SNRI)	HTR1A|SLC6A2|SLC6A4	neurology/psychiatry	depression
lofexidine	Launched	adrenergic receptor agonist		neurology/psychiatry	opioid withdrawal
lomefloxacin	Launched	bacterial DNA gyrase inhibitor		infectious disease	respiratory tract infections|urinary tract infections
lomeguatrib	Phase 2	O6-alkylguanine-DNA alkyltransferase inhibitor	MGMT		
lomerizine	Launched	calcium channel blocker	CACNA1B|SCN5A	neurology/psychiatry	migraine headache
lometrexol	Phase 2	glycinamide ribonucleotide formyltransferase inhibitor	GART		
lomitapide	Launched	microsomal trigylceride transfer protein inhibitor	MTTP	endocrinology	hypercholesterolemia
lomustine	Launched	DNA synthesis inhibitor		hematologic malignancy|oncology	Hodgkin's lymphoma|brain tumors
lonafarnib	Phase 3	farnesyltransferase inhibitor	FNTA|HRAS|KRAS|NRAS		
lonidamine	Launched	glucokinase inhibitor	GCK		
loperamide	Launched	opioid receptor agonist	CACNA1A|CALM1|OPRD1|OPRK1|OPRM1|POMC	gastroenterology	diarrhea
lopinavir	Launched	HIV protease inhibitor		infectious disease	human immunodeficiency virus (HIV-1)
loracarbef	Launched	bacterial cell wall synthesis inhibitor		infectious disease|otolaryngology|pulmonary	ear infections|laryngitis|bronchitis|pneumonia|urinary tract infections|skin infections
loratadine	Launched	histamine receptor antagonist	HRH1	allergy|neurology/psychiatry	allergic rhinitis|itching
loreclezole	Phase 2	benzodiazepine receptor agonist	GABRB2|GABRB3		
lorediplon	Phase 2	GABA receptor modulator	GABRA1		
lorglumide	Phase 1	CCK receptor antagonist	CCKAR|CCKBR		
lorlatinib	Launched	ALK tyrosine kinase receptor inhibitor	ALK	oncology	non-small cell lung cancer (NSCLC)
lornoxicam	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	rheumatology|neurology/psychiatry	osteoarthritis|sciata
losartan	Launched	angiotensin receptor antagonist	AGTR1	cardiology|nephrology	hypertension|diabetic nephropathy|hypertension
losmapimod	Phase 3	p38 MAPK inhibitor	MAPK14		
lotamilast	Preclinical	phosphodiesterase inhibitor			
loteprednol	Launched	glucocorticoid receptor agonist|phospholipase inhibitor	NR3C1	ophthalmology	conjunctivitis
lovastatin	Launched	HMGCR inhibitor	HDAC2|HMGCR|ITGAL|NR1I2	cardiology|endocrinology	coronary heart disease|myocardial infarction|hypercholesterolemia
loxapine	Launched	dopamine receptor antagonist|serotonin receptor antagonist	ADRA1A|ADRA1B|ADRA2A|ADRA2B|ADRA2C|ADRB1|CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|DRD1|DRD2|DRD3|DRD4|DRD5|HRH1|HRH2|HRH4|HTR1A|HTR1B|HTR1D|HTR1E|HTR2A|HTR2C|HTR3A|HTR5A|HTR6|HTR7|SLC6A2|SLC6A3|SLC6A4	neurology/psychiatry	schizophrenia
loxistatin-acid	Preclinical	cysteine peptidase inhibitor	CTSB		
loxoprofen	Launched	cyclooxygenase inhibitor|prostanoid receptor antagonist	PTGS2	neurology/psychiatry	pain relief
LP-533401	Preclinical	tryptophan hydroxylase inhibitor			
LPA2-antagonist-1	Preclinical	lysophosphatidic acid receptor antagonist	LPAR2		
LRRK2-IN-1	Preclinical	leucine rich repeat kinase inhibitor	LRRK2		
LSN-2463359	Preclinical	glutamate receptor positive allosteric modulator	GRM5		
LSZ-102	Phase 1	selective estrogen receptor modulator (SERM)			
LTA	Phase 2				
LTB4	Phase 2	leukocyte activator	LTB4R|LTB4R2		
LTX-315	Phase 2	anticancer agent			
Lu-AA-47070	Phase 2	adenosine receptor antagonist	ADORA2A		
lubiprostone	Launched	chloride channel activator	CLCN2	gastroenterology	constipation|irritable bowel syndrome
lucanthone	Phase 2	endonuclease inhibitor	APEX1|TOP1|TOP2A		
lucitanib	Phase 2	FGFR inhibitor|VEGFR inhibitor	FGFR1|FLT1|KDR|KIT|PDGFRA|PDGFRB|RET		
LUF-5834	Preclinical	adenosine receptor agonist	ADORA2A|ADORA2B		
lufenuron	Launched	chitin inhibitor		infectious disease	flea control
luliconazole	Launched	sterol demethylase inhibitor		infectious disease	tinea pedis|tinea cruris|tinea corporis
lumacaftor	Launched	CFTR channel agonist	CFTR	pulmonary	cystic fibrosis
lumateperone	Launched	dopamine receptor modulator|serotonin receptor antagonist	DRD2|HTR2A		
lumefantrine	Launched	antimalarial agent	ATP1A1	infectious disease	malaria
lumiracoxib	Withdrawn	cyclooxygenase inhibitor	PTGS1|PTGS2		
lupanine	Phase 1	sodium channel blocker	INS		
lurasidone	Launched	dopamine receptor antagonist|serotonin receptor antagonist	ADRA2A|ADRA2C|DRD2|HTR1A|HTR2A|HTR7	neurology/psychiatry	schizophrenia
lurbinectedin	Phase 3	DNA binding agent			
lusaperidone	Preclinical	adrenergic receptor antagonist			
lusutrombopag	Launched	thrombopoietin receptor agonist			
lutein	Launched	antioxidant		ophthalmology	macular degeneration|cataracts|retinitis pigmentosa (RP)
luteolin	Phase 2	glucosidase inhibitor	TOP1		
luzindole	Preclinical	melatonin receptor antagonist	MTNR1A|MTNR1B		
LXH254	Phase 1	RAF inhibitor			
LXR-623	Phase 1	LXR agonist	AR|NR1H2|NR1H3|NR1I2|NR3C1		
LXS196	Phase 1	PKC inhibitor			
LX1031	Phase 2	tryptophan hydroxylase inhibitor	TPH1		
LX7101	Phase 1/Phase 2	LIM kinase inhibitor|rho associated kinase inhibitor	LIMK2|ROCK1|ROCK2		
lycopene	Launched	free radical scavenger			
lylamine	Preclinical	cannabinoid receptor agonist	CNR1		
lymecycline	Launched	bacterial 50S ribosomal subunit inhibitor		dermatology	acne vulgaris (AV)
lynestrenol	Launched	progestogen hormone		endocrinology	contraceptive
lypressin	Launched	vasopressin receptor agonist	AVPR1A|AVPR1B|AVPR2	endocrinology	central diabetes insipidus
LY2090314	Phase 2	glycogen synthase kinase inhibitor	GSK3B		
LY2109761	Preclinical	TGF beta receptor inhibitor	TGFBR1|TGFBR2		
LY2140023	Phase 3	glutamate receptor agonist	GRM3		
LY215490	Phase 1	glutamate receptor antagonist	GRIA1|GRIA2|GRIA3|GRIA4|GRIK1		
LY2157299	Phase 2/Phase 3	TGF beta receptor inhibitor	TGFBR1		
LY2183240	Preclinical	FAAH inhibitor|FAAH reuptake inhibitor	FAAH		
LY2228820	Phase 2	p38 MAPK inhibitor	MAPK14		
LY223982	Phase 2	leukotriene receptor antagonist	LTB4R		
LY225910	Preclinical	CCK receptor antagonist	CCKBR		
LY231617	Preclinical	lipid peroxidase inhibitor			
LY2334737	Phase 1	antitumor agent|ribonucleotide reductase inhibitor			
LY2365109	Preclinical	glycine transporter inhibitor	SLC6A9		
LY2452473	Phase 2	androgen receptor modulator	AR		
LY2510924	Phase 2	CC chemokine receptor antagonist			
LY255283	Preclinical	leukotriene receptor antagonist	LTB4R|LTB4R2		
LY2584702	Phase 1	ribosomal protein inhibitor	RPS6KB1		
LY2603618	Phase 2	CHK inhibitor	CHEK1		
LY2606368	Phase 2	CHK inhibitor	CHEK1		
LY2608204	Phase 2	glucokinase activator	GCK		
LY266097	Preclinical	serotonin receptor antagonist	HTR2B		
LY2784544	Phase 2	JAK inhibitor	JAK2|JAK3		
LY2795050	Preclinical	opioid receptor antagonist			
LY2801653	Phase 2	MET inhibitor	MET		
LY2811376	Phase 1	beta-secretase inhibitor	BACE1		
LY2828360	Phase 2	cannabinoid receptor agonist			
LY2857785	Preclinical	CDK inhibitor	CDK9		
LY2874455	Phase 1	FGFR antagonist	FGFR1|FGFR2|FGFR3|FGFR4|KDR		
LY288513	Preclinical	CCK receptor antagonist	CCKBR		
LY2886721	Phase 1/Phase 2	beta-secretase inhibitor	BACE1		
LY294002	Preclinical	DNA dependent protein kinase inhibitor|mTOR inhibitor|phosphodiesterase inhibitor|PI3K inhibitor|PLK inhibitor	AKT1|CHEK1|GSK3B|LCK|MAPK1|MAPK11|MAPK12|MAPK14|MAPK8|MTOR|PIK3CA|PIK3CB|PIK3CD|PIK3CG|PIM1|PLK1|PRKCA|PRKDC|ROCK1|RPS6KB1|SGK1		
LY2979165	Phase 1	glutamate receptor agonist	GRM2		
LY3000328	Phase 1	cathepsin inhibitor	CTSS		
LY3009120	Phase 1	RAF inhibitor	BRAF|RAF1		
LY3023414	Phase 2	mTOR inhibitor|PI3K inhibitor	MTOR		
LY303511	Preclinical	casein kinase inhibitor|mTOR inhibitor|PI3K inhibitor	BRD2|BRD3|BRD4		
LY310762	Preclinical	serotonin receptor antagonist	HTR1D		
LY311727	Preclinical	phospholipase inhibitor			
LY3200882	Phase 1	TGF beta receptor inhibitor			
LY320135	Preclinical	cannabinoid receptor antagonist	CNR1		
LY3214996	Phase 1	ERK inhibitor			
LY3295668	Phase 1/Phase 2	Aurora kinase inhibitor			
LY334370	Preclinical	serotonin receptor agonist			
LY344864	Preclinical	serotonin receptor agonist	HTR1A|HTR1B|HTR1D|HTR1E|HTR1F|HTR2A|HTR2B|HTR2C|HTR7		
LY364947	Preclinical	p38 MAPK inhibitor|TGF beta receptor inhibitor	TGFBR1		
LY393558	Preclinical	serotonin receptor antagonist	HTR1B|HTR1D|HTR2A|HTR2B		
LY404187	Preclinical	glutamate receptor positive allosteric modulator	GRIA1|GRIA2|GRIA3|GRIA4		
LY411575	Preclinical	gamma secretase inhibitor			
LY450108	Phase 1	glutamate receptor modulator			
LY456236	Preclinical	glutamate receptor antagonist	GRM1		
m-chlorophenylbiguanide	Preclinical	serotonin receptor agonist	HTR3A|HTR3B		
m-THP	Phase 1				
M-14157	Phase 2	ATP-sensitive potassium channel antagonist	KCNQ1		
M-25	Preclinical	smoothened receptor antagonist	DHH|IHH|SMO		
m-3M3FBS	Preclinical	phospholipase activator	PLCB2|PLCB3|PLCD1|PLCG1|PLCG2		
M-344	Preclinical	HDAC inhibitor	HDAC8		
mabuprofen	Launched	cyclooxygenase inhibitor		neurology/psychiatry	pain relief
mabuterol	Launched	adrenergic receptor agonist	ADRB2	pulmonary	asthma
macelignan	Preclinical	anti-inflammatory agent|antioxidant			
macitentan	Launched	endothelin receptor antagonist	EDNRA|EDNRB	endocrinology	contraceptive
macitentan-n-butyl-analogue	Preclinical	endothelin receptor antagonist			
macozinone	Preclinical	DPRE1 inhibitor			
madecassoside	Preclinical	anti-inflammatory agent			
madrasin	Preclinical	cell splicing inhibitor			
mafenide	Launched	carbonic anhydrase inhibitor	CA12|CA14|CA2|CA4|CA6|CA9	infectious disease	first-aid antibiotic|skin infections
magnolol	Preclinical	PPAR receptor agonist	GABRA1|PPARG		
malathion	Launched	cholinesterase inhibitor	ACHE	infectious disease	lice
malic-acid	Launched		PKD2L1		
malotilate	Launched	protein synthesis stimulant		gastroenterology	hepatic cirrhosis
maltobionic-acid	Launched	matrix metalloprotease inhibitor		dermatology	cosmetic
mandelic-acid	Launched				
mangafodipir	Launched	contrast agent		radiology	contrast agent
manidipine	Launched	calcium channel blocker	CACNA1C|CACNA1D	cardiology	hypertension
manitimus	Preclinical	dehydrogenase inhibitor			
mannitol-D	Launched	diuretic		neurology/psychiatry|ophthalmology|gastroenterology	intracranial pressure|intraocular pressure|constipation
maprotiline	Launched	norepinephrine reputake inhibitor|tricyclic antidepressant	SLC6A2	neurology/psychiatry	depression|dysthymic disorder
maraviroc	Launched	CC chemokine receptor antagonist	CCR5	infectious disease	human immunodeficiency virus (HIV-1)
marbofloxacin	Launched	bacterial DNA gyrase inhibitor		infectious disease	gram-negative bacterial infections
maribavir	Phase 3	cytomegalovirus inhibitor|protein kinase inhibitor	PYGM		
marimastat	Phase 3	matrix metalloprotease inhibitor	MMP1|MMP10|MMP11|MMP12|MMP13|MMP14|MMP15|MMP16|MMP17|MMP19|MMP2|MMP20|MMP21|MMP23A|MMP24|MMP25|MMP26|MMP27|MMP28|MMP3|MMP7|MMP8|MMP9		
maropitant	Launched	neurokinin receptor antagonist	TACR1	gastroenterology	vomiting
masitinib	Launched	KIT inhibitor|PDGFR tyrosine kinase receptor inhibitor|SRC inhibitor	FGFR3|KIT|PDGFRA|PDGFRB	dermatology	mastocytoma
masoprocol	Launched	lipoxygenase inhibitor	ALOX5	dermatology	actinic keratosis (AK)
matrine	Phase 2	opioid receptor agonist	OPRK1		
mavacamten	Phase 3	myosin inhibitor 			
mavatrep	Preclinical	transient receptor potential channel antagonist			
mavoglurant	Phase 2	glutamate receptor antagonist	GRM5		
maxacalcitol	Launched	vitamin D receptor agonist	VDR	endocrinology	hyperparathyroidism
maytansinol-isobutyrate	Preclinical				
MBX-2982	Phase 2	glucose dependent insulinotropic receptor agonist	GPR119		
MC-1	Phase 3		AADAT|ABAT|AGXT|AGXT2|ALAS1|AZIN2|BCAT1|BCAT2|CBS|CCBL1|CCBL2|CSAD|CTH|DDC|FTCD|GAD1|GAD2|GADL1|GCAT|GLDC|GOT1|GOT2|GPT|GPT2|HDC|IGSF10|KYNU|MOCOS|NFS1|OAT|ODC1|PDXDC1|PDXP|PHYKPL|PNPO|PROSC|PSAT1|PYGB|PYGL|PYGM|SCLY|SDS|SDSL|SEPSECS|SGPL1|SHMT1|SHMT2|SPTLC1|SPTLC2|SPTLC3|SRR|TAT|THNSL1		
MCC950	Preclinical	NOD like receptor inhibitor	NLRP3		
McN-5652-(+/-)	Preclinical	selective serotonin reuptake inhibitor (SSRI)			
MCOPPB	Preclinical	nociceptin/orphanin FQ receptor agonist	OPRL1		
mCPP	Phase 2	serotonin receptor agonist	HTR1A|HTR1D|HTR1E|HTR2A|HTR2B|HTR2C|HTR6		
MC1568	Preclinical	HDAC inhibitor	HDAC2		
MD-920	Phase 1	NFkB pathway inhibitor	AADACL2		
mdivi-1	Preclinical	dynamin inhibitor	DNM1		
MDL-11939	Phase 2	serotonin receptor antagonist	HTR2A|HTR2B|HTR2C		
MDL-27531	Preclinical	glycine receptor agonist			
MDL-29951	Preclinical	glutamate receptor antagonist	FBP1		
MDL-72832	Preclinical	serotonin receptor agonist	HTR1A		
MDL-73005EF	Phase 1	serotonin receptor antagonist	HTR1A		
MDMS	Phase 2	DNA inhibitor			
ME-0328	Preclinical	PPAR receptor antagonist	PARP3		
mebendazole	Launched	tubulin polymerization inhibitor	TUBA1A|TUBB|TUBB4B	infectious disease	pinworm|whipworm|hookworm|ascariasis
mebeverine	Launched	acetylcholine receptor antagonist	CHRM1	gastroenterology	irritable bowel syndrome
mebhydrolin	Launched	antihistamine		allergy	allergic rhinitis|urticaria
mebicar	Launched	anxiolytic		neurology/psychiatry	anxiety
mebrofenin	Launched			radiology	diagnostic agent
mecamylamine	Launched	acetylcholine receptor antagonist	CHRNA1|CHRNA2|CHRNA3|CHRNA4|CHRNA6|CHRNA7|CHRNB4	cardiology	hypertension
mecarbinate	Preclinical				
meclinertant	Phase 2/Phase 3	neurotensin receptor antagonist	NTSR1|NTSR2		
meclizine	Launched	constitutive androstane receptor (CAR) agonist	NR1I3	gastroenterology|neurology/psychiatry	nausea|vomiting|motion sickness
meclocycline-sulfosalicylate	Launched	bacterial 50S ribosomal subunit inhibitor		dermatology|infectious disease	acne vulgaris (AV)|skin infections
meclofenamic-acid	Launched	cyclooxygenase inhibitor|prostanoid receptor antagonist	ALOX5|CNR1|KCNQ2|KCNQ3|PTGS1|PTGS2	rheumatology|neurology/psychiatry|endocrinology	joint pain|muscle pain|rheumatoid arthritis|primary dysmenorrhea (PD)
meclofenoxate	Launched	nootropic agent		neurology/psychiatry	senile dementia|Alzheimer's disease
mecysteine	Launched	analgesic agent		pulmonary	chest congestion
medetomidine	Launched	adrenergic receptor agonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C	neurology/psychiatry	sedative
medica-16	Phase 2	ATP citrase lyase inhibitor	FFAR1		
medorinone	Phase 1				
medronic-acid	Launched	bone resorption inhibitor		radiology	skeletal imaging agent
medroxyprogesterone	Launched	progesterone receptor agonist	PGR	endocrinology	contraceptive
medroxyprogesterone-acetate	Launched	progesterone receptor agonist	ESR1|PGR	endocrinology	contraceptive
medrysone	Launched	glucocorticoid receptor agonist	NR3C1	ophthalmology	conjunctivitis|episcleritis
mefenamic-acid	Launched	cyclooxygenase inhibitor	KCNQ1|PTGS1|PTGS2|TRPM3	endocrinology	primary dysmenorrhea (PD)
mefexamide	Preclinical	psychoactive drug			
mefloquine	Launched	adenosine receptor antagonist|hemoglobin antagonist		infectious disease	malaria
megestrol	Launched	progesterone receptor agonist		oncology	breast cancer
megestrol-acetate	Launched	progesterone receptor agonist	NR3C1|PGR	neurology/psychiatry|endocrinology	anorexia|cachexia
meglitinide	Phase 2	potassium channel blocker	CCR2		
meglumine	Launched	excipient			
meglutol	Launched	HMGCR inhibitor	HMGCR		
meisoindigo	Phase 3	STAT inhibitor	STAT3		
MEK1-2-inhibitor	Preclinical	MEK inhibitor	MAP2K2		
melanotan-ii	Launched	melanocortin receptor agonist			
melatonin	Launched	melatonin receptor agonist|nitric oxide synthase inhibitor	ASMT|CALM1|CALR|EPX|ESR1|HTR2B|MPO|MTNR1A|MTNR1B|NQO2|RORB	neurology/psychiatry	sleep cycle support
meldonium	Launched	gamma butyrobetaine hydroxylase inhibitor	BBOX1	cardiology	coronary artery disease (CAD)
melengestrol-acetate	Preclinical	progesterone receptor agonist			
melevodopa	Launched	dopamine precursor|dopamine receptor agonist	DDC	neurology/psychiatry	Parkinson's Disease
meloxicam	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	rheumatology	osteoarthritis|rheumatoid arthritis
melperone	Launched	dopamine receptor antagonist|serotonin receptor antagonist	DRD2|HTR2A	neurology/psychiatry	psychosis
melphalan	Launched	DNA alkylating agent|DNA inhibitor		hematologic malignancy	multiple myeloma
melphalan-n-oxide	Phase 1	hypoxia inducible factor inhibitor	HIF1A		
meluadrine	Preclinical				
memantine	Launched	glutamate receptor antagonist		neurology/psychiatry	Alzheimer's disease|senile dementia
menadione	Launched	mitochondrial DNA polymerase inhibitor|phosphatase inhibitor	AOX1|BGLAP|F10|F2|F7|F9|GGCX|NQO1|NQO2|PROC|PROS1|PROZ|VKORC1|VKORC1L1	gastroenterology|neurology/psychiatry|dermatology|rheumatology	ulcerative colitis|diarrhea|headache|varicose veins|rheumatoid arthritis
menadione-bisulfite	Phase 2	vitamin K	GGCX|VKORC1|VKORC1L1		
menatetrenone	Launched	bone resorption inhibitor		orthopedics	osteoporosis
menbutone	Launched			gastroenterology	bile stimulation
mepacrine	Launched	cytokine production inhibitor|NFkB pathway inhibitor|TP53 activator	PLA2G1B	infectious disease	giardiasis
meparfylon	Preclinical				
mepazine	Phase 2	MALT1 inhibitor (JH)	MALT1		
mepenzolate	Launched	acetylcholine receptor antagonist		gastroenterology	peptic ulcer disease (PUD)
mephenesin	Launched	muscle relaxant		neurology/psychiatry	muscle relaxant
mephentermine	Launched	adrenergic receptor agonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|ADRB1|ADRB2|ADRB3	cardiology	hypotension
mephenytoin	Launched	hydantoin antiepileptic	SCN5A	neurology/psychiatry	seizures
mepiroxol	Preclinical				
mepivacaine	Launched	potassium channel blocker|sodium channel blocker		neurology/psychiatry	local anesthetic
meprednisone	Launched		NR3C1		
meprylcaine	Preclinical	local anesthetic			
meptazinol	Launched	opioid receptor agonist	BCHE	neurology/psychiatry	pain relief
mepyramine	Launched	histamine receptor antagonist	HRH1	otolaryngology|obstetrics/gynecology	common cold|menstrual pain
mequinol	Launched		TYR	dermatology	skin depigmentation
merbarone	Phase 2	topoisomerase inhibitor	TOP2A		
merbromin	Launched	antiseptic		infectious disease	first-aid antiseptic
mercaptopurine	Launched	immunosuppressant|protein synthesis inhibitor|purine antagonist	HPRT1|IMPDH1|IMPDH2|PPAT	hematologic malignancy	acute lymphoblastic leukemia (ALL)
mercaptosuccinic-acid	Launched				
Merck60	Preclinical	HDAC inhibitor	HDAC1|HDAC2		
mericitabine	Phase 2	HCV inhibitor			
merimepodib	Phase 2	inosine monophosphate dehydrogenase inhibitor	IMPDH1		
meropenem	Launched	bacterial cell wall synthesis inhibitor		infectious disease	skin infections|intra-abdominal infections|meningitis
mertansine	Phase 2	microtubule inhibitor			
mesalazine	Launched	cyclooxygenase inhibitor|lipoxygenase inhibitor|prostanoid receptor antagonist	ALOX5|CHUK|IKBKB|MPO|PPARG|PTGS1|PTGS2	gastroenterology	ulcerative colitis|inflammatory bowel disease
mesna	Launched	antioxidant		urology	hemorrhagic cystitis
mesoridazine	Launched	dopamine receptor antagonist	DRD2|HTR2A	neurology/psychiatry	schizophrenia
mestinon	Launched	cholinesterase inhibitor	ACHE|BCHE	neurology/psychiatry	myasthenia gravis
mestranol	Launched	estrogen receptor agonist	ESR1	endocrinology	contraceptive
mesulergine	Phase 2	dopamine receptor agonist	HTR2A|HTR2B|HTR2C|HTR3A|HTR3B|HTR6|HTR7		
meta-cresyl-acetate	Preclinical				
metacetamol	Preclinical	analgesic agent			
metacresol	Launched		INS		
metafolin	Launched				
metamizole	Withdrawn	cyclooxygenase inhibitor|opioid receptor agonist	PTGS1		
metaphit	Preclinical	phencyclidine receptor acylator			
metaproterenol	Launched	adrenergic receptor agonist	ADRB2	pulmonary	bronchospasm|asthma|bronchitis|emphysema
metaraminol	Launched	adrenergic receptor agonist	ADRA1A	cardiology	hypotension
metatinib	Phase 1	Bcr-Abl kinase inhibitor	ABL1|BCR		
metaxalone	Launched	muscle relaxant		neurology/psychiatry	muscle pain
metazosin	Phase 2	adrenergic receptor antagonist	ADRA1A		
metenkephalin	Phase 2	immunostimulant	OPRD1		
metergoline	Launched	dopamine receptor agonist|serotonin receptor antagonist	HTR1A|HTR1B|HTR1D|HTR1E|HTR1F|HTR2A|HTR2B|HTR2C|HTR5A|HTR6|HTR7	neurology/psychiatry|endocrinology	seasonal affective disorder|anxiety|hyperprolactinemia
metformin	Launched	insulin sensitizer	ACACB|PRKAB1	endocrinology	diabetes mellitus
methacholine	Launched	acetylcholine receptor agonist	CHRM2|CHRM4	pulmonary	bronchial hyperresponsiveness diagnostic
methacycline	Preclinical	protein synthesis inhibitor		pulmonary	bronchitis
methanesulfonyl-fluoride	Phase 2	acetylcholinesterase inhibitor	ACHE		
methantheline	Launched	acetylcholine receptor antagonist	CHRM1|HRH2	gastroenterology|neurology/psychiatry|urology	peptic ulcer disease (PUD)|irritable bowel syndrome|pancreatitis|dyskinesia|neurogenic bladder
methapyrilene	Withdrawn	histamine receptor antagonist	HRH1		
metharbital	Launched	GABA receptor modulator	CHRNA4|CHRNA7|GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ|GRIA2|GRIK2	neurology/psychiatry	epilepsy
methazolamide	Launched	carbonic anhydrase inhibitor	CA1|CA12|CA14|CA2|CA4|CA7	ophthalmology	glaucoma|intraocular pressure
methenamine	Launched	bacterial DNA inhibitor		infectious disease	urinary tract infections
methiazole	Preclinical	anthelmintic agent			
methicillin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-negative bacterial infections|gram-positive bacterial infections
methimazole	Launched	antithyroid agent	TPO	endocrinology	hyperthyroidism
methionine	Launched		METAP2		
methiopril	Phase 2	angiotensin converting enzyme inhibitor	ACE		
methocarbamol	Launched	muscle relaxant	CA1	neurology/psychiatry	muscle relaxant
methoprene-(s)	Preclinical				
methotrexate	Launched	dihydrofolate reductase inhibitor	DHFR	oncology|hematologic malignancy|dermatology|rheumatology	gestational choriocarcinoma|hydatidiform mole|acute lymphoblastic leukemia (ALL)|psoriasis|rheumatoid arthritis
methoxamine	Launched	adrenergic receptor agonist	ADRA1A|ADRA1B|ADRA1D	cardiology	hypotension
methoxsalen	Launched	DNA synthesis inhibitor	CYP1A1|CYP1A2|CYP2A13|CYP2A6|CYP3A4	dermatology	psoriasis
methoxyamine	Phase 2	DNA repair enzyme inhibitor	APEX1		
methoxyflurane	Launched	membrane permeability inhibitor	ATP2C1|ATP5D|GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ|GLRA1|GLRB|GRIA1|KCNA1|MT-ND1	neurology/psychiatry	general anaesthetic
methoxyphenamine	Launched	adrenergic receptor agonist		pulmonary	asthma
methscopolamine	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3	gastroenterology	peptic ulcer disease (PUD)
methsuximide	Launched	T-type calcium channel blocker	CACNA1G|CACNA1H|CACNA1I	neurology/psychiatry	seizures
methyclothiazide	Launched	chloride reabsorption inhibitor	SLC12A1|SLC12A3	cardiology	hypertension|edema
methyl-aminolevulinate	Launched	oxidizing agent	FCGR1A|FECH	dermatology	actinic keratosis (AK)
methyl-nicotinate	Phase 2				
methyl-salicylate	Launched			endocrinology|neurology/psychiatry	fever|pain relief
methyl-5-hydroxytryptamine	Preclinical				
methylatropine-nitrate	Preclinical	acetylcholine receptor antagonist	CHRM1		
methylbenactyzium-bromide	Preclinical	cholinergic receptor antagonist			
methylbenzethonium-chloride	Preclinical	other antibiotic			
methylcobalamin	Phase 3	vitamin B			
methyldopa	Launched	adrenergic receptor agonist	ADRA2A|ADRA2B|ADRA2C|DDC	cardiology	hypertension
methyldopate	Launched			cardiology	hypertension
methylene-blue	Launched	guanylyl cyclase inhibitor|nitric oxide production inhibitor	ACHE	hematology	methemoglobinemia
methylergometrine	Launched	dopamine receptor antagonist|serotonin receptor antagonist	DRD1|HTR1E|HTR1F|HTR2A|HTR2B|HTR2C	hematology|neurology/psychiatry	postpartum hemorrhage (PPH)|migraine headache
methyllycaconitine	Preclinical	acetylcholine receptor antagonist	CHRNA7		
methylnaltrexone	Launched	opioid receptor antagonist	OPRD1|OPRK1|OPRM1	gastroenterology	constipation
methylparaben	Launched	other antifungal		dermatology	cosmetic
methylprednisolone	Launched	glucocorticoid receptor agonist	NR3C1	endocrinology|rheumatology|dermatology|infectious disease|allergy|hematology|neurology/psychiatry|gastroenterology	hypercalcemia|thyroiditis|ankylosing spondylitis|bursitis|osteoarthritis|psoriatic arthritis|seborrheic dermatitis|mycosis|allergic rhinitis|psoriasis|anemia|multiple sclerosis|ulcerative colitis|enteritis
methylprednisolone-aceponate	Launched	anti-inflammatory agent|glucocorticoid receptor agonist	NR3C1	endocrinology|rheumatology|infectious disease|allergy|pulmonary|gastroenterology|dermatology|neurology/psychiatry|hematology	congenital adrenal hyperplasia|thyroiditis|hypercalcemia|rheumatoid arthritis|bursitis|epicondylitis|allergic rhinitis|asthma|ulcerative colitis|enteritis|osteoarthritis|psoriasis|multiple sclerosis|anemia
methylprednisolone-sodium-succinate	Launched	glucocorticoid receptor agonist		endocrinology|rheumatology|dermatology|pulmonary|allergy|infectious disease|ophthalmology|gastroenterology|hematology|neurology/psychiatry	hypercalcemia|thyroiditis|osteoarthritis|rheumatoid arthritis|seborrheic dermatitis|asthma|allergic rhinitis|shingles|conjunctivitis|ulcerative colitis|enteritis|anemia|multiple sclerosis|mycosis
methylthiouracil	Launched			endocrinology	hyperthyroidism
methysergide	Launched	serotonin receptor antagonist	HTR1B|HTR1D|HTR1E|HTR1F|HTR2A|HTR2B|HTR2C|HTR5A|HTR6|HTR7	neurology/psychiatry	headache
meticrane	Launched	diuretic		cardiology	edema
metipranolol	Withdrawn	adrenergic receptor antagonist			
metirosine	Launched	tyrosine hydroxylase inhibitor	TH	cardiology	hypertension
metitepine	Preclinical	anti-HCVE2	HTR1A|HTR1B|HTR1D|HTR1E|HTR1F|HTR2A|HTR2B|HTR2C|HTR5A|HTR6|HTR7		
metixene	Launched	acetylcholine receptor antagonist	CHRM5	neurology/psychiatry	Parkinson's Disease
metoclopramide	Launched	dopamine receptor antagonist|serotonin receptor antagonist	CHRM1|DRD2|HTR3A|HTR3B|HTR4	gastroenterology	gastroparesis|nausea|vomiting
metocurine	Launched	acetylcholine receptor antagonist	CHRM2|CHRNA2	neurology/psychiatry	muscle relaxant
metolazone	Launched	carbonic anhydrase inhibitor	SLC12A3	cardiology	edema|hypertension
metoprolol	Launched	adrenergic receptor antagonist	ADRB1|ADRB2	cardiology	hypertension|angina pectoris|myocardial infarction
metoxibutropate	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2		
metrifonate	Phase 3	acetylcholinesterase inhibitor	ACHE		
metrizamide	Launched	radiopaque medium		radiology	contrast agent
metrizoic-acid	Launched	radiopaque medium		radiology	contrast agent
metronidazole	Launched	DNA inhibitor	CYP2C9|CYP3A4	dermatology	rosacea
metyrapone	Launched	cytochrome P450 inhibitor	CYP11B1	nephrology	adrenal diagnostic agent
mevastatin	Preclinical	HMGCR inhibitor	HMGCR		
mexeneone	Preclinical				
mexiletine	Launched	sodium channel blocker	PLAU|SCN4A|SCN5A	cardiology	ventricular arrhythmias|ventricular tachycardia (VT)
mezlocillin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-negative bacterial infections|gram-positive bacterial infections
ME0328	Preclinical	PARP inhibitor	PARP3		
MF-101	Phase 3	estrogen receptor agonist	CYP19A1|XDH		
MG-132	Preclinical	proteasome inhibitor	PSMB1		
MG-624	Preclinical	acetylcholine receptor antagonist	CHRNA7		
MGCD-265	Preclinical	VEGFR inhibitor	AXL|MET		
MI-14	Preclinical	PI4K inhibitor	PI4KB		
mianserin	Launched	serotonin receptor antagonist	ADRA1A|ADRA1B|ADRA1D|HRH1|HRH2|HTR2A|HTR2B|HTR2C|HTR6|HTR7	neurology/psychiatry	depression
mibampator	Phase 2	glutamate receptor modulator	GRIA1		
mibefradil	Withdrawn	T-type calcium channel blocker	ANO1|CACNA1C|CACNA1D|CACNA1F|CACNA1G|CACNA1H|CACNA1I|CACNA1S|CACNB1|CACNB2|CACNB3|CACNB4|CATSPER1|CATSPER2|CATSPER3|CATSPER4		
micafungin	Launched	"fungal 1,3-beta-D-glucan synthase inhibitor"		infectious disease	candidemia|peritonitis|esophageal candidiasis
miconazole	Launched	bacterial cell wall synthesis inhibitor	TRPM2|TRPV5	infectious disease|neurology/psychiatry	yeast infection|itching
micronomicin	Launched	protein synthesis inhibitor		infectious disease	gram-negative bacterial infections
midafotel	Phase 3	glutamate receptor antagonist	GRIN2A|GRIN2B|GRIN2C|GRIN2D		
midecamycin	Launched	protein synthesis inhibitor		infectious disease	respiratory tract infections|ear infections|skin infections
midodrine	Launched	adrenergic receptor agonist		cardiology	hypotension
midostaurin	Launched	FLT3 inhibitor|KIT inhibitor|PKC inhibitor	FLT3|PRKCG	hematologic malignancy	acute myeloid leukemia (AML)
mifepristone	Launched	glucocorticoid receptor antagonist|progesterone receptor antagonist	AR|NR1I2|NR3C1|PGR	endocrinology	hyperglycemia|diabetes mellitus
mifobate	Phase 2	PPAR receptor antagonist	PPARG		
miglitol	Launched	glucosidase inhibitor	GAA|GANAB|GANC|MGAM	endocrinology	diabetes mellitus
miglustat	Launched	glycosyl transferase inhibitor	UGCG	hematology	Gaucher disease
milacemide	Phase 3	monoamine oxidase inhibitor	MAOB		
milademetan	Phase 1	MDM inhibitor			
milnacipran	Launched	serotonin–norepinephrine reuptake inhibitor (SNRI)	SLC6A2|SLC6A4	rheumatology	fibromyalgia
milrinone	Launched	phosphodiesterase inhibitor	PDE2A|PDE3A|PDE3B|PDE5A	cardiology	congestive heart failure
miltefosine	Launched	membrane integrity inhibitor	PLA2G1B	infectious disease	leishmaniasis
mimosine	Preclinical	DNA replication inhibitor	CCL2|SHMT1|SHMT2|TYR		
minaprine	Withdrawn	serotonin reuptake inhibitor	ACHE|CHRM1|DRD1|DRD2|HTR2A|HTR2B|HTR2C|MAOA|SLC6A4		
minerval	Phase 1/Phase 2	FAAH inhibitor			
minocycline	Launched	bacterial 30S ribosomal subunit inhibitor		endocrinology|infectious disease|ophthalmology|urology	fever|respiratory tract infections|psittacosis|trachoma|conjunctivitis|urethritis|chancroid|tularemia|cholera|brucellosis
minodronic-acid	Launched	bone resorption inhibitor	FDPS|GGPS1	orthopedics	osteoporosis
minoxidil	Launched	KATP activator|Kir6 channel (KATP) activator|vasodilator	ABCC9|KCNJ1|KCNJ10|KCNJ11|KCNJ8|PTGS1	endocrinology	androgenetic alopecia
miocamycin	Launched	other antibiotic		infectious disease	urinary tract infections|chlamydia
MIRA-1	Preclinical	apoptosis stimulant			
mirabegron	Launched	adrenergic receptor agonist	ADRB1|ADRB2|ADRB3	urology	urinary incontinence
miridesap	Preclinical	amyloid protein inhibitor			
mirin	Preclinical	MRE11A exonuclease inhibitor	MRE11A		
miriplatin	Launched	DNA synthesis inhibitor		oncology	hepatocellular carcinoma (HCC)
mirodenafil	Launched	phosphodiesterase inhibitor	PDE5A	urology	erectile dysfunction
mirogabalin-besylate	Preclinical	calcium channel antagonist			
mirtazapine	Launched	adrenergic receptor antagonist|serotonin receptor antagonist	ADRA2A|ADRA2B|ADRA2C|HTR2A|HTR2C	neurology/psychiatry	depression
misonidazole	Phase 3				
misoprostol	Launched	prostanoid receptor agonist	PTGER2|PTGER3|PTGER4|PTGIR	gastroenterology	duodenal ulcer disease
mitapivat	Preclinical	pyruvate kinase isozyme activator			
mitiglinide	Launched	insulin secretagogue	ABCC8|KCNJ10|PPARG	endocrinology	diabetes mellitus
mitoflaxone	Phase 2	antitumor agent	VWF		
mitomycin-C	Launched	DNA alkylating agent|DNA synthesis inhibitor		oncology	pancreatic cancer|gastric adenocarcinoma
mitoquinone	Launched	antioxidant			
mitotane	Launched	antineoplastic agent	CYP11A1|CYP11B1|ESR1	oncology	adrenal cortical carcinoma
mitoxantrone	Launched	topoisomerase inhibitor	TOP2A	neurology/psychiatry|oncology|hematologic malignancy	multiple sclerosis|prostate cancer|acute myeloid leukemia (AML)
mivacurium	Launched	acetylcholine receptor antagonist	CHRNA2	critical care|neurology/psychiatry	endotracheal intubation|muscle relaxant
mivebresib	Phase 1	bromodomain inhibitor			
mivobulin	Phase 2	microtubule inhibitor			
MIW-815	Preclinical	interferon inducer			
mizolastine	Launched	histamine receptor antagonist	HRH1	allergy	urticaria|allergic rhinitis
mizoribine	Launched	immunosuppressant|inosine monophosphate dehydrogenase inhibitor	IMPDH1	transplant|rheumatology	organ rejection|nephrotic syndrome
MJ-15	Preclinical	cannabinoid receptor antagonist	CNR1		
MK-0354	Phase 2	niacin receptor agonist	HCAR2|HCAR3		
MK-0557	Phase 3	neuropeptide receptor antagonist			
MK-0608	Phase 1	antiviral			
MK-0752	Phase 1/Phase 2	gamma secretase inhibitor			
MK-0773	Phase 2	androgen receptor modulator	AR		
MK-0812	Phase 2	CC chemokine receptor antagonist	CCR2		
MK-0893	Phase 2	glucagon receptor antagonist	GCGR		
MK-1064	Phase 1	orexin receptor antagonist			
MK-1775	Phase 2	WEE1 kinase inhibitor	WEE1		
MK-1903	Phase 2	niacin receptor agonist			
MK-2048	Preclinical	HIV integrase inhibitor			
MK-2206	Phase 2	AKT inhibitor	AKT1|AKT2|AKT3		
MK-2295	Phase 2	TRPV antagonist	TRPV1		
MK-2461	Phase 1/Phase 2	FGFR inhibitor|VEGFR inhibitor	FGFR1|FGFR2|FGFR3|FLT1|FLT3|FLT4|KDR|MERTK|MET|MST1R|NTRK1|NTRK2|PDGFRB		
MK-2894	Preclinical	prostaglandin inhibitor	PTGER4		
MK-3207	Phase 2	calcitonin antagonist	CALCA		
MK-3697	Phase 2	orexin receptor antagonist	HCRTR2		
MK-4074	Phase 1	acetyl-CoA carboxylase inhibitor			
MK-5046	Preclinical	bombesin receptor agonist	BRS3|GRPR|NMBR		
MK-5108	Phase 1	Aurora kinase inhibitor	AURKA|AURKB|AURKC		
MK-571	Phase 2	leukotriene receptor antagonist	ABCC2|CYSLTR1		
MK-6096	Phase 2	orexin receptor antagonist	HCRTR1|HCRTR2		
MK-7246	Preclinical	CRTH receptor antagonist			
MK-7622	Phase 2	cholinergic receptor agonist			
MK-8033	Phase 1	c-Met inhibitor	MET		
MK-8245	Phase 2	stearoyl-CoA desaturase inhibitor	SCD		
MK-8617	Preclinical	hypoxia inducible factor prolyl hydroxylase inhibitor			
MK-8745	Preclinical	Aurora kinase inhibitor	AURKA		
MK-886	Preclinical	lipoxygenase inhibitor			
MK-8998	Phase 2	T-type calcium channel blocker			
MKT-077	Phase 1	HSP inhibitor			
MK2-IN-1	Preclinical	MAP kinase inhibitor	MAPKAPK2		
MLN0128	Phase 2	mTOR inhibitor	MTOR|PIK3CA|PIK3CD|PIK3CG		
MLN1117	Phase 2	PI3K inhibitor	PIK3CA		
MLN2480	Phase 1/Phase 2	RAF inhibitor			
MLN8054	Phase 1	Aurora kinase inhibitor	AURKA		
MLN9708	Phase 3	proteasome inhibitor			
ML10302	Preclinical	serotonin receptor partial agonist	HTR3A|HTR3B|HTR4		
ML130	Preclinical	NOD1 inhibitor			
ML133	Preclinical	potassium channel blocker			
ML141	Preclinical	GTPase inhibitor	CDC42		
ML161	Preclinical	protease-activated receptor inhibitor			
ML167	Preclinical	CLK inhibitor|DYRK inhibitor	CLK4|DYRK1B		
ML179	Preclinical	liver receptor homolog inverse agonist	NR5A2		
ML193	Preclinical	G protein-coupled receptor antagonist	GPR55		
ML204	Preclinical	transient receptor potential channel antagonist	TRPC4|TRPC5		
ML213	Preclinical	potassium channel activator	KCNQ4		
ML218	Preclinical	T-type calcium channel blocker	CACNA1G|CACNA1H|CACNA1I		
ML228	Preclinical	hypoxia inducible factor activator	HIF1A		
ML277	Preclinical	potassium channel activator	KCNQ1		
ML281	Preclinical	serine/threonine kinase inhibitor	STK33		
ML297	Preclinical	inward rectifier potassium channel activator	KCNJ3		
ML298	Preclinical	phospholipase inhibitor	PLD2		
ML314	Preclinical	neurotensin agonist	NTSR1		
ML323	Preclinical	ubiquitin specific protease inhibitor	USP1		
ML324	Preclinical	histone lysine demethylase inhibitor	KDM4A		
ML3403	Preclinical	MAP kinase inhibitor	CYP3A4|MAPK11|MAPK12|MAPK14		
ML347	Preclinical	ALK tyrosine kinase receptor inhibitor	ACVR1|ACVRL1|BMPR1A		
ML348	Preclinical	lysophospholipase inhibitor	LYPLA1		
ML365	Preclinical	potassium channel blocker	KCNK3|KCNK9		
ML786	Preclinical	RAF inhibitor	BRAF|RAF1		
ML9	Preclinical	myosin light chain kinase inhibitor	TRPC6		
MM-102	Preclinical	WDR5/MLL interaction inhibitor			
MM-11253	Preclinical	retinoid receptor antagonist	RARG		
MM-206	Preclinical	STAT inhibitor			
MMPX	Preclinical	phosphodiesterase inhibitor			
MMV-390048	Preclinical	PI4K inhibitor			
MM77	Preclinical	serotonin receptor antagonist	HTR1A		
MN-64	Preclinical	tankyrase inhibitor	TNKS		
MNITMT	Preclinical	lymphocyte inhibitor			
mocetinostat	Phase 2	HDAC inhibitor	HDAC1|HDAC11|HDAC2|HDAC3		
moclobemide	Launched	monoamine oxidase inhibitor	MAOA|MAOB	neurology/psychiatry	depression|anxiety
modaline	Preclinical				
moexipril	Launched	angiotensin converting enzyme inhibitor	ACE|ACE2	cardiology	hypertension
mofegiline	Phase 1	monoamine oxidase inhibitor	MAOA|MAOB		
mofezolac	Launched	cyclooxygenase inhibitor	PTGS1	rheumatology|orthopedics	rheumatoid arthritis|osteoporosis
moguisteine	Phase 2	ATP-sensitive potassium channel inhibitor			
molidustat	Phase 3	hypoxia inducible factor inhibitor	EGLN2		
molindone	Launched	dopamine receptor antagonist	DRD2|HRH1|HTR2A	neurology/psychiatry	schizophrenia
molsidomine	Launched	guanylate cyclase stimulant	GUCY1A3	cardiology	coronary artery disease (CAD)
mometasone	Launched	glucocorticoid receptor agonist	NR3C1	dermatology	corticosteroid-responsive dermatoses
mometasone-furoate	Launched	glucocorticoid receptor agonist	NR3C1	dermatology	corticosteroid-responsive dermatoses
monastrol	Preclinical	kinesin inhibitor	KIF11		
monensin	Launched	bacterial permeability inducer		infectious disease	gastrointestinal parasites
monepantel	Preclinical	mTOR inhibitor			
monobenzone	Launched	melanin inhibitor	TYR	dermatology	skin depigmentation
monocrotaline	Preclinical	antitumor agent			
monoctanoin	Launched			gastroenterology	gallstones
monomethyl-fumarate	Launched			neurology/psychiatry	multiple sclerosis
monosodium-alpha-luminol	Launched				
monostearin	Preclinical				
montelukast	Launched	leukotriene receptor antagonist	ALOX5|CYSLTR1	pulmonary|allergy	asthma|allergic rhinitis|exercise-induced bronchoconstriction (EIB)
moprolol	Launched	adrenergic receptor antagonist		cardiology|ophthalmology|neurology/psychiatry	hypertension|glaucoma|anxiety
moracizine	Withdrawn	sodium channel blocker	SCN5A	cardiology	ventricular arrhythmias
morantel	Launched	acetylcholine receptor agonist		infectious disease	tapeworm
morin	Preclinical	cytochrome P450 inhibitor	ADORA2A|ESR2|FASN|MCL1|SLC22A12		
morinidazole	Launched	other antibiotic	CYP51A1		
morniflumate	Launched	anti-inflammatory agent		neurology/psychiatry	pain relief
moroxydine	Launched	antiviral		infectious disease	influenza A virus infection
morphothiadin	Preclinical	antiinfective drug			
mosapride	Launched	serotonin receptor agonist	HTR4	gastroenterology	hypertrophic gastritis (GHG)|gastroesophageal reflux disease (GERD)|dyspepsia|irritable bowel syndrome
motapizone	Preclinical	phosphodiesterase inhibitor			
motesanib	Phase 3	KIT inhibitor|PDGFR tyrosine kinase receptor inhibitor|VEGFR inhibitor	FLT1|FLT4|KDR|KIT		
motolimod	Phase 2	toll-like receptor agonist	TLR8		
moxalactam	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-positive bacterial infections|gram-negative bacterial infections|skin infections|bone and joint infections|pneumonia|urinary tract infections|meningitis
moxaverine	Launched	phosphodiesterase inhibitor		neurology/psychiatry	spasms
moxidectin	Launched	chloride channel antagonist		infectious disease	gastrointestinal parasites
moxifloxacin	Launched	bacterial DNA gyrase inhibitor	TOP2A	otolaryngology|pulmonary|infectious disease	sinusitis|bronchitis|pneumonia|skin infections|intra-abdominal infections
moxisylyte	Withdrawn	adrenergic receptor antagonist			
moxonidine	Launched	imidazoline receptor agonist	ADRA2A|ADRA2B|ADRA2C	cardiology	hypertension
mozavaptan	Launched	vasopressin receptor antagonist	AVPR1A|AVPR1B|AVPR2	endocrinology	hyponatremia
MPEP	Preclinical	glutamate receptor antagonist	GRM1|GRM4|GRM5		
MPI-0479605	Preclinical	mitotic kinase inhibitor	TTK		
Mps-BAY-2a	Preclinical	monopolar spindle 1 kinase inhibitor	TTK		
Mps1-IN-1	Preclinical	monopolar spindle 1 kinase inhibitor	TTK		
Mps1-IN-5	Phase 1	protein kinase inhibitor			
MR-16728	Preclinical	acetylcholine release enhancer			
MR-948	Phase 1	thromboxane synthase inhibitor	TBXAS1		
MRK-016	Phase 1	GABA receptor inverse agonist	GABRA1|GABRA2|GABRA3|GABRA5		
MRK-409	Phase 1	benzodiazepine receptor agonist			
MRK-560	Preclinical	gamma secretase inhibitor	APP		
MRS-1220	Preclinical	adenosine receptor antagonist	ADORA2B|ADORA3		
MRS-1334	Preclinical	adenosine receptor antagonist	ADORA3		
MRS-1845	Preclinical	calcium channel blocker			
MRS-2578	Preclinical	purinergic receptor antagonist	P2RY6		
MRS-3777	Preclinical	adenosine receptor antagonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
MRX-2843	Phase 1	MER tyrosine kinase inhibitor			
MS-424	Phase 2	glutamate transporter modulator			
MSDC-0160	Phase 2	insulin sensitizer			
MSDC-0602K	Phase 2	mitochondrial pyruvate carrier modulator			
MSX-122	Phase 2	CC chemokine receptor antagonist	CXCR4		
MTPG	Preclinical	glutamate receptor antagonist	GRM2|GRM3		
mubritinib	Phase 1	protein tyrosine kinase inhibitor	EGFR|ERBB2		
mupirocin	Launched	isoleucyl-tRNA synthetase inhibitor		infectious disease	impetigo
muscimol	Phase 1	benzodiazepine receptor agonist	GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRR1|GABRR2|GABRR3		
MUT056399	Phase 1	FABI inhibitor			
MY-5445	Preclinical	phosphodiesterase inhibitor|platelet aggregation inhibitor	PDE5A		
mycophenolate-mofetil	Launched	dehydrogenase inhibitor|inositol monophosphatase inhibitor	IMPDH1|IMPDH2	transplant	organ rejection
mycophenolic-acid	Launched	dehydrogenase inhibitor|inositol monophosphatase inhibitor	IMPDH1|IMPDH2	transplant	organ rejection
myricetin	Preclinical	androgen receptor agonist|cytochrome P450 inhibitor	PIK3CG		
myricitrin	Preclinical	PKC inhibitor	NOS1|PRKCA		
myristyl-nicotinate	Phase 1	topical sunscreen agent			
M8-B	Preclinical	transient receptor potential channel antagonist	TRPM8		
N-(p-amylcinnamoyl)-anthranilic-acid	Preclinical	phospholipase inhibitor			
N-(2-chlorophenyl)-2-({(2E)-2-[1-(2-pyridinyl)ethylidene]hydrazino}carbothioyl)hydrazinecarbothioamide	Preclinical				
N-[2-(piperidinylamino)ethyl]-4-iodobenzamide	Preclinical	sigma receptor ligand			
N-acetyl-D-glucosamine	Phase 2/Phase 3		B4GALT1|B4GALT2|B4GALT3|B4GALT4|NAGK|NAGLU|NAGPA|RENBP		
N-acetyl-tyrosine	Launched				
N-acetylcarnosine	Launched				
N-acetylglycyl-D-glutamic-acid	Preclinical	glutamate receptor agonist			
N-acetylmannosamine	Phase 2				
N-acetyltryptamine	Preclinical	melatonin receptor agonist			
N-alpha-methylhistamine-dihydrochloride	Phase 3	histamine receptor agonist	HRH4		
N-benzylnaltrindole	Preclinical	opioid receptor antagonist			
N-cyclohexyl-2-benzothiazolesulfenamide	Preclinical				
N-hydroxynicotinamide	Preclinical				
"N-methyl-(-)ephedrine-[1R,2S]"	Preclinical				
N-methylformamide	Phase 2				
N-methyllidocaine-iodide	Preclinical	antiarrhythmic medication			
N-methylpyrrolidone	Phase 1				
N-methylquipazine	Preclinical	serotonin receptor agonist			
N-MPPP	Preclinical	opioid receptor agonist			
N-oxydiethylenebenzothiazole-2-sulfenamide	Preclinical				
N-salicoylaminophenol	Phase 1/Phase 2	ribonucleotide reductase inhibitor			
NAB-2	Preclinical	ubiquitin ligase transport promoter	NEDD4		
nabumetone	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	rheumatology	rheumatoid arthritis|osteoarthritis
nadide	Launched	free radical scavenger	AHCY|AKR1A1|ALDH2|BLVRA|DHPS|DLD|GALE|HMGCR|HSD17B1|HSD17B4|IMPDH2|MGAM|P2RY11|SORD|TRPM2		
nadifloxacin	Launched	bacterial DNA gyrase inhibitor		dermatology|infectious disease	acne vulgaris (AV)|skin infections
nadolol	Launched	adrenergic receptor antagonist	ADRB1|ADRB2|ADRB3	cardiology	angina pectoris|hypertension
NADPH	Preclinical		DRD2|DRD3|DRD4|GHSR|HTR2A|HTR2C		
nafadotride	Preclinical	dopamine receptor antagonist	DRD2|DRD3|HTR1A		
nafamostat	Launched	serine protease inhibitor	ASIC1|ASIC2|ASIC3|C1R|PRSS1|TPSAB1|TRPM7	cardiology	anticoagulent
nafcillin	Launched	bacterial cell wall synthesis inhibitor	CYP1A2|CYP3A4|SLC22A6	infectious disease	gram-positive bacterial infections
naftidrofuryl	Launched	adrenergic receptor antagonist		cardiology	claudication
naftifine	Launched	fungal squalene epoxidase inhibitor		infectious disease	tinea pedis|tinea cruris|tinea corporis
naftopidil	Launched	adrenergic receptor antagonist	ADRA1A	urology	benign prostatic hyperplasia (BPH)
nalbuphine	Launched	opioid receptor agonist|opioid receptor antagonist	OPRD1|OPRK1|OPRM1	neurology/psychiatry	pain relief
nalfurafine	Launched	opioid receptor agonist	OPRK1|OPRM1	nephrology	uremic pruritus
nalidixic-acid	Launched	bacterial DNA gyrase inhibitor		infectious disease	urinary tract infections
nalmefene	Launched	opioid receptor antagonist	OPRD1|OPRK1|OPRM1	pulmonary	respiratory depression
naloxegol	Launched	opioid receptor antagonist	OPRM1	gastroenterology	constipation
naloxone	Launched	opioid receptor antagonist	CREB1|ESR1|OPRD1|OPRK1|OPRM1|TLR4	pulmonary	respiratory depression
naloxone-benzoylhydrazone	Preclinical	opioid receptor antagonist	OPRK1|OPRM1		
naltrexone	Launched	opioid receptor antagonist	OPRD1|OPRK1|OPRM1|SIGMAR1	neurology/psychiatry	abstinence from alcohol
naltriben	Preclinical	opioid receptor antagonist	OPRD1|OPRK1|OPRM1		
naltrindole	Preclinical	opioid receptor antagonist	OPRD1|OPRK1|OPRM1		
Nampt-IN-1	Preclinical				
NAN-190	Preclinical	serotonin receptor agonist	ADRA1A|ADRA1B|ADRA1D|HTR1A|HTR1F		
nanchangmycin	Preclinical	other antibiotic			
napabucasin	Phase 3	STAT inhibitor	STAT3		
napamezole	Preclinical	adrenergic receptor antagonist|monoamine reuptake inhibitor			
naphazoline	Launched	adrenergic receptor agonist	ADRA1A|ADRA2A	ophthalmology	eye irritation
naphthoquine-phosphate	Launched	antimalarial agent		infectious disease	malaria
napirimus	Phase 1	immunosuppressant			
naproxen	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	neurology/psychiatry|rheumatology|dental|otolaryngology|endocrinology	pain relief|rheumatoid arthritis|headache|toothache|backache|muscle pain|common cold|fever
naquotinib	Phase 3	EGFR inhibitor			
narasin	Launched	antiprotozoal agent		infectious disease	coccidiosis
naratriptan	Launched	serotonin receptor agonist	HTR1A|HTR1B|HTR1D|HTR1E|HTR1F	neurology/psychiatry	migraine headache
naringenin	Phase 1	aromatase inhibitor|TRPV antagonist	CYP19A1|CYP1B1|ESR2|GLO1|HSD17B1		
naringeninic-acid	Phase 1		HCAR2|PTGR1		
naringin	Preclinical	cytochrome P450 inhibitor	SLCO1A2		
naringin-dihydrochalcone	Preclinical	cytochrome P450 inhibitor			
narlaprevir	Phase 3	HCV inhibitor			
NAS-181	Preclinical	serotonin receptor antagonist	HTR1B		
nastorazepide	Phase 2	CCK receptor antagonist	CCKBR		
natamycin	Launched	fungal ergosterol inhibitor		ophthalmology|infectious disease	conjunctivitis|fungal keratosis|blepharitis
nateglinide	Launched	insulin secretagogue	ABCC8|KCNJ10|KCNJ11|PPARG	endocrinology	diabetes mellitus
NAV-26	Preclinical	voltage-gated sodium channel blocker	SCN9A		
navarixin	Phase 2	CC chemokine receptor antagonist	CXCR1|CXCR2		
navitoclax	Phase 2	BCL inhibitor	BCL2|BCL2L1|BCL2L2		
naxagolide	Phase 3	dopamine receptor agonist			
NB-001	Preclinical	antiviral			
NBI-27914	Preclinical	corticotropin releasing factor receptor antagonist	CRHR1		
NBI-74330-(+/-)	Preclinical	CC chemokine receptor antagonist	CXCR3		
NBI-98782	Preclinical	vesicular monoamine transporter inhibitor			
NBQX	Preclinical	glutamate receptor antagonist	GRIA1|GRIA2|GRIA3|GRIA4|GRIK1|GRIN1|GRIN2A|GRIN2B		
NCS-382	Preclinical	GABA receptor antagonist	GABBR1|GABBR2|SLC52A2		
NCX-1015	Preclinical	interleukin sythesis stimulator			
NDD-094	Preclinical				
NDT-9513727	Preclinical	complement antagonist	C5AR1		
NE-100	Phase 2	sigma receptor antagonist	SIGMAR1		
nebivolol	Launched	adrenergic receptor antagonist	ADRB1	cardiology	hypertension
nebracetam	Phase 3	acetylcholine receptor agonist	CHRM1		
NECA	Launched	adenosine receptor agonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
necrostatin-1	Preclinical	RIPK inhibitor	RIPK1		
necrostatin-2	Preclinical	necroptosis inhibitor|RIPK inhibitor	RIPK2		
nedaplatin	Launched	DNA inhibitor		oncology	non-small cell lung cancer (NSCLC)|small cell lung cancer|esophageal cancer
nedocromil	Launched	histamine receptor antagonist	CYSLTR1|CYSLTR2|FPR1|HSP90AA1|PTGDR	neurology/psychiatry|ophthalmology	itching|conjunctivitis
nefazodone	Withdrawn	adrenergic inhibitor|norepinephrine reuptake inhibitor|serotonin receptor antagonist|serotonin reuptake inhibitor	ADRA1A|ADRA1B|ADRA2A|CYP3A4|HTR1A|HTR2A|HTR2C|SLC6A2|SLC6A3|SLC6A4		
nefiracetam	Phase 3	acetylcholine receptor agonist|benzodiazepine receptor agonist	CHRM1		
nefopam	Launched	cyclooxygenase inhibitor		neurology/psychiatry	pain relief
nelarabine	Launched	DNA synthesis inhibitor|T cell inhibitor	POLA1	hematologic malignancy	acute lymphoblastic leukemia (ALL)
nelfinavir	Launched	HIV protease inhibitor	CYP1A2|CYP2B6|CYP2C19|CYP2C9|CYP2D6|CYP3A4|CYP3A7	infectious disease	human immunodeficiency virus (HIV-1)
nelociguat	Preclinical	guanylate cyclase stimulant			
nelotanserin	Phase 2	serotonin receptor inverse agonist			
nemazoline	Phase 2	adrenergic receptor agonist|adrenergic receptor antagonist			
nemiralisib	Phase 2				
nemonapride	Launched	dopamine receptor antagonist	DRD2|DRD3|DRD4	neurology/psychiatry	schizophrenia
nemorexant	Preclinical	orexin receptor antagonist			
nemorubicin	Phase 2	topoisomerase inhibitor	TOP1|TOP2A		
neo-gilurytmal	Launched			cardiology	cardiac arrythmia
neohesperidin	Preclinical				
neohesperidin-dihydrochalcone	Preclinical				
neomycin	Launched	bacterial 30S ribosomal subunit inhibitor	CXCR4	infectious disease|gastroenterology	first-aid antibiotic|hepatic encephalopathy (HE)|intra-abdominal infections
neostigmine	Launched	acetylcholinesterase inhibitor	ACHE	neurology/psychiatry	myasthenia gravis
nepafenac	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	ophthalmology	eye inflammation
nepicastat	Phase 2	dopamine beta hydroxylase inhibitor	DBH		
neratinib	Launched	EGFR inhibitor	EGFR|ERBB2|KDR	oncology	breast cancer
nerbacadol	Phase 3	cyclooxygenase inhibitor			
neridronic-acid	Launched	bone resorption inhibitor	FDPS	endocrinology	brittle bone disease|Paget's disease
nesbuvir	Phase 2	RNA polymerase inhibitor			
netilmicin	Launched	protein synthesis inhibitor		infectious disease	gram-negative bacterial infections
netupitant	Launched	tachykinin antagonist	TACR1	gastroenterology	nausea|vomiting
neurodazine	Preclinical	neurogenesis of non-pluripotent C2C12 myoblast inducer			
neuropathiazol	Preclinical	neural stem cell inducer	BMP2|LIF		
Neu2000	Phase 2	ionotropic glutamate receptor antagonist			
nevirapine	Launched	non-nucleoside reverse transcriptase inhibitor	CYP1A2|CYP2A6|CYP2B6|CYP2C9|CYP2D6|CYP3A4|CYP3A5	infectious disease	human immunodeficiency virus (HIV-1)
nexturastat-A	Preclinical	HDAC inhibitor	HDAC1|HDAC6		
NFKB-activation-inhibitor-II	Preclinical	NFkB pathway inhibitor	RELA		
NG-nitro-arginine	Phase 1	nitric oxide synthase inhibitor	NOS1|NOS2|NOS3		
NGB-2904	Preclinical	dopamine receptor antagonist	DRD3		
NGD-94-1	Phase 1	dopamine receptor antagonist	DRD4		
NGD-98-2	Preclinical	corticotropin releasing factor receptor antagonist	CRHR1		
NGP555	Phase 1	gamma secretase modulator			
NHI-2	Preclinical	lactate dehydrogenase inhibitor	LDHA		
NH125	Preclinical	eukaryotic translation elongation factor 2 inhibitor			
NI-57	Preclinical	bromodomain inhibitor	BRD1|BRPF1|BRPF3		
niacin	Launched	NAD precursor|vitamin B	DGAT2|HCAR1|HCAR2|HCAR3|NNMT|QPRT	endocrinology	hypertriglyceridemia
nialamide	Withdrawn	monoamine oxidase inhibitor	COMT|MAOA|MAOB		
nibentan	Phase 2	potassium channel blocker			
nicainoprol	Preclinical	angiotensin converting enzyme inhibitor			
nicaraven	Phase 3	free radical scavenger			
nicardipine	Launched	calcium channel blocker	ADORA3	cardiology	chronic stable angina|hypertension
nicergoline	Launched	adrenergic receptor antagonist	ADRA1A	rheumatology|neurology/psychiatry|cardiology|hematology	Raynaud's disease|migraine headache|atherosclerosis|thrombosis
niceritrol	Launched	NAD precursor		endocrinology	hyperlipidemia
niclosamide	Launched	DNA replication inhibitor|STAT inhibitor	STAT3	infectious disease	tapeworm
nicodicosapent	Preclinical	sterol regulatory element binding protein (SREBP) inhibitor			
nicorandil	Launched	nitric oxide donor|potassium channel activator	KCNJ11	cardiology	angina pectoris
nicotinamide	Launched	protein synthesis stimulant	BST1|LDHA|PARP1|SIRT5	dermatology	acne vulgaris (AV)
nicotine	Launched	acetylcholine receptor agonist	CHAT|CHRNA10|CHRNA2|CHRNA3|CHRNA4|CHRNA5|CHRNA6|CHRNA7|CHRNA9|CHRNB2|CHRNB3|CHRNB4|CYP19A1|TBXAS1|TRPA1	neurology/psychiatry	smoking cessation
nicotinyl-alcohol-tartrate	Launched			cardiology|neurology/psychiatry	vascular spasm|vertigo
NIDA-41020	Preclinical	cannabinoid receptor antagonist	CNR1		
nifedipine	Launched	calcium channel blocker	CACNA1C|CACNA1D|CACNA1F|CACNA1H|CACNA1S|CACNA2D1|CACNB2|CALM1|GLRA1|GLRA3|GLRB|KCNA1|KCNA5|NR1I2|TRPM3	cardiology	vasospastic angina|chronic stable angina
nifekalant	Launched	potassium channel blocker		cardiology	ventricular arrhythmias|ventricular tachycardia (VT)
nifenalol	Launched	adrenergic receptor antagonist	ADRB1|ADRB2		
nifenazone	Launched	analgesic agent		neurology/psychiatry	pain relief
niflumic-acid	Launched	cyclooxygenase inhibitor	ANO1|CLCN1|CLCNKA|CLCNKB|KCNQ1|PLA2G1B|PLA2G4A|PTGS1|PTGS2|UGT1A9	rheumatology|neurology/psychiatry	joint pain|muscle pain
nifuroxazide	Launched	bacterial DNA inhibitor		gastroenterology	colitis|diarrhea
nifursol	Launched	bacterial DNA inhibitor			
nifurtimox	Launched	DNA inhibitor		infectious disease	Chagas disease|African trypanosomiasis
niguldipine-(R)-(-)	Preclinical				
niguldipine-(S)-(+)	Preclinical	adrenergic receptor antagonist	ADRA1A		
nikethamide	Withdrawn	immunostimulant			
nilotinib	Launched	Abl kinase inhibitor|Bcr-Abl kinase inhibitor	ABL1|KIT	hematologic malignancy	chronic myeloid leukemia (CML)
nilutamide	Launched	androgen receptor antagonist	AR	oncology	prostate cancer
nilvadipine	Launched	calcium channel blocker	CACNA1C|CACNA1D	cardiology	hypertension|cerebral artery occlusion
nimesulide	Launched	cyclooxygenase inhibitor	LTF|PLA2G2E|PTGS1|PTGS2	rheumatology|obstetrics/gynecology	osteoarthritis|menstrual pain
nimodipine	Launched	calcium channel blocker	CFTR|NR3C2	hematology	hemorrhage
nimorazole	Launched	bacterial DNA inhibitor		oncology	head and neck squamous cell carcinoma (HNSCC)
nimustine	Launched	DNA alkylating agent			
NIM811	Phase 2	mitochondrial permeability transition inhibitor			
ningetinib-tosylate	Preclinical	protein tyrosine kinase inhibitor			
nintedanib	Launched	FGFR inhibitor|PDGFR tyrosine kinase receptor inhibitor|VEGFR inhibitor	FGFR1|FGFR2|FGFR3|FGFR4|FLT1|FLT4|KDR|PDGFRA|PDGFRB	pulmonary	idiopathic pulmonary fibrosis (IPF)
niraparib	Launched	PARP inhibitor	PARP1	oncology	primary peritoneal cancer (PPC)
niridazole	Launched	phosphofructokinase inhibitor		infectious disease	schistosomiasis
nisin	Phase 1	bacterial cell wall synthesis inhibitor			
nisoldipine	Launched	calcium channel blocker	CACNA1C|CACNA1D|CACNA1F|CACNA1S	cardiology	hypertension
nisoxetine	Phase 1	norepinephrine reuptake inhibitor	SLC6A2|SLC6A3|SLC6A4		
nitarsone	Launched			dermatology	blackhead disease
nitazoxanide	Launched	pyruvate ferredoxin oxidoreductase inhibitor		gastroenterology	diarrhea
nitecapone	Phase 2	catechol O methyltransferase inhibitor	COMT		
nitenpyram	Launched			infectious disease	flea control
nithiamide	Preclinical	bacterial DNA inhibitor			
nitisinone	Launched	hydroxyphenylpyruvate dioxygenase inhibitor		metabolism	tyrosinemia
nitrendipine	Launched	calcium channel blocker	CACNA1D|CACNA2D1|KCNN4	cardiology	hypertension
nitrocaramiphen	Preclinical	cholinergic receptor antagonist	CHRM1		
nitroflurbiprofen	Preclinical	cyclooxygenase inhibitor			
nitrofurantoin	Launched	DNA inhibitor		infectious disease	urinary tract infections|pyelonephritis
nitrofurazone	Launched	bacterial DNA inhibitor		infectious disease	first-aid antibiotic
nitromide	Launched			infectious disease	coccidiosis
nitrosodimethylurea	Preclinical	DNA synthesis inhibitor			
nitroxoline	Launched	cathepsin inhibitor	METAP2	infectious disease	urinary tract infections
nizatidine	Launched	histamine receptor antagonist	HRH2	gastroenterology	duodenal ulcer disease|erosive esophagitis (EE)|ulcerative esophagitis (UE)|gastroesophageal reflux disease (GERD)
nizofenone	Launched	ion channel antagonist		neurology/psychiatry	stroke
NK-252	Preclinical	nuclear factor erythroid derived|like (NRF2) activator	NFE2L2		
NKP-1339	Phase 1	HSP inhibitor			
NKY-80	Preclinical	adenylyl cyclase inhibitor	ADCY5		
NLG919	Phase 1	"indoleamine 2,3-dioxygenase inhibitor"	IDO1		
NMDA	Preclinical	glutamate receptor agonist	GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D		
NMS-E973	Preclinical	HSP inhibitor			
NMS-P715	Preclinical	protein kinase inhibitor			
NMS-1286937	Phase 2	PLK inhibitor	FLT3|PLK1|PLK2|PLK3		
NMS-873	Preclinical	ATPase inhibitor	VCP		
NM107	Phase 2	RNA polymerase inhibitor			
NN-DNJ	Preclinical	glucosidase inhibitor	GBA		
NNC-05-2090	Preclinical	GABA uptake inhibitor|GAT inhibitor	SLC6A12		
NNC-55-0396	Preclinical	T-type calcium channel blocker	CATSPER1|CATSPER2|CATSPER3|CATSPER4		
NNC-63-0532	Preclinical	opioid receptor agonist	OPRL1		
NNC-711	Preclinical	GABA uptake inhibitor	SIGMAR1|SLC6A1		
NO-ASA	Phase 2	cyclooxygenase inhibitor	PTGS2		
nobiletin	Preclinical	MEK inhibitor	MAP2K1		
nocodazole	Preclinical	tubulin polymerization inhibitor	HPGDS		
nolatrexed	Phase 3	thymidylate synthase inhibitor	TYMS		
nomegestrol-acetate	Launched	progesterone receptor agonist	PGR	endocrinology	contraceptive
nomifensine	Withdrawn	dopamine reuptake inhibitor|noradrenaline uptake inhibitor	DRD2|SLC6A2|SLC6A3		
nonivamide	Launched	TRPV agonist	TRPV1	rheumatology|neurology/psychiatry	rheumatoid arthritis|muscle pain
nonoxynol-9	Launched	membrane integrity inhibitor		endocrinology	contraceptive
nor-binaltorphimine	Preclinical	opioid receptor antagonist	OPRD1|OPRK1|OPRM1		
norcyclobenzaprine	Preclinical	adrenergic receptor agonist|serotonin receptor antagonist			
norelgestromin	Launched		PGR	endocrinology	contraceptive
norepinephrine	Launched	adrenergic receptor agonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|ADRB1|ADRB2|ADRB3|PAH|SLC18A1|SLC18A2	cardiology|allergy|neurology/psychiatry	hypertension|urticaria|headache|seasonal affective disorder
norethindrone	Launched	progesterone receptor agonist	PGR	obstetrics/gynecology	endometriosis
norethindrone-acetate	Launched	progesterone receptor agonist	PGR	endocrinology|orthopedics|obstetrics/gynecology	menopause|osteoporosis|vaginal atrophy
norethisterone-enanthate	Launched	contraceptive agent		endocrinology	contraceptive
noretynodrel	Launched	progestogen hormone	PGR	endocrinology	contraceptive
norfloxacin	Launched	bacterial DNA gyrase inhibitor	TOP2A	infectious disease|urology	urinary tract infections|gonorrhea|prostatitis
norfluoxetine	Phase 1	selective serotonin reuptake inhibitor (SSRI)	HTR2B		
norgestimate	Launched	progesterone receptor agonist	ESR1|PGR	endocrinology	contraceptive
norgestrel	Launched	progesterone receptor agonist	AR|ESR1|PGR|SRD5A1	endocrinology	contraceptive
nornicotine	Preclinical	acetylcholine receptor agonist			
nortriptyline	Launched	tricyclic antidepressant	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|ADRB1|ADRB2|ADRB3|CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|DRD2|HRH1|HTR1A|HTR2A|HTR2C|HTR6|KCNJ10|PGRMC1|SIGMAR1|SLC6A2|SLC6A4	neurology/psychiatry	depression
norvancomycin	Preclinical				
noscapine	Launched	bradykinin receptor antagonist|tubulin polymerization inhibitor	SIGMAR1	pulmonary	cough suppressant
NOV-002	Phase 3		GSR		
novobiocin	Launched	bacterial DNA gyrase inhibitor		obstetrics/gynecology	mastitis
NPC-01	Phase 3	steroid			
NPC-15199	Phase 2	ICAM1 antagonist	PPARG		
NPPB	Preclinical	chloride channel blocker	ANO1|CLCN2|CLCN7|TRPA1		
NPS-2143	Preclinical	calcium receptor antagonist	CASR		
NPS-2407	Preclinical	glutamate receptor antagonist			
NPY-5RA972	Preclinical	neuropeptide receptor antagonist	NPY5R		
NQDI-1	Preclinical	caspase inhibitor	CASP3		
NS-018	Phase 1/Phase 2	JAK inhibitor	JAK1|JAK2|JAK3|TYK2		
NS-11021	Preclinical	calcium-activated potassium channel activator	KCNMA1		
NS-11394	Preclinical	GABA receptor agonist			
NS-1643	Preclinical	voltage-gated potassium channel activator	KCNH2|KCNH6|KCNMA1		
NS-19504	Preclinical	calcium-activated potassium channel activator	KCNMA1		
NS-309	Preclinical	calcium-activated potassium channel activator	KCNN1|KCNN2|KCNN3|KCNN4		
NS-3623	Preclinical	voltage-gated potassium channel activator	KCNH2		
NS-3861	Preclinical	acetylcholine receptor agonist	CHRNA3|CHRNB4		
NS-5806	Preclinical	voltage-gated potassium channel activator	KCND3		
NS-8	Phase 2	potassium channel agonist	KCNMA1		
NS-8593	Preclinical	calcium-activated potassium channel modulator	KCNN1|KCNN2|KCNN3		
NS-9283	Preclinical	acetylcholine receptor allosteric modulator	CHRNA4		
NSC-23766	Preclinical	Ras GTPase inhibitor			
NSC-319726	Preclinical	p53 activator			
NSC-3852	Preclinical	HDAC inhibitor	HDAC1		
NSC-405020	Preclinical	matrix metalloprotease inhibitor	MMP1		
NSC-4644	Phase 2	ACAT inhibitor|sterol regulatory element binding protein (SREBP) inhibitor	PYGM		
NSC-5844	Preclinical	CC chemokine receptor agonist	CCR1		
NSC-625987	Preclinical	CDK inhibitor	CDK2|CDK4		
NSC-632839	Preclinical	ubiquitin specific protease inhibitor	SENP2|USP1|USP2|USP7		
NSC-636819	Preclinical	histone demethylase inhibitor	KDM4A|KDM4B		
NSC-663284	Preclinical	CDC inhibitor	CDC25A|CDC25B|CDC25C		
NSC-697923	Preclinical	ubiquitin-conjugating enzyme inhibitor	UBE2N		
NSC-95397	Preclinical	CDC inhibitor	CDC25A|CDC25B		
NSC-9965	Preclinical	acetylcholine receptor antagonist	CHRNA4|CHRNB2		
NSI-189	Phase 2	neurotrophic agent			
NSP-805	Preclinical	phosphodiesterase inhibitor			
NTNCB	Preclinical	neuropeptide receptor antagonist	NPY5R		
NTRC-824	Preclinical	neurotensin receptor antagonist	NTSR2		
nTZDpa	Preclinical	PPAR receptor agonist	PPARG		
NT157	Preclinical	IGF-1 inhibitor	IGF1R		
NU-1025	Preclinical	PARP inhibitor	PARP1		
NU-2058	Preclinical	cyclin D inhibitor	CCNA2|CDK2		
NU-6027	Preclinical	CDK inhibitor	CCNA2|CDK2		
NU-7026	Preclinical	DNA dependent protein kinase inhibitor|mTOR inhibitor|PI3K inhibitor	PRKDC		
NU-7441	Preclinical	DNA dependent protein kinase inhibitor	PRKDC		
nuclomedone	Phase 3	immunosuppressant			
nutlin-3	Preclinical	MDM inhibitor	MDM2|TP53		
nuvenzepine	Preclinical	acetylcholine receptor antagonist			
NVP-ADW742	Preclinical	insulin growth factor receptor inhibitor	IGF1R		
NVP-AEW541	Preclinical	IGF-1 inhibitor	IGF1R|INSR		
NVP-AUY922	Phase 2	HSP inhibitor	HSP90AA1|HSP90AB1		
NVP-BEZ235	Phase 3	mTOR inhibitor|PI3K inhibitor	ATR|MTOR|PIK3CA|PIK3CD|PIK3CG		
NVP-BGJ398	Phase 3	FGFR inhibitor	FGFR1|FGFR2|FGFR3|FGFR4|KDR		
NVP-BHG712	Preclinical	ephrin inhibitor	EPHB4		
NVP-BSK805	Preclinical	JAK inhibitor	JAK2		
NVP-BVU972	Preclinical	MET inhibitor	MET		
NVP-DPP728	Phase 2	dipeptidyl peptidase inhibitor	DPP4		
NVP-HSP990	Phase 1	HSP inhibitor	HSP90AA1|HSP90AB1		
NVP-TAE226	Preclinical	protein tyrosine kinase inhibitor	PTK2		
NVP-TAE684	Preclinical	ALK tyrosine kinase receptor inhibitor	ALK|INSR		
NVP-TNKS656	Preclinical	tankyrase inhibitor	TNKS2		
NVP-231	Preclinical	ceramidase inhibitor	CERK		
NVS-PAK1-1	Preclinical	p21 activated kinase inhibitor	PAK1		
NXY-059	Phase 3	free radical scavenger			
nystatin	Launched	fungal ergosterol inhibitor		infectious disease	esophageal candidiasis|skin infections|yeast infection
N20C	Preclinical	glutamate receptor antagonist			
N6-cyclopentyladenosine	Preclinical	adenosine receptor agonist	ADORA1|ADORA2A|ADORA2B|ADORA3|SLC29A1		
N6-methyladenosine	Preclinical				
N6022	Phase 1/Phase 2	alcohol dehydrogenase inhibitor	ADH5		
O-acetyl-L-serine	Preclinical		PTGS1		
o-mercapto-benzoic-acid	Preclinical				
O-1918	Preclinical	cannabinoid receptor antagonist			
o-3M3FBS	Preclinical	phospholipase activator			
O-304	Preclinical	AMPK activator			
OAC1	Preclinical	Oct activator			
OAC2	Preclinical	Oct activator	POU5F1		
obatoclax	Phase 3	BCL inhibitor	BCL2		
obeticholic-acid	Launched	FXR agonist	NR1H4	gastroenterology	primary biliary cholangitis
obidoxime	Launched	cholinesterase reactivator	ACHE	critical care|neurology/psychiatry	poison antidote|nerve gas poisoning
ocaperidone	Preclinical	serotonin receptor antagonist			
ochromycinone	Phase 1	STAT inhibitor	STAT3		
ocinaplon	Phase 3	GABA receptor modulator	GABRA1|GABRA2|GABRA3|GABRA5		
OCO-1112	Phase 2	cholesterol inhibitor			
octadecan-1-ol	Preclinical				
octamethyltrisiloxane	Preclinical				
octenidine	Launched	membrane integrity inhibitor		infectious disease	gram-negative bacterial infections|gram-positive bacterial infections
octinoxate	Launched			dermatology	sunscreen lotion
octisalate	Launched			dermatology	sunscreen lotion
octocrylene	Launched			dermatology	sunscreen lotion
octodrine	Preclinical	antitumor agent			
octopamine	Preclinical	trace amine associated receptor agonist	F10|TAAR1		
octreotide	Launched	somatostatin receptor agonist	SSTR2|SSTR3|SSTR5	gastroenterology|endocrinology|oncology	diarrhea|acromegaly|carcinoid tumors
OC000459	Phase 2	CRTH receptor antagonist	PTGDR2		
odanacatib	Phase 3	cathepsin inhibitor	CTSK		
ODQ	Preclinical	guanylyl cyclase inhibitor	GUCY1A2|GUCY1A3|GUCY1B3		
OF-1	Preclinical	bromodomain inhibitor	BRD1		
ofloxacin	Launched	bacterial DNA gyrase inhibitor		infectious disease|otolaryngology|gastroenterology|endocrinology	respiratory tract infections|sinusitis|skin infections|bone and joint infections|intra-abdominal infections|diarrhea|fever|urinary tract infections
OG-L002	Preclinical	histone lysine demethylase inhibitor	KDM1A		
ogerin	Preclinical	G protein-coupled receptor modulator			
oglemilast	Phase 2	phosphodiesterase inhibitor			
oglufanide	Phase 2	VEGF antagonist			
OICR-9429	Preclinical	WDR5/MLL interaction inhibitor	WDR5		
olanzapine	Launched	dopamine receptor antagonist|serotonin receptor antagonist	ADRA1A|ADRA1B|ADRA2A|ADRA2B|ADRA2C|ADRB1|ADRB2|ADRB3|CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|DRD1|DRD2|DRD3|DRD4|DRD5|GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ|HRH1|HRH2|HRH4|HTR1A|HTR1B|HTR1D|HTR1E|HTR1F|HTR2A|HTR2B|HTR2C|HTR3A|HTR5A|HTR6|HTR7	neurology/psychiatry	schizophrenia|bipolar disorder
olaparib	Launched	PARP inhibitor	PARP1|PARP2	oncology	ovarian cancer
OLDA	Preclinical	TRPV agonist	GPR119		
oleamide	Preclinical	cannabinoid receptor agonist	HTR7|PLA2G2A		
oleandrin	Phase 1	Na/K-ATPase inhibitor			
oleanolic-acid	Preclinical	G protein-coupled receptor agonist	GPBAR1		
oleoylethanolamide	Preclinical	cannabinoid receptor agonist|glucose dependent insulinotropic receptor agonist|potassium channel blocker|PPAR receptor agonist	CNR1|GPR119|GPR55|PPARA		
olesoxime	Phase 2/Phase 3	apoptosis stimulant			
oleuropein	Phase 2	estrogen receptor agonist	GPER1		
oligomycin-A	Preclinical	ATP synthase inhibitor|ATPase inhibitor	ATP5A1		
olmesartan	Launched	angiotensin receptor antagonist	AGTR1	cardiology	hypertension
olmesartan-medoxomil	Launched	angiotensin receptor antagonist	AGTR1	cardiology	hypertension
olmutinib	Launched	Bruton's tyrosine kinase (BTK) inhibitor|EGFR inhibitor	BTK|EGFR	oncology	non-small cell lung cancer (NSCLC)
olodanrigan	Phase 2	angiotensin antagonist			
olomoucine	Preclinical	CDK inhibitor	CDK1|CDK2|CDK5|MAPK1		
olopatadine	Launched	histamine receptor antagonist	HRH1|S100A1|S100A12|S100A13|S100A2|S100B	ophthalmology	conjunctivitis
olprinone	Launched	phosphodiesterase inhibitor	PDE3A	cardiology	congestive heart failure
olsalazine	Launched	cyclooxygenase inhibitor	IFNG|TPMT	gastroenterology	ulcerative colitis
oltipraz	Phase 3	nuclear factor erythroid derived|like (NRF2) activator	ANG		
olumacostat-glasaretil	Phase 3	acetyl-CoA carboxylase inhibitor			
olvanil	Preclinical	TRPV agonist	CNR1|GPR119|TRPV1		
omadacycline	Launched	bacterial 30S ribosomal subunit inhibitor		infectious disease	pneumonia
omapatrilat	Preclinical	metalloproteinase inhibitor	ACE|MME		
omarigliptin	Launched	dipeptidyl peptidase inhibitor	DPP4	endocrinology	diabetes mellitus
ombitasvir	Launched	HCV inhibitor		infectious disease	hepatitis C
ombrabulin	Phase 3	tubulin polymerization inhibitor			
OMDM-2	Preclinical	FAAH inhibitor	GPR119		
omecamtiv-mecarbil	Phase 3	cardiac myosin activator	MYBPC3		
omega-(4-iodophenyl)pentadecanoic-acid	Preclinical				
omega-3-acid-esters	Launched	cholesterol inhibitor			
omeprazole	Launched	ATPase inhibitor	ATP4A|CLCN2	gastroenterology	heartburn
omeprazole-magnesium	Launched	proton pump inhibitor	ATP4A|ATP4B	gastroenterology	gastroesophageal reflux disease (GERD)|heartburn
omeprazole-sulfide	Phase 1	ATPase inhibitor			
omtriptolide	Preclinical	ERK1 and ERK2 phosphorylation inhibitor			
ON-01500	Preclinical	apoptosis stimulant			
oncrasin-1	Preclinical	apoptosis stimulant			
ONC201	Phase 2	AKT inhibitor|MAP kinase inhibitor	TNFSF10		
ondansetron	Launched	serotonin receptor antagonist	HTR3A|HTR3B	gastroenterology	nausea|vomiting
ONO-AE3-208	Preclinical	prostanoid receptor antagonist	PTGER4		
ONO-4059	Phase 1	Bruton's tyrosine kinase (BTK) inhibitor	BTK		
ONO-4817	Phase 1	matrix metalloprotease inhibitor	MMP8		
ONO-8130	Preclinical	prostanoid receptor antagonist	PTGER1		
ONX-0914	Preclinical	proteasome inhibitor			
ON123300	Preclinical	CDK inhibitor	CDK4|NUAK1|PDGFRB		
OP-0595	Preclinical	beta lactamase inhibitor			
OPC-21268	Phase 1	vasopressin receptor antagonist	AVPR1A|AVPR2|OXTR		
opicapone	Phase 3	catechol O methyltransferase inhibitor	COMT		
opipramol	Launched	sigma receptor agonist		neurology/psychiatry	generalized anxiety disorder (GAD)
oprozomib	Phase 1/Phase 2	proteasome inhibitor			
OR-486	Preclinical	catechol O methyltransferase inhibitor	COMT		
orantinib	Phase 3	FGFR inhibitor|PDGFR tyrosine kinase receptor inhibitor|VEGFR inhibitor	AURKA|AURKB|EGFR|FGFR1|FGFR2|KDR|PDGFRA|PDGFRB		
orbifloxacin	Launched	bacterial DNA gyrase inhibitor		infectious disease	urinary tract infections
ORE1001	Phase 1/Phase 2	angiotensin converting enzyme inhibitor	ACE2		
ORG-12962	Phase 2	serotonin receptor agonist	HTR2A|HTR2B|HTR2C		
ORG-25543	Preclinical	glycine transporter inhibitor	GLRB|SLC6A5		
ORG-26576	Phase 2	glutamate receptor modulator			
ORG-27569	Preclinical	cannabinoid receptor modulator	CNR1		
ORG-9768	Phase 1	adrenergic receptor antagonist	ADRA2A		
oridonin	Preclinical	BCL inhibitor	BCL2		
oritavancin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	skin infections
orlistat	Launched	lipase inhibitor	CNR1|DAGLA|DAGLB|FASN|LIPF|PNLIP	endocrinology	weight-loss aid
ormeloxifene	Launched	selective estrogen receptor modulator (SERM)		endocrinology	contraceptive
ornidazole	Launched	antiprotozoal agent		infectious disease	protozoan infection
ornipressin	Preclinical	vasoconstrictor			
ornithine	Launched	NFkB pathway modulator	GPRC6A		
orotic-acid	Phase 2		DHODH		
orphanin-fq	Phase 1	opioid receptor agonist	OPRL1|OPRM1		
orphenadrine	Launched	acetylcholine receptor antagonist		neurology/psychiatry	muscle pain
orteronel	Phase 3	androgen biosynthesis inhibitor|androgen receptor antagonist|cytochrome P450 inhibitor	CYP17A1		
ORY-1001	Phase 1/Phase 2	histone lysine demethylase inhibitor	KDM1A		
oseltamivir-carboxylate	Launched	neuraminidase inhibitor		infectious disease	influenza A virus infection
oseltamivir-phosphate	Launched	neuraminidase inhibitor	CES1|NEU1|NEU2	infectious disease	influenza A virus infection
osemozotan	Phase 2/Phase 3	serotonin receptor agonist	HTR1A		
OSI-027	Phase 1	mTOR inhibitor	MTOR		
OSI-420	Preclinical	EGFR inhibitor	EGFR		
OSI-930	Phase 1	KIT inhibitor|VEGFR inhibitor	FLT1|KDR|KIT		
osilodrostat	Launched	cytochrome P450 inhibitor			
osimertinib	Launched	EGFR inhibitor	EGFR	oncology	non-small cell lung cancer (NSCLC)
ospemifene	Launched	selective estrogen receptor modulator (SERM)	ESR1|ESR2	obstetrics/gynecology|endocrinology	vaginal atrophy|dyspareunia|menopause
ostarine	Phase 3	androgen receptor modulator	AR		
osthol	Preclinical	calcium channel blocker			
OT-R-antagonist-1	Preclinical	oxytocin receptor antagonist	AVPR1A|OXTR		
otamixaban	Phase 3	coagulation factor inhibitor	F10		
otenzepad	Phase 3	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5		
otilonium	Launched	acetylcholine receptor antagonist	CACNA1C	gastroenterology	irritable bowel syndrome
OTS167	Phase 1/Phase 2	maternal embryonic leucine zipper kinase inhibitor	MELK		
OTS514	Preclinical	TOPK inhibitor			
OTX015	Phase 1/Phase 2	bromodomain inhibitor	BRD2|BRD3|BRD4		
ouabain	Launched	ATPase inhibitor	ATP1A1	cardiology	hypertension|cardiac arrythmia
OXA-06	Preclinical	rho associated kinase inhibitor	ROCK1|ROCK2		
oxaceprol	Preclinical	anti-inflammatory agent			
oxacillin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	staphylococcal infections
oxacyclohexadecan-2-one	Preclinical	protein kinase inhibitor			
oxaliplatin	Launched	DNA inhibitor		oncology	colorectal cancer
oxaloacetate	Phase 2/Phase 3	glutamate release inhibitor			
oxantel	Launched	anthelmintic agent		infectious disease	gastrointestinal parasites
oxaprozin	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	rheumatology	osteoarthritis|rheumatoid arthritis
oxatomide	Launched	histamine receptor antagonist	HRH1	allergy	allergic rhinitis
oxcarbazepine	Launched	sodium channel blocker	SCN10A|SCN11A|SCN1A|SCN2A|SCN3A|SCN4A|SCN5A|SCN7A|SCN8A|SCN9A	neurology/psychiatry	seizures
oxelaidin	Launched	antitussive		pulmonary	cough suppressant
oxethazaine	Launched	local anesthetic		neurology/psychiatry	local anesthetic
OXF-BD-02	Preclinical	bromodomain inhibitor	BRD4		
oxfendazole	Launched	anthelmintic agent		infectious disease	lungworms|tapeworm|gastrointestinal roundworms
oxfenicine	Phase 1	carnitine palmitoyltransferase inhibitor	CPT1A|CPT1B		
oxibendazole	Launched	tubulin polymerization inhibitor	TUBB|TUBB4B	infectious disease	strongyles
oxiconazole	Launched	bacterial cell wall synthesis inhibitor		infectious disease	tinea pedis|tinea cruris|tinea corporis
oxidopamine	Preclinical	neurotoxin			
oxiniacic-acid	Preclinical				
oxiperomide	Phase 2	dopamine receptor antagonist			
oxiracetam	Launched	acetylcholine receptor agonist		neurology/psychiatry	senile dementia
oxolamine	Launched	antitussive		pulmonary	cough suppressant
oxolinic-acid	Preclinical	bacterial DNA gyrase inhibitor			
oxonic-acid	Preclinical	uricase inhibitor			
oxotremorine-M	Preclinical	acetylcholine receptor agonist	CHRM1|CHRM2|CHRM3|CHRM4		
oxotremorine-sesquifumarate	Preclinical	cholinergic receptor agonist	CHRM1|CHRM2|CHRM3|CHRM4		
oxprenolol	Launched	adrenergic receptor antagonist	ADRB1	cardiology	angina pectoris|hypertension|cardiac arrythmia
oxybenzone	Launched	lipase inhibitor	LIPE	dermatology	sunscreen lotion
oxybuprocaine	Launched	local anesthetic	SCN10A	neurology/psychiatry	local anesthetic
oxybutynin	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3	urology	urinary incontinence
oxyclozanide	Launched			infectious disease	fascioliasis
oxyfedrine	Launched	adrenergic receptor agonist		cardiology	angina pectoris
oxymatrine	Launched				
oxymetazoline	Launched	adrenergic receptor agonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|HTR1B|HTR1D|HTR2C	otolaryngology	nasal congestion
oxyphenbutazone	Withdrawn	cyclooxygenase inhibitor			
oxyphencyclimine	Launched	cholinergic receptor antagonist		gastroenterology	peptic ulcer disease (PUD)
oxyphenonium	Launched	cholinergic receptor antagonist	CHRM1|CHRM3	gastroenterology	peptic ulcer disease (PUD)
oxypurinol	Phase 2/Phase 3	xanthine oxidase inhibitor	XDH		
oxyquinoline	Launched	chelating agent	METAP2	dermatology	cosmetic
oxytetracycline	Launched	bacterial 30S ribosomal subunit inhibitor		infectious disease|urology	chlamydia|urinary tract infections|skin infections|ear infections|gonorrhea|urethritis|Lyme disease
oxytocin	Launched	oxytocin receptor agonist	AVPR1A|AVPR1B|AVPR2|OXTR	obstetrics/gynecology	labor induction
ozagrel	Launched	thromboxane synthase inhibitor	TBXAS1	neurology/psychiatry	stroke
ozanimod	Phase 3	sphingosine 1-phosphate receptor agonist	S1PR1		
ozenoxacin	Phase 3	antiinfective drug			
ozolinone	Phase 3	diuretic			
O4I1	Preclinical	Oct inducer	POU5F1		
O6-benzylguanine	Phase 3	O6-alkylguanine-DNA alkyltransferase inhibitor	MGMT		
p-dimethylinamyl-benzoate	Preclinical				
PA-452	Preclinical	retinoid receptor antagonist	RXRA		
PAC-1	Phase 1	caspase activator	CASP3		
paclitaxel	Launched	tubulin polymerization inhibitor	BCL2|MAP2|MAP4|MAPT|NR1I2|TLR4|TUBA1A|TUBA1B|TUBA1C|TUBA3C|TUBA3D|TUBA3E|TUBA4A|TUBB|TUBB1|TUBB2A|TUBB2B|TUBB3|TUBB4A|TUBB4B|TUBB6|TUBB8	oncology	ovarian cancer|breast cancer|non-small cell lung cancer (NSCLC)
PACOCF3	Preclinical	phospholipase inhibitor	PLA2G4A		
pacritinib	Phase 3	FLT3 inhibitor|JAK inhibitor	FLT3|JAK1|JAK2|JAK3		
padsevonil	Phase 3	antiepileptic			
paeoniflorin	Preclinical	anticonvulsant			
paeonol	Preclinical	anti-inflammatory agent			
pafuramidine	Phase 3	DNA synthesis inhibitor			
pagoclone	Phase 2/Phase 3	GABA receptor agonist			
palbociclib	Launched	CDK inhibitor	CDK4|CDK6	oncology	breast cancer
palifosfamide	Phase 3	DNA alkylating agent			
paliperidone	Launched	dopamine receptor antagonist|serotonin receptor antagonist	DRD2|HTR2A	neurology/psychiatry	schizophrenia
palmatine-chloride	Preclinical	dopamine synthesis inhibitor	CYP3A4		
palmitoleic-acid	Preclinical				
palmitoylcarnitine	Preclinical	protein kinase inhibitor			
palmitoylethanolamide	Launched	cannabinoid receptor agonist	CNR2|GPR119|GPR55		
palomid-529	Phase 1	AKT inhibitor|mTOR inhibitor	MTOR		
palonosetron	Launched	serotonin receptor antagonist	HTR3A	gastroenterology	nausea|vomiting
palosuran	Phase 2	urotensin receptor antagonist	UTS2R		
palovarotene	Phase 3	retinoid receptor agonist	RARG		
pamabrom	Launched	diuretic		gastroenterology	bloating
pamidronate	Launched	bone resorption inhibitor	FDPS	endocrinology|oncology|hematologic malignancy	hypercalcemia|Paget's disease|breast cancer|multiple myeloma
pamiparib	Phase 3	PARP inhibitor			
pancuronium	Launched	acetylcholine receptor antagonist	CHRM2|CHRM3|CHRNA1|CHRNA2	critical care|neurology/psychiatry	endotracheal intubation|muscle relaxant
panipenem	Preclinical	antibacterial 			
panobinostat	Launched	HDAC inhibitor	HDAC1|HDAC2|HDAC3|HDAC4|HDAC6|HDAC7|HDAC8|HDAC9	hematologic malignancy	multiple myeloma
pantethine	Launched	coenzyme A precursor			
pantoprazole	Launched	ATPase inhibitor	ATP4A	gastroenterology	gastroesophageal reflux disease (GERD)|erosive esophagitis (EE)|Zollinger-Ellison syndrome
pantothenic-acid	Launched	coenzyme A precursor			
PAOPA	Preclinical	dopamine receptor modulator	DRD2		
papaverine	Launched	phosphodiesterase inhibitor	PDE10A|PDE4B|PDE5A	cardiology|hematology|gastroenterology	myocardial infarction|angina pectoris|pulmonary embolism (PE)|colitis|vascular spasm
paquinimod	Phase 2	S100A9 inhibitor			
para-toluenesulfonamide	Phase 3		CA12|CA2|CA6|CA9		
paracetamol	Launched	cyclooxygenase inhibitor	FAAH|PTGS1|PTGS2|TRPV1	neurology/psychiatry|endocrinology	pain relief|fever
parachlorophenol	Launched	antiinfective drug		infectious disease	first-aid antiseptic
paramethadione	Launched	anticonvulsant	CACNA1G	neurology/psychiatry	seizures
paraxanthine	Phase 1	adenosine receptor antagonist			
parbendazole	Preclinical	tubulin polymerization inhibitor	TUBB		
parcetasal	Preclinical	anti-inflammatory agent			
pardoprunox	Phase 3	dopamine receptor agonist|serotonin receptor agonist	DRD2|DRD3|DRD4|HTR1A|HTR7		
parecoxib	Launched	cyclooxygenase inhibitor	LTF	neurology/psychiatry	pain relief
parethoxycaine	Preclinical	local anesthetic			
pargyline	Launched	monoamine oxidase inhibitor	MAOA|MAOB	cardiology	hypertension
paricalcitol	Launched	vitamin D receptor agonist	VDR	nephrology|endocrinology	chronic kidney disease (CKD)|hyperthyroidism
paritaprevir	Launched	HCV inhibitor		infectious disease	hepatitis C
paromomycin	Launched	bacterial 30S ribosomal subunit inhibitor		infectious disease	amebiasis
paroxetine	Launched	selective serotonin reuptake inhibitor (SSRI)	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|HTR2A|SLC6A2|SLC6A4	neurology/psychiatry	depression|obsessive compulsive disorder (OCD)|generalized anxiety disorder (GAD)|panic disorders|posttraumatic stress disorder|social anxiety disorder
paroxypropione	Launched	gonadotropin inhibitor			
parsaclisib	Phase 2	PI3K inhibitor			
parthenolide	Phase 1	NFkB pathway inhibitor			
parthenolide-(-)	Preclinical	NFkB pathway inhibitor	HDAC1		
parthenolide-(alternate-stereo)	Preclinical	NFkB pathway inhibitor	IKBKB|RELA		
pasireotide	Launched	somatostatin receptor agonist	SSTR1|SSTR2|SSTR3|SSTR5	endocrinology	Cushing's syndrome|acromegaly
PAT-1251	Phase 1	lysyl oxidase inhibitor			
pavinetant	Phase 2	neurokinin receptor antagonist			
pazopanib	Launched	KIT inhibitor|PDGFR tyrosine kinase receptor inhibitor|VEGFR inhibitor	CSF1R|FGF1|FGFR1|FGFR3|FLT1|FLT4|ITK|KDR|KIT|PDGFRA|PDGFRB|SH2B3	oncology	renal cell carcinoma (RCC)|soft tissue sarcoma (STS)
pazufloxacin	Launched	topoisomerase inhibitor		infectious disease	pneumonia|peritonitis|bacterial septicemia
PBI-4050	Phase 2/Phase 3	free fatty acid receptor agonist			
PBT-1033	Preclinical	chelating agent			
PCA-4248	Phase 1	platelet activating factor receptor antagonist	PTAFR		
PCI-24781	Phase 3	HDAC inhibitor	HDAC1|HDAC2|HDAC3|HDAC6		
PCI-27483	Phase 2	ERK1 and ERK2 phosphorylation inhibitor			
PCI-29732	Preclinical	Bruton's tyrosine kinase (BTK) inhibitor	BTK		
PCI-34051	Preclinical	HDAC inhibitor	HDAC1|HDAC10|HDAC6|HDAC8		
PCO-400	Phase 1	potassium channel activator	KCNJ8		
PD-0325901	Phase 2	MEK inhibitor	MAP2K1		
PD-102807	Preclinical	acetylcholine receptor antagonist	CHRM4		
PD-118057	Preclinical	potassium channel activator	KCNH2		
PD-123319	Phase 1	angiotensin antagonist	AGTR2		
PD-128907	Preclinical	dopamine receptor agonist	DRD2|DRD3		
PD-153035	Phase 1	EGFR inhibitor	EGFR|KDR		
PD-156707	Preclinical	endothelin receptor antagonist	EDNRA|EDNRB		
PD-158780	Preclinical	EGFR inhibitor	EGFR		
PD-160170	Preclinical	neuropeptide receptor antagonist	NPY1R		
PD-161570	Preclinical	FGFR inhibitor	FGFR1		
PD-166285	Preclinical	SRC inhibitor	EGFR|FGFR1|PDGFRB|PKMYT1|SRC|WEE1		
PD-166793	Preclinical	collagenase inhibitor|metalloproteinase inhibitor	MMP13|MMP2|MMP3		
PD-168077	Preclinical	dopamine receptor agonist	DRD2		
PD-168393	Preclinical	EGFR inhibitor	EGFR|ERBB2|SRC		
PD-168568	Preclinical	dopamine receptor antagonist	DRD2|DRD4		
PD-173074	Preclinical	FGFR inhibitor|VEGFR inhibitor	FGFR1|FGFR2|FGFR3|FGFR4|FLT1|FLT4|KDR|PDGFRA|PDGFRB		
PD-173212	Preclinical	calcium channel blocker	CACNA1B		
PD-184352	Phase 2	MEK inhibitor	MAP2K1|MAP3K1|MAP3K2		
PD-198306	Preclinical	MAP kinase inhibitor|MEK inhibitor	MAP2K1|MAP2K2		
PD-318088	Preclinical	MEK inhibitor			
PD-407824	Preclinical	PKC inhibitor	WEE1		
PD-81723	Preclinical	adenosine receptor agonist	ADORA1		
PD-98059	Preclinical	MEK inhibitor	AKT1|CHEK1|GSK3B|LCK|MAP2K1|MAPK1|MAPK11|MAPK12|MAPK14|MAPK8|PRKCA|RAF1|ROCK1|RPS6KB1|SGK1		
PDD-00017273	Preclinical	PARG inhibitor			
PDE10-IN-1	Preclinical	phosphodiesterase inhibitor	PDE10A		
PDP-EA	Preclinical	FAAH activator	FAAH		
PD1-PDL-inhibitor-1	Preclinical	programmed death ligand inhibitor	CD274		
peficitinib	Launched	JAK inhibitor	JAK1|JAK2|JAK3	rheumatology	rheumatoid arthritis
pefloxacin	Launched	bacterial DNA gyrase inhibitor	TOP2A	infectious disease|urology	gastrointestinal infections|urethritis|gonorrhea|urinary tract infections
pelanserin	Phase 2	serotonin receptor antagonist	HTR2A		
pelitinib	Phase 2	EGFR inhibitor	EGFR		
pelrinone	Phase 2	phosphodiesterase inhibitor			
pemafibrate	Phase 3	PPAR receptor agonist			
pemetrexed	Launched	dihydrofolate reductase inhibitor|thymidylate synthase inhibitor	ATIC|DHFR|GART|TYMS	oncology	non-small cell lung cancer (NSCLC)|mesothelioma
pemirolast	Launched	mediator release inhibitor	HRH1	pulmonary	asthma
pempidine	Launched	ganglionic blocker		cardiology	hypertension
penbutolol	Launched	adrenergic receptor antagonist	ADRB1|ADRB2|HTR1A|HTR1B	cardiology	hypertension
penciclovir	Launched	DNA directed DNA polymerase inhibitor		dental	cold sore
penfluridol	Launched	T-type calcium channel blocker	CACNA1G	neurology/psychiatry	schizophrenia
penicillamine-(D)	Launched	chelating agent		metabolism|rheumatology|nephrology	Wilson's disease|rheumatoid arthritis|cystinuria
penicillamine-(racemic)	Launched				
penicillin-v-potassium	Launched	bacterial cell wall synthesis inhibitor		infectious disease	pneumonia|ear infections|skin infections|throat infections|cholera|scarlet fever
pentacosanoic-acid	Preclinical				
pentagastrin	Launched	CCK receptor agonist	CCKBR	gastroenterology	anacidity diagnostic|gastric hypersecretion diagnostic
pentamidine	Launched	anti-pneumocystis agent	TRDMT1	infectious disease	pneumonia
pentetic-acid	Phase 2	chelating agent			
pentolinium	Launched	cholinergic receptor antagonist	CHRNA10|CHRNA3|CHRNA4|CHRNB4	cardiology	hypertension
pentostatin	Launched	adenosine deaminase inhibitor|ribonucleotide reductase inhibitor	ADA	hematologic malignancy	hairy cell leukemia
pentoxifylline	Launched	phosphodiesterase inhibitor	ADORA1|ADORA2A|ADORA2B|ADRA2B|NT5E|PDE10A|PDE1A|PDE1B|PDE1C|PDE2A|PDE3A|PDE3B|PDE4A|PDE4B|PDE4C|PDE4D|PDE5A|PDE6A|PDE6B|PDE6C|PDE6D|PDE6G|PDE6H|PDE7A|PDE7B|PDE8A|PDE8B|PDE9A|TNF	cardiology	claudication
pentylenetetrazol	Withdrawn	GABA receptor antagonist			
peposertib	Phase 1/Phase 2	DNA dependent protein kinase inhibitor			
pepstatin	Preclinical	aspartic protease inhibitor	CTSB|CTSD|CTSL|REN		
peramivir	Launched	neuraminidase inhibitor		infectious disease	influenza A virus infection
perchlozone	Launched			infectious disease	tuberculosis
peretinoin	Phase 3	retinoid receptor agonist	RXRA		
perfluamine	Launched				
perflubron	Launched	contrast agent		radiology	contrast agent
perfluorodecalin	Launched			dermatology	cosmetic
perfluorohexyloctane	Launched				
pergolide	Withdrawn	dopamine receptor agonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|DRD1|DRD2|DRD3|DRD4|DRD5|HTR1A|HTR1B|HTR1D|HTR2A|HTR2B|HTR2C		
perhexiline	Launched	carnitine palmitoyltransferase inhibitor	CPT1A	cardiology	angina pectoris
perifosine	Phase 3	AKT inhibitor	AKT1		
perillyl-alcohol	Phase 2	apoptosis stimulant|farnesyltransferase inhibitor	FNTA		
perindopril	Launched	angiotensin converting enzyme inhibitor	ACE	cardiology	hypertension|myocardial infarction|coronary artery disease (CAD)
perindoprilat	Phase 2	angiotensin converting enzyme inhibitor	ACE		
permethrin	Launched			infectious disease	lice
perospirone	Launched	dopamine receptor antagonist|serotonin receptor antagonist	DRD2|DRD3|DRD4	neurology/psychiatry	schizophrenia|bipolar disorder
perphenazine	Launched	dopamine receptor antagonist	CALM1|DRD1|DRD2|HRH1|HTR2A|HTR2C|HTR6|HTR7	neurology/psychiatry|gastroenterology	schizophrenia|nausea|vomiting
peruvoside	Phase 1	cardiac glycoside			
perzinfotel	Phase 2	glutamate receptor antagonist	GRIN1|GRIN2A|GRIN2B		
PETCM	Preclinical	caspase activator	CASP3		
pevonedistat	Phase 3	nedd activating enzyme inhibitor	NAE1|UBA3		
pexidartinib	Launched	tyrosine kinase inhibitor	CSF1R|FLT3|KIT		
pexmetinib	Phase 1	MAP kinase inhibitor|TIE tyrosine kinase inhibitor	MAPK14|TEK		
PF-02413873	Phase 1	progesterone receptor antagonist			
PF-02545920	Phase 2	phosphodiesterase inhibitor	PDE10A		
PF-03049423	Phase 2	phosphodiesterase inhibitor	PDE5A		
PF-03084014	Phase 3	gamma secretase inhibitor			
PF-03758309	Phase 1	p21 activated kinase inhibitor	PAK4		
PF-03814735	Phase 1	Aurora kinase inhibitor	AURKA|AURKB		
PF-03882845	Phase 1	mineralocorticoid receptor antagonist			
PF-04136309	Phase 2	CC chemokine receptor antagonist			
PF-04217903	Phase 1	c-Met inhibitor	MET		
PF-04418948	Phase 1	prostaglandin inhibitor	PTGER2		
PF-04447943	Phase 2	phosphodiesterase inhibitor	PDE9A		
PF-04457845	Phase 2	FAAH inhibitor	FAAH		
PF-04620110	Phase 1	diacylglycerol O acyltransferase inhibitor	DGAT1		
PF-04691502	Phase 2	mTOR inhibitor|PI3K inhibitor	MTOR|PIK3CA		
PF-04885614	Preclinical	voltage-gated sodium channel blocker	SCN10A		
PF-04937319	Phase 2	glucokinase activator	GCK		
PF-04995274	Phase 1	serotonin receptor agonist			
PF-05089771	Preclinical	sodium channel blocker			
PF-05175157	Phase 2	acetyl-CoA carboxylase inhibitor			
PF-05180999	Phase 1	phosphodiesterase inhibitor			
PF-05190457	Phase 2	growth hormone secretagogue receptor inverse agonist	GHSR		
PF-05212384	Phase 2	mTOR inhibitor|PI3K inhibitor	MTOR|PIK3CA		
PF-06260414	Phase 1	androgen receptor modulator			
PF-06273340	Phase 1	tyrosine kinase receptor inhibitor			
PF-06282999	Phase 1	myeloperoxidase inhibitor			
PF-06305591	Phase 1	sodium channel blocker			
PF-06409577	Phase 1	protein kinase activator			
PF-06412562	Phase 1	dopamine receptor partial agonist			
PF-06447475	Preclinical	serine/threonine kinase inhibitor	LRRK2		
PF-06459988	Phase 2	receptor tyrosine protein kinase inhibitor			
PF-06463922	Launched	ALK tyrosine kinase receptor inhibitor	ALK|FES|ROS1	oncology	non-small cell lung cancer (NSCLC)
PF-06650833	Phase 1	kinase inhibitor			
PF-06651600	Phase 2/Phase 3	JAK inhibitor			
PF-06747775	Phase 2	EGFR inhibitor			
PF-06751979	Phase 1	beta secretase inhibitor			
PF-06840003	Phase 1	"indoleamine 2,3-dioxygenase inhibitor"			
PF-06873600	Phase 2	CDK inhibitor			
PF-06928215	Preclinical	cyclic GMP-AMP synthase inhibitor			
PF-3274167	Phase 2	oxytocin receptor antagonist	AVPR1A|OXTR		
PF-3845	Preclinical	FAAH inhibitor	FAAH		
PF-4191834	Preclinical	lipoxygenase inhibitor			
PF-429242	Preclinical	SREBP inhibitor	MBTPS1		
PF-431396	Preclinical	focal adhesion kinase inhibitor	PTK2|PTK2B		
PF-4708671	Preclinical	ribosomal protein inhibitor	RPS6KB1		
PF-477736	Phase 1	CHK inhibitor	CHEK1|CHEK2		
PF-4800567	Preclinical	casein kinase inhibitor	CSNK1D|CSNK1E		
PF-4981517	Preclinical	cytochrome P450 inhibitor	CYP3A4		
PF-514273	Preclinical	cannabinoid receptor antagonist			
PF-5274857	Preclinical	smoothened receptor antagonist	SMO		
PF-562271	Phase 1	focal adhesion kinase inhibitor	PTK2|PTK2B		
PF-573228	Preclinical	focal adhesion kinase inhibitor	CDK1|CDK2|CDK7|GSK3B|IKBKB		
PF-670462	Preclinical	casein kinase inhibitor	CSNK1D|CSNK1E		
PF-750	Preclinical	FAAH inhibitor	FAAH		
PF-8380	Preclinical	autotaxin inhibitor	ENPP2		
PF-915275	Phase 1	11-beta hydroxysteroid dehydrogenase inhibitor	HSD11B1		
PFI-1	Preclinical	bromodomain inhibitor	BRD4		
PFI-3	Preclinical	bromodomain inhibitor	PBRM1|SMARCA4		
PFI-4	Preclinical	bromodomain inhibitor	BRPF1		
PFK-015	Phase 1	phosphofructokinase inhibitor	PFKFB3		
PFK-158	Phase 1	phosphofructokinase inhibitor	PFKFB3		
PG-9	Preclinical	acetylcholine receptor agonist			
PGL5001	Phase 2	JNK inhibitor	MAPK10|MAPK8|MAPK9		
PH-797804	Phase 2	p38 MAPK inhibitor	MAPK11|MAPK14		
PHA-543613	Preclinical	nicotinic receptor agonist			
PHA-568487	Preclinical	nicotinic receptor agonist	CHRNA7		
PHA-665752	Preclinical	c-Met inhibitor	MET		
PHA-680632	Preclinical	Aurora kinase inhibitor	AURKA|AURKB|AURKC		
PHA-767491	Preclinical	CDC inhibitor	CDK1|RPS6KB1		
PHA-793887	Phase 1	CDK inhibitor	CDK1|CDK2|CDK4|CDK5|CDK7|CDK9		
PHA-848125	Phase 2	CDK inhibitor|growth factor receptor inhibitor	CDK2|CDK4|CDK7|NTRK1		
PHCCC	Preclinical	glutamate receptor agonist	GRM1|GRM4		
phenacaine	Launched	local anesthetic		neurology/psychiatry	local anesthetic
phenacemide	Launched	sodium channel blocker	SCN10A|SCN11A|SCN1A|SCN2A|SCN3A|SCN4A|SCN5A|SCN7A|SCN8A|SCN9A	neurology/psychiatry	epilepsy|seizures
phenacetin	Withdrawn	cyclooxygenase inhibitor	PTGS1		
phenazone	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	neurology/psychiatry	pain relief
phenazopyridine	Launched	local anesthetic	SCN1A	infectious disease	urinary tract infections
phenelzine	Launched	monoamine oxidase inhibitor	ABAT|AOC3|GAD2|GPT|GPT2|MAOA|MAOB|SLC6A2|SLC6A3|SLC6A4	neurology/psychiatry	depression
phenethicillin	Launched	bacterial cell wall synthesis inhibitor			
phenethyl-isothiocyanate	Phase 2	anticancer agent	CYP2E1		
phenformin	Withdrawn	AMPK activator	KCNJ8|PRKAA1		
phenindamine	Launched	histamine receptor antagonist	HRH1	allergy|otolaryngology	allergic rhinitis|common cold
phenindione	Launched	vitamin K antagonist	VKORC1	hematology	deep vein thrombosis (DVT)
pheniramine	Launched	histamine receptor antagonist	HRH1	allergy	allergic rhinitis|urticaria
phenol	Preclinical		CA1|CA12|CA14|CA2|CA4|CA9	otolaryngology	pharyngitis
phenolphthalein	Withdrawn	indicator dye	UGT1A9		
phenolsulfonphthalein	Launched				
phenothiazine	Preclinical	dopamine receptor antagonist			
phenothrin	Launched			infectious disease	lice
phenoxybenzamine	Launched	adrenergic receptor antagonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C	cardiology|endocrinology	hypertension|pheochromocytoma
phenprobamate	Launched	muscle relaxant		neurology/psychiatry	anxiety|muscle relaxant
phenprocoumon	Launched	vitamin K antagonist	VKORC1	hematology	thrombosis|pulmonary embolism (PE)
phenserine	Phase 3	acetylcholinesterase inhibitor|beta amyloid synthesis inhibitor	ACHE|BCHE		
phensuximide	Launched	succinimide antiepileptic		neurology/psychiatry	seizures
phentolamine	Launched	adrenergic receptor antagonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C	endocrinology|cardiology	pheochromocytoma|hypertension
phenyl-aminosalicylate	Launched			infectious disease	tuberculosis
phenyl-salicylate	Launched	antiseptic		urology	interstitial cystitis (IC)
phenylacetylglutamine	Phase 2	DNA methylase inhibitor|protein synthesis inhibitor			
phenylbenzimidazole-sulfonic-acid	Launched			dermatology	sunscreen lotion
phenylbutazone	Withdrawn	cyclooxygenase inhibitor|prostanoid receptor antagonist	PTGIS|PTGS1|PTGS2		
phenylbutyrate	Launched	HDAC inhibitor	HDAC1	metabolism	urea cycle disorders
phenylephrine	Launched	adrenergic receptor agonist	ADRA1A|ADRA1B|ADRA1D	otolaryngology|gastroenterology|cardiology	nasal congestion|hemorrhoids|hypotension
phenylethyl-alcohol	Preclinical				
phenylmercuric-acetate	Preclinical	other antifungal			
phenylmethylsulfonyl-fluoride	Preclinical	serine protease inhibitor			
phenylpiracetam	Launched	noradrenaline uptake inhibitor		neurology/psychiatry	anxiety|fatigue|depression
phenytoin	Launched	hydantoin antiepileptic	SCN10A|SCN11A|SCN1A|SCN2A|SCN3A|SCN4A|SCN5A|SCN7A|SCN8A|SCN9A	neurology/psychiatry	seizures
PhiKan-083	Preclinical	p53 stabilizing agent	TP53		
phloretin	Launched	sodium/glucose cotransporter inhibitor	AQP9|CLCN3|SLC23A1		
phlorizin	Preclinical	sodium/glucose cotransporter inhibitor	SLC5A1|SLC5A11|SLC5A2|SLC5A3		
phloroglucin	Launched			neurology/psychiatry	spasms
phortress	Phase 1	aryl hydrocarbon receptor ligand	AHR		
phosphatidylcholine	Launched			infectious disease|dermatology|gastroenterology|cardiology|obstetrics/gynecology	hepatitis B|hepatitis C|eczema|gallbladder disease|cholesterol|premenstrual syndrome
PHP-501	Preclinical	GABA receptor antagonist	GABRA1|GABRB2|GABRG2		
PHT-427	Preclinical	AKT inhibitor|pyruvate dehydrogenase inhibitor	AKT2|PDPK1		
phthalylsulfacetamide	Preclinical				
phthalylsulfathiazole	Launched	dihydropteroate synthetase inhibitor		infectious disease|gastroenterology	dysentry|colitis
PHTPP	Preclinical	estrogen receptor antagonist	ESR2		
physostigmine	Launched	acetylcholinesterase inhibitor|cholinesterase inhibitor	ACHE|BCHE	cardiology|neurology/psychiatry|ophthalmology|gastroenterology	hypotension|Alzheimer's disease|glaucoma|gastroparesis
phytonadione	Launched		BGLAP|GGCX	hematology	vitamin K deficiency|anticoagulation reversal
phytosphingosine	Phase 1				
PI-103	Preclinical	mTOR inhibitor|PI3K inhibitor	MTOR|PIK3CA|PIK3CB|PIK3CD|PIK3CG|PRKDC		
PI-828	Preclinical	PI3K inhibitor			
pibenzimol	Phase 2	DNA inhibitor			
piboserod	Phase 2	serotonin receptor antagonist	HTR2B|HTR4		
picartamide	Phase 2	H+/K+-ATPase inhibitor	ATP4A		
piceatannol	Preclinical	SYK inhibitor	ATP5A1|ATP5B|ATP5C1|IRF3		
piclamilast	Phase 2	phosphodiesterase inhibitor	PDE4A|PDE4B|PDE4C|PDE4D		
picolamine	Preclinical				
picolinic-acid	Phase 2	chelating agent			
piconol	Preclinical				
picotamide	Launched	thromboxane receptor antagonist|thromboxane synthase inhibitor	TBXA2R	hematology	thrombosis
picrotin	Phase 2	GABA receptor antagonist	GLRA1|GLRA2|GLRA3|GLRB		
picrotoxinin	Preclinical	GABA receptor antagonist	GLRA1|GLRA2|GLRA3|GLRB|HTR3A|HTR3B		
pidolic-acid	Launched		ADAM28|AMY1A|AMY2A|AMY2B|ANG|CCL8|HCRT|IGLC1|KRTAP5-2|TFF2|VEGFA	dermatology	xerosis cutis
pidotimod	Launched	interferon receptor agonist|interleukin receptor agonist		infectious disease	immune adjuvant
pifithrin-alpha	Preclinical	TP53 inhibitor	TP53		
pifithrin-cyclic	Preclinical	TP53 inhibitor	TP53		
pifithrin-mu	Preclinical	HSP inhibitor	HSPA1A|TP53		
PIK-293	Preclinical	PI3K inhibitor	PIK3CA|PIK3CB|PIK3CD|PIK3CG		
PIK-294	Preclinical	PI3K inhibitor	PIK3CB|PIK3CD|PIK3CG		
PIK-75	Preclinical	DNA protein kinase inhibitor|PI3K inhibitor	PIK3CA|PIK3CB|PIK3CD|PIK3CG|PRKDC		
PIK-93	Preclinical	PI3K inhibitor	PI4KB|PIK3C3|PIK3CG		
pikamilone	Phase 1				
piketoprofen	Launched	cyclooxygenase inhibitor		neurology/psychiatry	pain relief
pilaralisib	Phase 2	PI3K inhibitor			
pilocarpine	Launched	acetylcholine receptor agonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5	ophthalmology|cardiology	glaucoma|hypertension
pilsicainide	Launched	sodium channel blocker	SCN5A	cardiology	cardiac arrythmia
PIM-1-Inhibitor-2	Preclinical	Pim kinase inhibitor	PIM1		
PIM-447	Phase 1	Pim kinase inhibitor			
pimavanserin	Launched	serotonin receptor inverse agonist	DRD2|HTR2A	neurology/psychiatry	Parkinson's Disease
pimecrolimus	Launched	calcineurin inhibitor		dermatology	eczema
pimethixene	Launched	antihistamine		neurology/psychiatry|allergy	attention-deficit/hyperactivity disorder (ADHD)|anxiety|sleep cycle support|allergic rhinitis
pimobendan	Launched	calcium sensitizer|phosphodiesterase inhibitor	PDE3A	cardiology	congestive heart failure
pimodivir	Phase 3	antiviral			
pimonidazole	Phase 3				
pimozide	Launched	dopamine receptor antagonist	CACNA1I|CALM1|DRD1|DRD2|DRD3|DRD4|DRD5|HRH1|HTR1A|HTR2A|KCNA10|KCNH2	neurology/psychiatry	Tourette's disorder
pinacidil	Launched	ATP channel activator|potassium channel activator	ABCC8|ABCC9	cardiology	hypertension
pinanediol	Preclinical				
pinaverium	Launched	T-type calcium channel blocker	CACNA1C	gastroenterology	irritable bowel syndrome
pincainide	Phase 1	antiarrhythmic			
pindolol	Launched	adrenergic receptor antagonist	ADRB1|ADRB2|HTR1A|HTR2A|HTR2B	cardiology	hypertension
pindolol-(-)	Phase 2	adrenergic receptor antagonist|serotonin receptor antagonist	HTR1A		
pinitol	Phase 2	gamma secretase inhibitor			
pinocembrin	Phase 2	cytochrome P450 inhibitor	CYP1B1		
pioglitazone	Launched	insulin sensitizer|PPAR receptor agonist	PPARG|TRPM3	endocrinology	diabetes mellitus
pipamperone	Launched	dopamine receptor antagonist	DRD2|HRH1|HTR1A|HTR1B|HTR1D|HTR2A	neurology/psychiatry	schizophrenia
pipecuronium	Launched	neuromuscular blocker	CHRM2|CHRM3|CHRNA2	neurology/psychiatry	anesthetic
pipemidic-acid	Launched	topoisomerase inhibitor		infectious disease	gram-negative bacterial infections
pipenzolate	Launched	cholinergic receptor antagonist	CHRM1	neurology/psychiatry	spasms
piperacetazine	Launched	dopamine receptor antagonist		neurology/psychiatry	schizophrenia
piperacillin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	intra-abdominal infections|skin infections|pelvic inflammatory disease|pneumonia
piperaquine-phosphate	Launched	antimalarial agent		infectious disease	malaria
piperazine	Launched	benzodiazepine receptor agonist	GABRB3	infectious disease	gastrointestinal roundworms
piperazinedione	Phase 2	DNA synthesis inhibitor			
piperidolate	Launched	acetylcholine receptor antagonist	CHRM1	neurology/psychiatry	spasms
piperine	Phase 1	monoamine oxidase inhibitor	MAOA|MAOB|TRPV1		
piperonyl-butoxide	Launched	cytochrome P450 inhibitor		infectious disease	lice
pipobroman	Launched	DNA alkylating agent		hematology	polycythemia vera|thrombocythemia
pipofezine	Preclinical	selective serotonin reuptake inhibitor (SSRI)			
pipotiazine	Launched	dopamine receptor antagonist	DRD1|DRD2|HTR1A|HTR2A	neurology/psychiatry	schizophrenia
pipotiazine-palmitate	Launched	dopamine receptor antagonist|serotonin receptor antagonist	DRD1|DRD2|HTR1A|HTR2A	neurology/psychiatry	schizophrenia
piracetam	Launched	acetylcholine receptor agonist	GRIA1|GRIA2|GRIA3|GRIA4	neurology/psychiatry	senile dementia
pirarubicin	Launched	topoisomerase inhibitor	TOP2A	oncology	breast cancer
pirenoxine	Launched	AGE inhibitor		ophthalmology	cataracts
pirenperone	Preclinical	serotonin receptor antagonist	HTR2A|HTR7		
pirenzepine	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5	gastroenterology	peptic ulcer disease (PUD)
piretanide	Launched	glucocorticoid receptor agonist	SLC12A1|SLC12A2	cardiology	hypertension|edema
pirfenidone	Launched	TGF beta receptor inhibitor	FURIN|TNF	pulmonary	idiopathic pulmonary fibrosis (IPF)
piribedil	Launched	dopamine receptor agonist	ADRA1A|ADRA2A|ADRA2C|DRD2|DRD3|DRD4|HTR1A|HTR2B	neurology/psychiatry	Parkinson's Disease|dizziness
piricapiron	Phase 2	dopamine receptor antagonist|serotonin receptor antagonist	HTR2A		
pirinixic-acid	Preclinical	PPAR receptor agonist	PPARA		
pirlindole	Launched	monoamine oxidase inhibitor	MAOA	neurology/psychiatry	depression
pirmenol	Preclinical	acetylcholine receptor inhibitor			
piroctone-olamine	Launched			infectious disease	fungal infection
pirodavir	Phase 2				
piromidic-acid	Phase 2	bacterial DNA gyrase inhibitor			
piroxicam	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	rheumatology	osteoarthritis|rheumatoid arthritis
piroximone	Phase 2	phosphodiesterase inhibitor	PDE3A		
pirozadil	Preclinical	hypolipidemic			
pirquinozol	Phase 1	histamine release inhibitor			
PIT	Preclinical	purinergic receptor antagonist	P2RY1		
pitavastatin	Launched	HMGCR inhibitor	HMGCR	endocrinology	hyperlipidemia
pitolisant	Launched	histamine receptor antagonist	HRH3		
pivagabine	Launched	corticotropin releasing factor receptor antagonist	CRHR1|CRHR2	neurology/psychiatry	depression
pivampicillin	Launched	bacterial cell wall synthesis inhibitor		pulmonary|infectious disease	bronchitis|pneumonia|gynecologic infections
pivanex	Phase 2	HDAC inhibitor	HDAC1|HDAC2|HDAC3|HDAC8		
pivmecillinam	Launched	bacterial cell wall synthesis inhibitor		infectious disease	urinary tract infections|gram-negative bacterial infections
pixantrone	Launched	topoisomerase inhibitor	TOP2A	hematologic malignancy	non-Hodgkin lymphoma (NHL)
pizotifen	Launched	serotonin receptor antagonist	HTR1A|HTR2A|HTR2C	neurology/psychiatry	migraine headache
PI3K-IN-2	Phase 2	PI3K inhibitor			
PI3Kd-IN-2	Preclinical	PI3K inhibitor			
PI4KIII-beta-inhibitor-1	Preclinical	PI4K inhibitor	PI4K2B		
PJ-34	Preclinical	PARP inhibitor	EEF2|PARP1|PARP15|PARP3		
PK-THPP	Preclinical	potassium channel blocker	KCNK9		
PK-11195	Phase 1	benzodiazepine receptor antagonist	TSPO		
PK-44	Preclinical	dipeptidyl peptidase inhibitor	DPP4		
PKI-166	Phase 1	EGFR inhibitor	EGFR		
PKI-179	Phase 1	mTOR inhibitor|PI3K inhibitor	MTOR		
pleconaril	Phase 3				
plerixafor	Launched	CC chemokine receptor antagonist	ACKR3|CCR4|CXCR4	hematologic malignancy	non-Hodgkin lymphoma (NHL)|multiple myeloma
plicamycin	Launched	alcohol dehydrogenase inhibitor		oncology|endocrinology	testicular carcinoma|Paget's disease|hypercalcemia
plinabulin	Phase 3	tubulin polymerization inhibitor			
plovamer-acetate	Phase 2		TAT|TH|YARS|YARS2		
plumbagin	Preclinical	anticancer agent			
plurisin-1	Preclinical	stearoyl-CoA desaturase inhibitor	SCD		
PLX4720	Preclinical	RAF inhibitor	BRAF|KDR		
PLX51107	Phase 1	bromodomain inhibitor			
PLX647	Preclinical	receptor tyrosine protein kinase inhibitor	CSF1R|KIT		
PLX8394	Phase 1/Phase 2	serine/threonine kinase inhibitor	BRAF		
PMPA	Preclinical	glutamate receptor antagonist	FOLH1		
PNU-120596	Preclinical	acetylcholine receptor agonist	CHRNA7		
PNU-142633	Phase 2	serotonin receptor agonist	HTR1D		
PNU-177864	Preclinical	dopamine receptor antagonist	DRD3		
PNU-22394	Phase 2	serotonin receptor agonist	HTR2A|HTR2B|HTR2C|MAOA|MAOB		
PNU-282987	Preclinical	cholinergic receptor agonist	CHRNA7		
PNU-37883	Preclinical	ATP-sensitive potassium channel antagonist			
PNU-74654	Preclinical	beta-catenin inhibitor	CTNNB1|TCF4		
PNU-89843	Preclinical	benzodiazepine receptor agonist	GABBR1		
pocapavir	Preclinical	Enterovirus capsid inhibitor			
podophyllotoxin	Launched	microtubule inhibitor|tubulin polymerization inhibitor	IGF1R|TOP2A|TUBA4A|TUBB	infectious disease	genital warts
polaprezinc	Preclinical	chelating agent			
polidocanol	Launched	local anesthetic		dermatology	varicose veins
polydatin	Phase 2	ICAM1 expression inhibitor	ICAM1		
polyinosine	Preclinical	immunostimulant	HPRT1|IMPDH2|PYGM		
polymyxin-B-sulfate	Launched	bacterial permeability inducer		ophthalmology	eye infection
polythiazide	Launched	sodium/chloride cotransporter inhibitor	SLC12A3	cardiology|gastroenterology|rheumatology|nephrology	edema|congestive heart failure|hepatic cirrhosis|nephrotic syndrome|acute glomerulonephritis (AGN)|chronic renal failure|hypertension
pomalidomide	Launched	angiogenesis inhibitor|tumor necrosis factor production inhibitor		hematologic malignancy	multiple myeloma
ponatinib	Launched	Bcr-Abl kinase inhibitor|FLT3 inhibitor|PDGFR tyrosine kinase receptor inhibitor	ABL1|BCR|FGFR1|FGFR2|FGFR3|FGFR4|FLT3|KDR|KIT|LCK|LYN|PDGFRA|RET|SRC|TEK	hematologic malignancy	chronic myeloid leukemia (CML)|acute lymphoblastic leukemia (ALL)
ponesimod	Phase 3	sphingosine 1-phosphate receptor agonist	S1PR1		
posaconazole	Launched	sterol demethylase inhibitor	CYP3A4	infectious disease	oropharyngeal candidiasis
potassium-canrenoate	Launched	mineralocorticoid receptor antagonist	NR3C2	cardiology	edema
potassium-iodide	Launched			pulmonary	asthma|bronchitis|emphysema
potassium-p-aminobenzoate	Launched			rheumatology|urology	scleroderma|dermatomyositis|Peyronie's disease
pozanicline	Phase 2	acetylcholine receptor antagonist	CHRNA4|CHRNB2		
poziotinib	Phase 2	EGFR inhibitor	EGFR|ERBB2|ERBB4		
PP-1	Preclinical	SRC inhibitor	HCK|RET		
PP-121	Preclinical	protein tyrosine kinase inhibitor	ABL1|EGFR|HCK|KDR|MTOR|PDGFRA|PIK3CA|PIK3CB|PIK3CD|PIK3CG|PRKDC|SRC		
PP-2	Preclinical	SRC inhibitor	ABL1|LCK|RIPK2|SRC		
PPT	Preclinical	estrogen receptor agonist	ESR1		
PPY-A	Preclinical	Abl kinase inhibitor	ABL1|BCR		
PP242	Preclinical	mTOR inhibitor	MTOR|PASK		
PQ-401	Preclinical	IGF-1 inhibitor	IGF1R		
PR-619	Preclinical	DUB inhibitor			
practolol	Withdrawn	adrenergic receptor antagonist	ADRB1		
pradefovir	Phase 2	cytochrome P450 activator			
pralatrexate	Launched	dihydrofolate reductase inhibitor	DHFR	hematologic malignancy	peripheral T-cell lymphoma (PTCL)
pralidoxime	Launched	acetylcholinesterase inhibitor	ACHE|BCHE	critical care	organophosphate poisoning
pralidoxime-chloride	Launched	acetylcholinesterase inhibitor	ACHE|BCHE	pulmonary	respiratory depression
pralmorelin	Launched	growth hormone releasing peptide ligand agonist			
pramipexole	Launched	dopamine receptor agonist	ADRA2A|ADRA2B|ADRA2C|DRD1|DRD2|DRD3|DRD4|DRD5|HTR1A|HTR1B|HTR1D|HTR2A|HTR2B|HTR2C	neurology/psychiatry	Parkinson's Disease
pramiracetam	Launched	acetylcholine receptor agonist		neurology/psychiatry	senile dementia
pramoxine	Launched	topical anesthetic		dermatology	corticosteroid-responsive dermatoses
pranidipine	Phase 2	calcium channel blocker	CACNA1C		
pranlukast	Launched	leukotriene receptor antagonist	CYSLTR1|CYSLTR2|IL5|MUC2|NFKB1|RNASE3|TNF	pulmonary	bronchospasm|asthma
pranoprofen	Launched	cyclooxygenase inhibitor		neurology/psychiatry	pain relief
prasterone-acetate	Preclinical				
prasugrel	Launched	purinergic receptor antagonist	P2RY12	cardiology	myocardial infarction|acute coronary syndrome (ACS)
pravadoline	Preclinical	cyclooxygenase inhibitor	CNR1|CNR2		
pravastatin	Launched	HMGCR inhibitor	HMGCR|SLCO1B1	endocrinology|cardiology	hypercholesterolemia|myocardial infarction|hyperlipidemia
praziquantel	Launched	anthelmintic agent		infectious disease	gastrointestinal parasites|cystic hydatid disease|schistosomiasis
prazosin	Launched	adrenergic receptor antagonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|KCNH2|KCNH6|KCNH7	cardiology	hypertension
PRE-084	Preclinical	sigma receptor agonist	SIGMAR1		
preclamol	Phase 2	dopamine receptor agonist	DRD2		
prednicarbate	Launched	phospholipase activator	PLA2G1B	dermatology|ophthalmology|neurology/psychiatry	eczema|contact dermatitis|itching
prednisolone	Launched	glucocorticoid receptor agonist	NR3C1|NR3C2|SERPINA6	ophthalmology|dermatology|infectious disease	conjunctivitis|rosacea|punctate keratitis|shingles|iritis|cyclitis
prednisolone-acetate	Launched	glucocorticoid receptor agonist	NR3C1	ophthalmology|dermatology|infectious disease	conjunctivitis|rosacea|punctate keratitis|shingles|iritis|cyclitis
prednisolone-hemisuccinate	Preclinical	glucocorticoid receptor agonist	NR3C1		
prednisolone-sodium-phosphate	Launched	glucocorticoid receptor agonist	NR3C1	allergy|pulmonary|ophthalmology|infectious disease|rheumatology|endocrinology|neurology/psychiatry|gastroenterology|hematology	allergic rhinitis|asthma|contact dermatitis|mycosis|lupus|hypercalcemia|thyroiditis|congenital adrenal hyperplasia|multiple sclerosis|ulcerative colitis|enteritis|thrombocythemia|pneumonia|meningitis|psoriatic arthritis|rheumatoid arthritis
prednisolone-tebutate	Launched	anti-inflammatory agent			
prednisone	Launched	glucocorticoid receptor agonist	HSD11B1|NR3C1	endocrinology|rheumatology|infectious disease|dermatology|ophthalmology|hematology|gastroenterology|neurology/psychiatry	congenital adrenal hyperplasia|hypercalcemia|rheumatoid arthritis|psoriatic arthritis|ankylosing spondylitis|bursitis|osteoarthritis|epicondylitis|dermatomyositis|psoriasis|mycosis|conjunctivitis|anemia|ulcerative colitis|enteritis|multiple sclerosis|meningitis
pregnenolone	Launched	glutamate receptor modulator	SULT2B1	rheumatology	rheumatoid arthritis
pregnenolone-succinate	Preclinical	GABA receptor negative allosteric modulator	CYP17A1		
preladenant	Phase 3	adenosine receptor antagonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
prenylamine	Withdrawn	calcium channel blocker			
presatovir	Phase 2	RSV fusion inhibitor			
pretomanid	Launched	nitric oxide donor	FASN		
pridinol	Launched	muscle relaxant		neurology/psychiatry	muscle relaxant
pridopidine	Phase 2	dopamine receptor antagonist			
prilocaine	Launched	local anesthetic	SCN5A	neurology/psychiatry	anesthetic
primaquine	Launched	antimalarial agent|DNA inhibitor		infectious disease	malaria
PRIMA1	Preclinical	TP53 inhibitor	ACHE		
primidone	Launched	GABA receptor antagonist	CHRNA4|CHRNA7|GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ|GRIA2|GRIK2|SCN10A|SCN11A|SCN1A|SCN2A|SCN3A|SCN4A|SCN5A|SCN7A|SCN8A|SCN9A	neurology/psychiatry	seizures
prinaberel	Phase 2	estrogen receptor agonist	ESR2|NCOA1		
prinomastat	Phase 3	matrix metalloprotease inhibitor			
priralfinamide	Phase 3	sodium channel blocker	CACNA1B		
prisotinol	Phase 2				
pritelivir	Phase 2	helicase primase inhibitor			
PRLX-93936	Phase 1/Phase 2	voltage-dependent anion selective channel protein inhibitor			
PRN1008	Preclinical	Bruton's tyrosine kinase (BTK) inhibitor			
PRN1371	Phase 1	protein tyrosine kinase inhibitor			
proacipimox	Phase 1	cholesterol inhibitor			
proadifen	Preclinical	nitric oxide synthase inhibitor	NOS1		
probenecid	Launched	uricosuric blocker	PANX1|SLC22A11|SLC22A6|SLC22A8|SLCO1C1	nephrology|rheumatology	hyperuricemia|gout
probucol	Launched	atherogenesis inhibitor	ABCA1|ABCB11|CES1	cardiology	coronary artery disease (CAD)
procainamide	Launched	sodium channel blocker	DNMT1|SCN5A	cardiology	ventricular arrhythmias|ventricular tachycardia (VT)
procaine	Launched	HMGCR inhibitor	CHRNA2|GRIN3A|HTR3A|KCNMA1|KCNMB1|KCNMB2|KCNMB3|KCNMB4|KCNN1|KCNN2|KCNN3|KCNN4|MAOA|MAOB|RYR1|RYR2|SCN10A|SLC6A3	neurology/psychiatry	anesthetic
procarbazine	Launched	monoamine oxidase inhibitor		hematologic malignancy	Hodgkin's lymphoma
procaterol	Launched	adrenergic receptor agonist	ADRB2	pulmonary	asthma
prochlorperazine	Launched	dopamine receptor antagonist	DRD1|DRD2|DRD3|DRD4	gastroenterology	nausea|vomiting
procodazole	Preclinical	immunostimulant			
procyanidin-B-2	Phase 2				
procyclidine	Launched	acetylcholine receptor antagonist		neurology/psychiatry	parkinsonism|Parkinson's Disease|akathisia|dystonia
procysteine	Phase 3	glutathione synthase stimulant			
profenamine	Launched	butyrylcholinesterase inhibitor|cholinergic receptor antagonist	CHRM1	neurology/psychiatry	Parkinson's Disease
proflavine-hemisulfate	Phase 2	topical anesthetic	F2		
progesterone	Launched	progesterone receptor agonist	CATSPER1|CATSPER2|CATSPER3|CATSPER4|CYP17A1|ESR1|NR3C2|OPRK1|PGR|TRPC5	obstetrics/gynecology|endocrinology	infertility|amenorrhea
proglumetacin	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	neurology/psychiatry	pain relief
proglumide	Withdrawn	CCK receptor antagonist	CCKAR|CCKBR		
proguanil	Launched	dihydrofolate reductase inhibitor	DHFR	infectious disease	malaria
prolylleucylglycinamide	Phase 2	melanocyte-stimulating hormone release inhibitor			
promazine	Launched	dopamine receptor antagonist	ADRA1A|ADRA1B|ADRA1D|CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|DRD1|DRD2|DRD3|DRD4|HRH1|HTR2A|HTR2C	neurology/psychiatry	schizophrenia
promestriene	Launched	estrogen receptor agonist	ESR1	endocrinology	androgenetic alopecia
promethazine	Launched	histamine receptor antagonist	HRH1	neurology/psychiatry|allergy	sedative|allergic rhinitis
pronethalol	Withdrawn	adrenergic receptor antagonist			
propacetamol	Launched	cyclooxygenase inhibitor	PTGS2	endocrinology|neurology/psychiatry	fever|pain relief
propafenone	Launched	antiarrhythmic	ADRB1|ADRB2|KCNA5|KCNH2	cardiology	atrial fibrillation (AF)|ventricular tachycardia (VT)|ventricular arrhythmias
propagermanium	Launched	CCR agonist|interferon receptor agonist	CCR2	infectious disease	hepatitis B
propantheline	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4	gastroenterology	peptic ulcer disease (PUD)
propatylnitrate	Launched			cardiology	angina pectoris
propentofylline	Launched	adenosine reuptake inhibitor|phosphodiesterase inhibitor	PDE1A	neurology/psychiatry	stroke
propidium-iodide	Preclinical		ACHE		
propiolactone	Launched			infectious disease	antiseptic
propiverine	Launched	acetylcholine receptor antagonist	CHRM1	urology	urinary incontinence
propofol	Launched	benzodiazepine receptor agonist	FAAH|GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ|SCN2A|SCN4A	neurology/psychiatry	anesthetic
propoxur	Launched			infectious disease	flea control
propoxycaine	Launched	local anesthetic		neurology/psychiatry	anesthetic
propranolol	Launched	adrenergic receptor antagonist	ADRB1|ADRB2	cardiology|neurology/psychiatry	hypertension|angina pectoris|migraine headache
propranolol-(R)	Preclinical	adrenergic receptor antagonist	ADRB2|ADRB3		
propranolol-(S)	Preclinical	adrenergic receptor antagonist	ADRB1|HTR1A|HTR5A|SLC10A1		
propyl-benzoate	Launched				
propylene-glycol	Launched				
propylhexedrine	Launched	adrenergic receptor agonist		otolaryngology|endocrinology|allergy	nasal congestion|fever|allergic rhinitis
propylparaben	Launched				
propylthiouracil	Launched	thyroid peroxidase inhibitor	DIO1|TPO	endocrinology	hyperthyroidism|Grave's disease|goiter
propyphenazone	Preclinical	anti-inflammatory agent			
proquazone	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	neurology/psychiatry	pain relief
proscillaridin-A	Launched			cardiology	congestive heart failure|cardiac arrythmia
protionamide	Launched			infectious disease	tuberculosis
protirelin	Launched	thyrotropin releasing hormone receptor agonist	TRHR	radiology	thyroid function diagnostic
protoporphyrin-IX	Preclinical	heme oxygenase inhibitor	HMOX1		
protriptyline	Launched	tricyclic antidepressant	SLC6A2|SLC6A4	neurology/psychiatry	depression
proxodolol	Launched	adrenergic receptor antagonist			
proxyfan	Preclinical	histamine receptor modulator	HRH3		
proxymetacaine	Launched	sodium channel blocker	SCN10A|SCN5A	neurology/psychiatry	anesthetic
Proxyphylline	Launched			pulmonary	asthma
PRT062070	Phase 2/Phase 3	JAK inhibitor|SYK inhibitor	SYK		
PRT062607	Phase 2	SYK inhibitor	FGR|MAP3K9|SYK		
PRT4165	Preclinical	polycomb repressive complex inhibitor	PRC1		
prucalopride	Launched	serotonin receptor agonist	HTR4	gastroenterology	constipation
prulifloxacin	Launched	bacterial DNA gyrase inhibitor		infectious disease|pulmonary|gastroenterology	urinary tract infections|bronchitis|diarrhea
pruvanserin	Phase 2	serotonin receptor antagonist	HTR2A|HTR2C		
PRX-07034	Phase 1	serotonin receptor antagonist			
PRX-08066	Phase 2	serotonin receptor antagonist	HTR2B		
PSB-06126	Preclinical	NTPDase inhibitor	ENTPD3		
PSB-11	Preclinical	adenosine receptor antagonist	ADORA1|ADORA2A|ADORA3		
PSB-1115	Preclinical	adenosine receptor antagonist	ADORA1|ADORA2B|ADORA3		
PSB-36	Preclinical	adenosine receptor antagonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
PSB-603	Preclinical	adenosine receptor antagonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
PSI-6130	Phase 1	RNA polymerase inhibitor			
PSI-697	Phase 1	P selectin inhibitor			
PSI-7976	Preclinical	HCV inhibitor			
PSN-375963	Preclinical	glucose dependent insulinotropic receptor agonist	GPR119		
PSNCBAM-1	Preclinical	cannabinoid receptor modulator	CNR1		
psoralen	Launched		MAOA|MAOB	dermatology	psoriasis|eczema|vitiligo
PS178990	Phase 1	androgen receptor modulator	AR		
PT-2385	Phase 1	hypoxia inducible factor inhibitor	EPAS1		
PTC-028	Preclinical	BMI-1 inhibitor			
PTC-209	Preclinical	BMI-1 inhibitor			
pterostilbene	Phase 2/Phase 3	cyclooxygenase inhibitor|PPAR receptor agonist	PTGS2		
PU-H71	Phase 1	HSP inhibitor	HSP90AA1		
puerarin	Phase 2	serotonin receptor antagonist			
pumosetrag	Phase 2	serotonin receptor agonist	HTR3A|HTR4		
purmorphamine	Preclinical	smoothened receptor agonist	SMO		
puromycin	Preclinical	protein synthesis inhibitor	NHP2L1|RPL10L|RPL11|RPL13A|RPL15|RPL19|RPL23|RPL23A|RPL26L1|RPL3|RPL37|RPL8|RSL24D1		
purvalanol-A	Preclinical	CDK inhibitor	CDK1|CDK2|CDK4|CDK5|CSNK1G3|RPS6KA1|SRC		
purvalanol-B	Preclinical	tyrosine kinase inhibitor	CDK2|CDK4|CDK5|MAPK1|MAPK3|SRPK2		
putrescine	Phase 2	tissue transglutaminase inhibitor	AMD1|KCNJ4|ODC1		
PX-12	Phase 2	thioredoxin inhibitor	CNR1|TXN		
PX-478	Phase 1	hypoxia inducible factor inhibitor			
PYM50028	Phase 2	neurotrophic agent			
PYR-41	Preclinical	ubiquitin activating enzyme inhibitor			
pyrantel	Launched	acetylcholine receptor agonist|nicotinic receptor agonist		infectious disease	gastrointestinal roundworms
pyrantel-pamoate	Launched	neuromuscular blocker		infectious disease	hookworm|tapeworm
pyrazinamide	Launched	fatty acid synthase inhibitor	FASN	infectious disease	tuberculosis
pyrazinoylguanidine	Phase 1	diuretic			
pyrazolanthrone	Preclinical	JNK inhibitor	MAPK10|MAPK8|MAPK8IP1|MAPK9|TTK		
pyrazoloacridine	Phase 2	topoisomerase inhibitor	TOP1|TOP2A		
pyrethrins	Launched			infectious disease	flea control
pyridoxal	Launched		PDXK	neurology/psychiatry	epilepsy
pyridoxal-isonicotinoyl-hydrazone	Phase 2	apoptosis stimulant			
pyridoxamine	Phase 3	AGE inhibitor			
pyridoxine	Launched	vitamin B	DDC|PDXK	metabolism	vitamin B6 deficiency
pyrimethamine	Launched	dihydrofolate reductase inhibitor	DHFR|SLC47A1	infectious disease	malaria
pyrintegrin	Preclinical	integrin signaling activator			
pyrithione-zinc	Launched	ATP synthase inhibitor	KCNQ1|KCNQ2|KCNQ4|KCNQ5	dermatology	dandruff|cosmetic
pyrithyldione	Withdrawn	psychoactive drug			
pyritinol	Launched			rheumatology|neurology/psychiatry	rheumatoid arthritis|senile dementia
pyronaridine	Phase 3	antimalarial agent			
pyrotinib	Phase 3	kinase inhibitor			
pyroxamide	Phase 1	HDAC inhibitor	HDAC1		
pyrrolidine-dithiocarbamate	Preclinical	NFkB pathway inhibitor	HSD11B1|RELA		
pyrvinium-pamoate	Launched	androgen receptor antagonist	AR	infectious disease	pinworm
PZ-2891	Preclinical	pantothenate kinase activator			
P22077	Preclinical	ubiquitin specific protease inhibitor	USP7		
P276-00	Phase 2	CDK inhibitor	CDK1|CDK4|CDK9		
P5091	Preclinical	ubiquitin specific protease inhibitor	USP7		
P7C3	Preclinical	NAMPT inhibitor	NAMPT		
Q-203	Phase 2	ATP synthase inhibitor			
quazinone	Phase 2	phosphodiesterase inhibitor	PDE3A|PDE3B		
quercetin	Launched	polar auxin transport inhibitor	ATP5A1|ATP5B|ATP5C1|HCK|HIBCH|PIK3CG|PIM1|STK17B|UGT3A1	neurology/psychiatry|allergy	fatigue|allergic rhinitis|drowsiness
quetiapine	Launched	dopamine receptor antagonist|serotonin receptor antagonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|DRD1|DRD2|DRD3|DRD4|DRD5|HRH1|HTR1A|HTR1B|HTR1D|HTR1E|HTR1F|HTR2A|HTR2C|HTR3A|HTR6|HTR7|SLC6A2	neurology/psychiatry	schizophrenia|bipolar disorder
quiflapon	Phase 2	leukotriene synthesis inhibitor	ALOX5|ALOX5AP		
quinagolide	Launched	dopamine receptor agonist	DRD2	endocrinology	hyperprolactinemia
quinapril	Launched	angiotensin converting enzyme inhibitor	ACE	cardiology	hypertension|congestive heart failure|angioedema
quinaprilat	Launched	angiotensin converting enzyme inhibitor	ACE	cardiology	hypertension|angioedema
quinelorane	Phase 3	dopamine receptor agonist	DRD2|DRD3		
quinestrol	Launched	estrogen receptor agonist	ESR1|ESR2	endocrinology	menopause
quinethazone	Launched	thiazide diuretic		cardiology	hypertension
quinidine	Launched	sodium channel blocker	KCNA5|KCNA7|KCNH1|KCNH2|KCNH5|KCNK1|KCNK6|SCN5A|SLC29A4	infectious disease|cardiology	malaria|atrial fibrillation (AF)|ventricular arrhythmias
quinine	Launched	hemozoin biocrystallization inhibitor	GP9|KCNB2|KCNN4|SLC29A4	infectious disease	malaria
quinine-ethyl-carbonate	Launched			infectious disease	malaria
quinolinic-acid	Preclinical	glutamate receptor agonist			
quinpirol-(-)	Phase 2	dopamine receptor agonist	DRD1|DRD2|DRD3|DRD4|HTR1A|HTR2A|HTR2B|HTR2C		
quipazine	Preclinical	serotonin receptor agonist	HTR1A|HTR1D|HTR2A|HTR2B|HTR2C|HTR3A|HTR3B|HTR6|SLC6A4		
quizartinib	Phase 3	FLT3 inhibitor	CSF1R|FLT3|KIT|PDGFRA|PDGFRB|RET		
QX-222	Preclinical	sodium channel blocker			
QX-314	Preclinical	sodium channel blocker	MAPK14|TGFBR1		
R-121919	Preclinical	CRF receptor antagonist			
R-1479	Phase 1	HCV inhibitor			
R-1485	Phase 1	serotonin receptor antagonist	HTR6		
R-1487	Phase 1	p38 MAPK inhibitor			
R-268712	Preclinical	serine/threonine kinase inhibitor	TGFBR1		
R-428	Phase 2	AXL kinase inhibitor	AXL		
R-59022	Preclinical	diacylglycerol kinase inhibitor|protein kinase inhibitor	DGKA		
R-96544	Preclinical	serotonin receptor antagonist	HTR2A		
rabeprazole	Launched	ATPase inhibitor|gastrin inhibitor	ATP4A	gastroenterology	gastroesophageal reflux disease (GERD)|duodenal ulcer disease|Zollinger-Ellison syndrome
rac-BHFF	Preclinical	GABA receptor positive allosteric modulator	GABBR1		
racecadotril	Launched	enkephalinase inhibitor	MME	gastroenterology	diarrhea
raclopride	Launched	dopamine receptor antagonist	DRD2|DRD3|HTR1A		
ractopamine	Launched	adrenergic receptor agonist		endocrinology	weight-gain aid
radafaxine	Phase 2	dopamine-norepinephrine reuptake inhibitor	SLC6A3		
radezolid	Phase 2	bacterial 30S ribosomal subunit inhibitor|bacterial 50S ribosomal subunit inhibitor			
radiprodil	Phase 2	acetylcholine receptor antagonist			
radotinib	Phase 3	Bcr-Abl kinase inhibitor			
RAD140	Phase 1	androgen receptor modulator			
RAF265	Phase 2	RAF inhibitor|VEGFR inhibitor	BRAF		
RAF709	Preclinical	RAF inhibitor			
ralinepag	Phase 3	IP1 prostacyclin receptor agonist			
raloxifene	Launched	estrogen receptor antagonist|selective estrogen receptor modulator (SERM)	ESR1|ESR2	orthopedics|oncology	osteoporosis|breast cancer
raltegravir	Launched	HIV integrase inhibitor		infectious disease	human immunodeficiency virus (HIV-1)
raltitrexed	Launched	thymidylate synthase inhibitor	FPGS|TYMS	oncology	mesothelioma
ramatroban	Launched	prostanoid receptor antagonist	PTGDR2|TBXA2R	cardiology|pulmonary	coronary artery disease (CAD)|asthma
ramelteon	Launched	melatonin receptor agonist	MTNR1A|MTNR1B	neurology/psychiatry	insomnia
ramifenazone	Launched	cyclooxygenase inhibitor		neurology/psychiatry|endocrinology	pain relief|fever
ramipril	Launched	angiotensin converting enzyme inhibitor	ACE	cardiology	hypertension
ramosetron	Launched	serotonin receptor antagonist	HTR3A	gastroenterology	nausea|vomiting|irritable bowel syndrome
ranirestat	Phase 3	aldose reductase inhibitor	AKR1B1		
ranitidine	Launched	histamine receptor antagonist	HRH2	gastroenterology	heartburn
ranolazine	Launched	sodium channel blocker	SCN10A|SCN9A	cardiology	chronic stable angina
rapastinel	Phase 2	glutamate receptor agonist			
rasagiline	Launched	monoamine oxidase inhibitor	BCL2|MAOB	neurology/psychiatry	Parkinson's Disease
rauwolscine	Preclinical	adrenergic receptor antagonist	ADRA2A|ADRA2B|ADRA2C|HTR1B|HTR1D|HTR1E|HTR2B		
ravoxertinib	Phase 1	ERK1 and ERK2 phosphorylation inhibitor	MAPK1|MAPK3		
ravuconazole	Phase 2	sterol demethylase inhibitor			
RBC8	Preclinical	Ral GTPase inhibitor	RALA|RALB		
rebamipide	Launched	free radical scavenger	FPR1	gastroenterology	peptic ulcer disease (PUD)|gastritis
rebastinib	Phase 1/Phase 2	Bcr-Abl kinase inhibitor|TIE tyrosine kinase inhibitor|VEGFR inhibitor	ABL1|BCR|FGR|FLT3|HCK|LYN|SRC		
reboxetine	Launched	adrenergic receptor antagonist	SLC6A2	neurology/psychiatry	depression
Rec-15/2615	Phase 2	adrenergic receptor antagonist	ADRA1A		
refametinib	Phase 2	MEK inhibitor	MAP2K1|MAP2K2		
regadenoson	Launched	adenosine receptor agonist	ADORA1|ADORA2A|ADORA2B|ADORA3	radiology	myocardial perfusion imaging (MPI)
regorafenib	Launched	FGFR inhibitor|KIT inhibitor|PDGFR tyrosine kinase receptor inhibitor|RAF inhibitor|RET tyrosine kinase inhibitor|VEGFR inhibitor	ABL1|BRAF|DDR2|EPHA2|FGFR1|FGFR2|FLT1|FLT4|FRK|KDR|KIT|MAPK11|NTRK1|PDGFRA|PDGFRB|RAF1|RET|TEK	oncology	colorectal cancer|gastrointestinal stromal tumors (GIST)
relcovaptan	Phase 2	vasopressin receptor antagonist	AVPR1A|AVPR1B|AVPR2|OXTR		
relebactam	Launched	beta lactamase inhibitor			
relugolix	Phase 3	gonadotropin releasing factor hormone receptor antagonist			
remacemide	Phase 3	glutamate receptor antagonist	GRIN1		
remetinostat	Phase 2	HDAC inhibitor			
remimazolam	Phase 3	benzodiazepine receptor agonist	GABBR1		
remodelin	Preclinical	transferase inhibitor	NAT10		
remoxipride	Withdrawn	dopamine receptor antagonist	DRD2|DRD3|DRD4|HTR2A|SIGMAR1		
repaglinide	Launched	insulin secretagogue	ABCC8|KCNJ11|PPARG	endocrinology	diabetes mellitus
reparixin	Phase 3	CC chemokine receptor antagonist	CXCR1|CXCR2		
repotrectinib	Phase 1/Phase 2	receptor tyrosine protein kinase inhibitor			
repsox	Preclinical	TGF beta receptor inhibitor	TGFBR1		
resatorvid	Phase 3	toll-like receptor inhibitor	TLR4		
reserpine	Launched	vesicular monoamine transporter inhibitor	SLC18A1|SLC18A2	cardiology	hypertension
resibufogenin	Phase 2	Na/K-ATPase inhibitor			
resiquimod	Phase 3	toll-like receptor agonist	TLR7|TLR8		
resmetirom	Phase 3	thyroid hormone receptor agonist			
resminostat	Phase 2	HDAC inhibitor	HDAC1|HDAC3|HDAC6|HDAC8		
resorcinol	Launched	phosphodiesterase inhibitor	CA12|CA14|CA2|PTGS1	dermatology	acne vulgaris (AV)|eczema|psoriasis|seborrheic dermatitis
resorcinol-monoacetate	Launched	antiseptic			
resveratrol	Launched	cytochrome P450 inhibitor|SIRT activator	CSNK2A1|NQO2|PTGS1|PTGS2		
retagliptin	Phase 1	dipeptidyl peptidase inhibitor			
retapamulin	Launched	protein synthesis inhibitor		infectious disease	impetigo
retaspimycin	Phase 3	HSP inhibitor	HSP90AA1		
retinaldehyde	Launched			dermatology	cosmetic
retinol	Launched	retinoid receptor ligand	ALDH1A1|ALDH1A2|ALDH1A3|DHRS3|DHRS4|LRAT|NR2C2|RBP1|RBP3|RDH11|RDH12|RDH13|RDH14|RDH5|RDH8|RETSAT|RHO|RLBP1|RXRA|RXRB|RXRG	dermatology	cosmetic|acne vulgaris (AV)|keratosis
retinyl-acetate	Launched				
retinyl-palmitate	Launched				
REV-5901	Phase 2	leukotriene receptor antagonist|lipoxygenase inhibitor	ALOX5		
revaprazan	Launched	potassium-competitive acid antagonist	ATP4A	gastroenterology	gastritis
revefenacin	Launched	cholinergic receptor antagonist			
reversan	Preclinical	MRP inhibitor	ABCC1		
reversine	Preclinical	Aurora kinase inhibitor	AURKB|INCENP|MAP2K1		
reynoutrin	Preclinical	antioxidant			
RGB-286638	Phase 1	CDK inhibitor	CDK1|CDK2|CDK3|CDK4|CDK5|CDK6|CDK7|CDK9|FLT3|GSK3B|JAK2|MAP3K7|MAPK9		
RGFP966	Preclinical	HDAC inhibitor	HDAC3		
RGX-104	Phase 1	LXR agonist			
RG108	Preclinical	DNA methyltransferase inhibitor	DNMT1|DNMT3B		
RG1530	Phase 1	FGFR inhibitor|PDGFR tyrosine kinase receptor inhibitor|VEGFR inhibitor	FGFR1|FGFR2		
RG2833	Phase 1	HDAC inhibitor	HDAC1|HDAC3		
RG4733	Phase 2	gamma secretase inhibitor	PSEN1		
RG7112	Phase 1	MDM inhibitor	MDM2		
RG7800	Preclinical	RNA splicing modifier			
RG7834	Preclinical	antiviral			
RHC-80267	Preclinical	triacylglycerol lipase inhibitor	DAGLA|DAGLB		
rhein	Phase 1		HSP90AA1		
rheochrysidin	Preclinical	protein tyrosine kinase inhibitor	PTPN1		
rhodamine-123	Phase 1				
RI-1	Preclinical		RAD51		
ribavirin	Launched	antiviral	ADK|ENPP1|IMPDH1|IMPDH2|NT5C2	infectious disease	hepatitis C
ribitol	Preclinical				
ribociclib	Launched	CDK inhibitor	CDK4|CDK6	oncology	breast cancer
riboflavin	Launched	vitamin B	BLVRB|RFK	gastroenterology	jaundice
riboflavin-tetrabutyrate	Preclinical	antioxidant			
riboflavin-5-phosphate-sodium	Launched		BLVRB|DHODH|DPYD|HAO1|HAO2|MT-ND1|NOS1|PNPO|POR|PPCDC|RFK|RPS6KA4|SGK1		
ribostamycin	Launched	bacterial 30S ribosomal subunit inhibitor	P4HB	infectious disease	human immunodeficiency virus (HIV-1)
ribostamycin-sulfate	Launched	bacterial 30S ribosomal subunit inhibitor		infectious disease	gram-negative bacterial infections
ricinoleic-acid	Launched	prostanoid receptor agonist	PTGER3		
ridinilazole	Phase 3	antibacterial			
rifabutin	Launched	protein synthesis inhibitor		infectious disease	human immunodeficiency virus (HIV-1)
rifampin	Launched	RNA polymerase inhibitor	NR1I2|SLCO1A2|SLCO1B1|SLCO1B3	infectious disease	tuberculosis|meningitis
rifamycin	Launched	DNA directed RNA polymerase inhibitor	SLCO1A2|SLCO1B1|SLCO1B3|SLCO2B1	infectious disease	tuberculosis|leprosy
rifamycin-sv	Phase 3	RNA synthesis inhibitor			
rifapentine	Launched	RNA polymerase inhibitor	CYP2C8|CYP2C9|CYP3A4	infectious disease	tuberculosis
rifaximin	Launched	RNA synthesis inhibitor		gastroenterology	diarrhea|irritable bowel syndrome|hepatic encephalopathy (HE)
rigosertib	Phase 3	cell cycle inhibitor|PLK inhibitor	PLK1		
rilapladib	Phase 2	phospholipase inhibitor			
rilmenidine	Launched	adrenergic receptor agonist|imidazoline receptor agonist	ADRA2A	cardiology	hypertension
rilpivirine	Launched	non-nucleoside reverse transcriptase inhibitor	NR1I2|SCN10A	infectious disease	human immunodeficiency virus (HIV-1)
riluzole	Launched	glutamate inhibitor	KCNK10|KCNK2|KCNK4|KCNN4|SCN10A|SCN11A|SCN1A|SCN2A|SCN3A|SCN4A|SCN5A|SCN7A|SCN8A|SCN9A|SLC7A11	neurology/psychiatry	amyotrophic lateral sclerosis (ALS)
rimantadine	Launched	antiviral|RNA synthesis inhibitor		infectious disease	influenza A virus infection
rimcazole	Phase 1	sigma receptor antagonist	SIGMAR1		
rimegepant	Launched	calcitonin antagonist	CALCA		
rimeporide	Phase 1	sodium/hydrogen exchanger inhibitor			
rimexolone	Launched	glucocorticoid receptor agonist	NR3C1|SERPINA6	ophthalmology	anterior uveitis
rimonabant	Withdrawn	cannabinoid receptor antagonist	CNR1|GPR55		
riociguat	Launched	guanylate cyclase stimulant	GUCY1A2|GUCY1A3|GUCY1B2|GUCY1B3	cardiology	hypertension
riodipine	Phase 2	calcium channel blocker			
riodoxol	Launched	other antibiotic			
ripasudil	Launched	rho associated kinase inhibitor	ROCK1|ROCK2	ophthalmology	glaucoma|ocular hypertension
ripazepam	Phase 2	benzodiazepine receptor agonist	GABRA1		
ripretinib	Phase 3	receptor tyrosine protein kinase inhibitor			
risdiplam	Phase 2/Phase 3	RNA splicing inhibitor			
risedronate	Launched	osteoclast inhibitor	FDPS	orthopedics|endocrinology	osteoporosis|Paget's disease
rislenemdaz	Preclinical	ionotropic glutamate receptor antagonist			
risperidone	Launched	dopamine receptor antagonist|serotonin receptor antagonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|DRD1|DRD2|DRD3|DRD4|HRH1|HTR1A|HTR1B|HTR1D|HTR1E|HTR1F|HTR2A|HTR2C|HTR6|HTR7	neurology/psychiatry	schizophrenia|bipolar disorder|irritability
RITA	Preclinical	MDM inhibitor	MDM2		
ritanserin	Phase 3	serotonin receptor antagonist	ADRA1A|ADRA1B|ADRA1D|HTR1A|HTR1B|HTR1D|HTR2A|HTR2B|HTR2C|HTR5A|HTR6|HTR7		
ritodrine	Withdrawn	adrenergic receptor agonist		obstetrics/gynecology	premature labor
ritonavir	Launched	HIV protease inhibitor	CYP1A2|CYP2B6|CYP2C19|CYP2C8|CYP2C9|CYP2D6|CYP2E1|CYP3A4|CYP3A5|CYP3A7	infectious disease	human immunodeficiency virus (HIV-1)
rivanicline	Phase 2	acetylcholine receptor agonist	CHRNA4|CHRNB2|CXCL8		
rivaroxaban	Launched	coagulation factor inhibitor	F10	neurology/psychiatry|hematology|cardiology	stroke|systemic embolism|atrial fibrillation (AF)|deep vein thrombosis (DVT)|pulmonary embolism (PE)
rivastigmine	Launched	acetylcholinesterase inhibitor	ACHE|BCHE	neurology/psychiatry	Alzheimer's disease|Parkinson's Disease|senile dementia
rizatriptan	Launched	serotonin receptor agonist	HTR1A|HTR1B|HTR1D|HTR1E|HTR1F	neurology/psychiatry	migraine headache
RKI-1447	Preclinical	rho associated kinase inhibitor	CDC42BPA|DMPK|LIMK1|MYLK|PAK1|PKN1|ROCK1|ROCK2		
RLX	Preclinical				
RMC-4550	Preclinical	SHIP2 phosphatase inhibitor			
RN-1	Preclinical	histone demethylase inhibitor	KDM1A		
RN-1734	Preclinical	TRPV antagonist	TRPV4		
RN-1747	Preclinical	TRPV agonist	TRPV4		
Ro-04-5595	Preclinical	glutamate receptor antagonist	GRIN2B		
Ro-08-2750	Preclinical	NGF binding inhibitor	NGF|NGFR		
Ro-10-5824	Preclinical	dopamine receptor agonist	DRD4		
Ro-106-9920	Preclinical	NFkB pathway inhibitor			
Ro-1138452	Preclinical	prostanoid receptor antagonist	PTGIR		
Ro-15-4513	Preclinical	GABA benzodiazepine site receptor inverse agonist	GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB2|GABRG2		
Ro-19-4605	Preclinical	GABA benzodiazepine site receptor inverse agonist	GABRA1|GABRA2|GABRA3|GABRA5		
Ro-20-1724	Preclinical	phosphodiesterase inhibitor	PDE3A|PDE4A|PDE4B|PDE4C|PDE4D		
Ro-25-6981	Preclinical	glutamate receptor antagonist|monamine transporter modulator	GRIN2B		
Ro-28-1675	Preclinical	glucokinase activator	GCK		
Ro-3	Preclinical	purinergic receptor antagonist	P2RX3		
Ro-3306	Preclinical	CDK inhibitor	CDK1		
Ro-48-6791	Preclinical	GABA receptor modulator			
Ro-48-8071	Preclinical	oxidosqualene cyclase inhibitor	LSS		
Ro-4987655	Phase 1	MEK inhibitor	MAP2K1		
Ro-5028442	Phase 1	vasopressin receptor antagonist			
Ro-5126766	Phase 1	MEK inhibitor|RAF inhibitor	BRAF|MAP2K1|MAP2K2|RAF1		
Ro-5263397	Preclinical	trace amine associated receptor agonist			
Ro-60-0175	Preclinical	serotonin receptor agonist	HTR2A|HTR2B|HTR2C		
Ro-61-8048	Preclinical	kynurenine 3-monooxygenase inhibitor	KMO		
Ro-67-7476	Preclinical	glutamate receptor positive allosteric modulator	GRM1		
Ro-90-7501	Preclinical	beta amyloid protein neurotoxicity inhibitor	APP		
Ro-9187	Preclinical	HCV inhibitor			
robalzotan	Phase 2	serotonin receptor antagonist	HTR1A		
roblitinib	Preclinical	FGFR inhibitor			
rociletinib	Phase 3	EGFR inhibitor	EGFR		
rocuronium	Launched	acetylcholine receptor antagonist	CHRM2|CHRNA2|HTR3A	neurology/psychiatry	anesthetic
rofecoxib	Withdrawn	cyclooxygenase inhibitor	ELN|PTGS2		
roflumilast	Launched	phosphodiesterase inhibitor	PDE4A|PDE4B|PDE4C|PDE4D	pulmonary	chronic obstructive pulmonary disease (COPD)|bronchitis
rogaratinib	Phase 2/Phase 3	FGFR inhibitor			
rolapitant	Phase 3	neurokinin receptor antagonist			
rolipram	Phase 3	phosphodiesterase inhibitor			
rolitetracycline	Launched	bacterial 30S ribosomal subunit inhibitor		infectious disease	gram-negative bacterial infections|gram-positive bacterial infections
roluperidone	Phase 2				
rolziracetam	Phase 2				
romidepsin	Launched	HDAC inhibitor	HDAC1|HDAC2|HDAC3|HDAC4|HDAC5|HDAC6|HDAC7|HDAC8|HDAC9	hematologic malignancy	cutaneous T-cell lymphoma (CTCL)
ronidazole	Launched	antiprotozoal agent		infectious disease	histomoniasis|dysentry
ropinirole	Launched	dopamine receptor agonist	ADRA2A|ADRA2B|ADRA2C|DRD1|DRD2|DRD3|DRD4|DRD5|HTR1A|HTR1B|HTR1D|HTR2A|HTR2B|HTR2C	neurology/psychiatry	Parkinson's Disease|restless leg syndrome
ropivacaine	Launched	sodium channel blocker	SCN10A	neurology/psychiatry	anesthetic
roquinimex	Phase 3	angiogenesis inhibitor|tumor necrosis factor production inhibitor			
rosamicin	Phase 2	protein synthesis inhibitor			
roscovitine	Phase 2	CDK inhibitor	CDK2|CDK9		
rose-bengal	Launched	contrast agent|immunostimulant		radiology	diagnostic agent
rose-bengal-lactone	Launched	coloring agent		ophthalmology	staining agent
rosiglitazone	Withdrawn	insulin sensitizer|PPAR receptor agonist	FFAR1|PPARG|TRPC5|TRPM3		
rosiptor	Phase 2	SHIP1 phosphatase activator			
rosmarinic-acid	Launched	GABA transaminase inhibitor	MCL1|TYR		
rosoxacin	Launched	topoisomerase inhibitor		infectious disease	urinary tract infections
rostafuroxine	Phase 2	ATPase inhibitor	ATP1A1		
rosuvastatin	Launched	HMGCR inhibitor	HMGCR	endocrinology|cardiology	hyperlipidemia|dyslipidemia|hypertriglyceridemia|hypercholesterolemia|atherosclerosis
rotigotine	Launched	dopamine receptor agonist	ADRA2B|DRD1|DRD2|DRD3|DRD4|DRD5|HTR1A	neurology/psychiatry	Parkinson's Disease|restless leg syndrome
rotundine	Launched	serotonin receptor agonist	DRD1|DRD2|DRD3|HTR1A	neurology/psychiatry	anxiety|sedative
rovazolac	Preclinical	LXR agonist			
roxarsone	Launched	antiprotozoal agent		endocrinology	weight-gain aid
roxatidine-acetate	Launched	histamine receptor antagonist	HRH2	gastroenterology	Zollinger-Ellison syndrome|erosive esophagitis (EE)|gastroesophageal reflux disease (GERD)|gastritis
roxithromycin	Launched	bacterial 50S ribosomal subunit inhibitor	MLNR	infectious disease	respiratory tract infections|urinary tract infections|skin infections
RP-001	Preclinical	sphingosine 1-phosphate receptor agonist	S1PR1		
RP67580	Preclinical				
RQ-00203078	Preclinical	transient receptor potential channel antagonist	TRPM8		
RRx-001	Phase 3	glucose 6-phosphate dehydrogenase inhibitor	G6PD		
RS-0481	Phase 2	immunostimulant			
RS-100329	Preclinical	adrenergic receptor antagonist	ADRA1A|ADRA1D		
RS-102221	Preclinical	serotonin receptor antagonist	HTR2A|HTR2B|HTR2C		
RS-102895	Preclinical	CCR antagonist	CCR2		
RS-127445	Phase 1	serotonin receptor antagonist	HTR2A|HTR2B|HTR2C		
RS-16566	Preclinical	serotonin receptor antagonist			
RS-17053	Preclinical	adrenergic receptor antagonist	ADRA1A|ADRA1D		
RS-23597-190	Preclinical	serotonin receptor antagonist	HTR4		
RS-39604	Preclinical	serotonin receptor antagonist	HTR4		
RS-45041-190	Preclinical	imidazoline receptor agonist			
RS-504393	Preclinical	CC chemokine receptor antagonist	CCL2|CCR2		
RS-56812	Preclinical	serotonin receptor partial agonist	HTR3A		
RS-67333	Preclinical	serotonin receptor partial agonist	HTR4		
RS-67506	Preclinical	serotonin receptor partial agonist	HTR4		
RS-79948	Preclinical	adrenergic receptor antagonist	ADRA2A		
RSV604	Phase 2	RSV replication inhibitor			
RTA-408	Phase 2	nitric oxide production inhibitor	NFE2L2		
RU-SKI-43	Preclinical	hedgehog pathway inhibitor	HHAT		
RU-24969	Phase 1	serotonin receptor agonist	HTR1A|HTR1B|HTR1D|HTR2A|HTR2B|HTR2C|HTR5A|HTR6		
RU-28318	Phase 2	cytochrome P450 inhibitor	NR3C2		
RU-42173	Phase 2	adrenergic receptor agonist	ADRB2		
RU-58841	Phase 2	androgen receptor antagonist	AR		
rubitecan	Phase 3	topoisomerase inhibitor	TOP1		
ruboxistaurin	Phase 3	PKC inhibitor			
rucaparib	Phase 3	PARP inhibitor	PARP1|PARP2		
rucinol	Phase 1	tyrosinase inhibitor	TYR		
rufinamide	Launched	voltage-gated sodium channel blocker	GRM5|SCN10A|SCN11A|SCN1A|SCN2A|SCN3A|SCN4A|SCN5A|SCN7A|SCN8A|SCN9A	neurology/psychiatry	seizures
rufloxacin	Launched	bacterial DNA gyrase inhibitor		infectious disease	gram-negative bacterial infections
rupatadine	Launched	histamine receptor antagonist|platelet activating factor receptor antagonist	HRH1|PTAFR	allergy	allergic rhinitis|urticaria
rutaecarpine	Preclinical	cyclooxygenase inhibitor	PTGS2		
rutin	Launched	antioxidant|capillary stabilizing agent|nitric oxide scavenger	AKR1C3	rheumatology|otolaryngology|gastroenterology|neurology/psychiatry|allergy	joint pain|nasal congestion|constipation|irritability|allergic rhinitis
ruxolitinib	Launched	JAK inhibitor	JAK1|JAK2|JAK3|TYK2	hematologic malignancy|hematology	myelofibrosis|polycythemia vera
ruxolitinib-(S)	Preclinical	JAK inhibitor	JAK1|JAK2		
RV1729	Phase 1	PI3K inhibitor			
RWJ-21757	Phase 2	toll-like receptor agonist	TLR7		
RWJ-50271	Preclinical	integrin inhibitor	ICAM1		
RWJ-67657	Phase 1	MAP kinase inhibitor	MAPK14|PTGS2		
RX-3117	Phase 1/Phase 2	CDK inhibitor|DNA synthesis inhibitor	CDK2|DNMT1		
RX-821002	Preclinical	adrenergic receptor antagonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C		
ryuvidine	Preclinical	histone lysine methyltransferase inhibitor	CDK2|CDK4		
R112	Phase 1	SYK inhibitor	SYK		
R306465	Phase 1	HDAC inhibitor			
R406	Phase 1	SYK inhibitor	RET|SYK		
R547	Phase 1	CDK inhibitor	CDK1|CDK2|CDK4|CDK7		
S-isopropylisothiourea	Preclinical	nitric oxide synthase inhibitor	NOS3		
S-methylcysteine	Phase 1		CTSD|MGMT		
S-nitrosoglutathione	Phase 1	nitric oxide stimulant	PTPN1		
S-sulfo-L-cysteine	Preclinical	glutamate receptor agonist			
S-trityl-L-cysteine	Preclinical	mitotic kinesin inhibitor			
S-07662	Preclinical	CAR antagonist	NR1I3		
S-111	Phase 2	PARP inhibitor	PARP1		
S-14506	Preclinical	serotonin receptor agonist	HTR1A		
S-17092	Preclinical	prolyl endopeptidase inhibitor			
S-3304	Phase 1/Phase 2	matrix metalloprotease inhibitor			
S-38093	Preclinical	histamine receptor antagonist			
SA-47	Preclinical	FAAH inhibitor	FAAH		
saccharin	Launched	DNA polymerase inhibitor	CA1|CA12|CA2|CA9		
saclofen	Preclinical	GABA receptor antagonist	GABBR1|GABBR2|KCTD12|KCTD16|KCTD8		
sacubitril	Launched	neprilysin inhibitor	MME	cardiology	congestive heart failure
sacubitrilat	Preclinical	neprilysin inhibitor			
safflower-yellow	Preclinical	anti-inflammatory agent			
safinamide	Launched	dopamine reuptake inhibitor|glutamate inhibitor|monoamine oxidase inhibitor	MAOB	neurology/psychiatry	Parkinson's Disease
safingol	Phase 1	PKC inhibitor	TRPM3		
safranal	Phase 2	benzodiazepine receptor agonist	GABBR1		
SAG	Preclinical	smoothened receptor agonist	SMO|TRPC6		
salazodine	Phase 2				
salicin	Phase 1	anti-inflammatory agent			
salicyl-alcohol	Preclinical				
salicylamide	Launched	analgesic agent		neurology/psychiatry|endocrinology	pain relief|fever
salicylanilide	Preclinical	other antibiotic			
salicylic-acid	Launched	cyclooxygenase inhibitor|prostanoid receptor antagonist	AKR1C1|ASIC3|PTGS1|PTGS2	dermatology|endocrinology|neurology/psychiatry	acne vulgaris (AV)|fever|pain relief
salidroside	Preclinical	beta amyloid protein neurotoxicity inhibitor	APP		
salinomycin	Launched			infectious disease	coccidiosis
salirasib	Phase 2	mTOR inhibitor	TRPA1		
salmeterol	Launched	adrenergic receptor agonist	ADRB2	pulmonary	asthma|chronic obstructive pulmonary disease (COPD)|bronchospasm
salsolinol-1-carboxylic-acid	Preclinical				
salubrinal	Preclinical	eukaryotic translation initiation factor inhibitor	EIF2S1		
salvianolic-acid-A	Phase 1	matrix metalloprotease inhibitor			
salvianolic-acid-B	Phase 2	EGFR inhibitor|metalloproteinase inhibitor	MMP9		
salvinorin-A	Phase 1	opioid receptor agonist	OPRD1|OPRK1|OPRM1		
sal003	Preclinical	eukaryotic translation initiation factor inhibitor	EIF2A		
SAM-315	Preclinical	serotonin receptor antagonist			
sameridine	Preclinical	opioid receptor modulator			
sanazole	Phase 1				
sancycline	Preclinical	antitumor agent			
sangivamycin	Phase 1	DNA inhibitor			
sanguinarium-chloride	Phase 1	apoptosis stimulant	CASP3		
SANT-1	Preclinical	smoothened receptor antagonist	SHH|SMO		
SANT-2	Preclinical	smoothened receptor antagonist	SHH|SMO		
sapacitabine	Phase 3	DNA synthesis inhibitor			
sapropterin	Launched	phenylalanine 4-hydroxylase stimulant	NOS3|PAH|TH|TPH1	metabolism	hyperphenylalaninemia (HPA)
saquinavir	Launched	HIV protease inhibitor	CYP3A4	infectious disease	human immunodeficiency virus (HIV-1)
SAR-245409	Phase 1/Phase 2	PI3K inhibitor	MTOR|PIK3CG		
saracatinib	Phase 2/Phase 3	SRC inhibitor	ABL1|LCK|SRC|YES1		
sarafloxacin	Launched	bacterial DNA gyrase inhibitor		infectious disease	gram-negative bacterial infections|gram-positive bacterial infections
sarcosine	Phase 2	glycine transporter inhibitor	SLC6A9		
sardomozide	Preclinical	S-adenosylmethionine decarboxylase inhibitor			
sari-59-801	Phase 1				
saroglitazar	Launched	PPAR receptor agonist	PPARA|PPARG	endocrinology|cardiology|gastroenterology	diabetes mellitus|dyslipidemia|non-alcoholic steatohepatitis (NASH)
sarpogrelate	Launched	serotonin receptor antagonist	HTR2A|HTR2B|HTR2C	endocrinology|cardiology|rheumatology	diabetes mellitus|angina pectoris|Raynaud's disease|atherosclerosis|Buerger's disease
SAR131675	Preclinical	VEGFR inhibitor	FLT4		
SAR405	Preclinical	PI3K inhibitor	PIK3C3		
SAR405838	Phase 1	MDM inhibitor	MDM2		
SAR407899	Phase 2	rho associated kinase inhibitor	ROCK1		
sasapyrine	Launched	NFkB pathway inhibitor	PTGS1|PTGS2	rheumatology	osteoarthritis|rheumatoid arthritis
satraplatin	Phase 3	DNA alkylating agent			
savolitinib	Phase 3	c-Met inhibitor	MET		
saxagliptin	Launched	dipeptidyl peptidase inhibitor	DPP4	endocrinology	diabetes mellitus
SB-200646	Preclinical	serotonin receptor antagonist	HTR2B|HTR2C		
SB-202190	Preclinical	p38 MAPK inhibitor	AKT1|ALOX5|CHEK1|GSK3B|LCK|MAPK1|MAPK11|MAPK12|MAPK14|MAPK8|PRKCA|ROCK1|RPS6KB1|SGK1		
SB-203186	Preclinical	serotonin receptor antagonist	HTR4		
SB-203580	Preclinical	p38 MAPK inhibitor	AKT1|ALOX5|CHEK1|CYP2D6|CYP3A4|GAK|GSK3B|LCK|MAPK1|MAPK10|MAPK11|MAPK12|MAPK14|MAPK8|MAPK9|PRKCA|RAF1|RIPK2|ROCK1|RPS6KB1|SGK1|SRC|TNF		
SB-205384	Preclinical	GABA receptor modulator	GABRA3|GABRA5|GABRA6		
SB-206553	Preclinical	serotonin receptor antagonist	HTR2A|HTR2B|HTR2C		
SB-216641	Preclinical	serotonin receptor antagonist	HTR1A|HTR1B|HTR1D|HTR2A|HTR2B|HTR2C		
SB-216763	Preclinical	glycogen synthase kinase inhibitor	CCNA2|CDK2|GSK3A|GSK3B		
SB-218078	Preclinical	CHK inhibitor	CHEK1		
SB-218795	Preclinical	tachykinin antagonist	TACR3		
SB-221284	Preclinical	serotonin receptor antagonist	HTR2A|HTR2B|HTR2C		
SB-222200	Preclinical	tachykinin antagonist	TACR3		
SB-225002	Preclinical	CC chemokine receptor antagonist	CXCR2		
SB-228357	Preclinical	serotonin receptor antagonist	HTR2A|HTR2B|HTR2C		
SB-2343	Phase 1	mTOR inhibitor|PI3K inhibitor	MTOR|PIK3CA|PIK3CB|PIK3CD|PIK3CG		
SB-239063	Preclinical	p38 MAPK inhibitor	MAPK11|MAPK14|PTGS2		
SB-242235	Phase 1	p38 MAPK inhibitor	HSPB1|MAPK14		
SB-243213	Phase 1	serotonin receptor inverse agonist	HTR2A|HTR2B|HTR2C|HTR6		
SB-258585	Preclinical	serotonin receptor antagonist	HTR6		
SB-268262	Preclinical	calcitonin antagonist	CALCA		
SB-269970	Preclinical	serotonin receptor antagonist	HTR7		
SB-271046	Phase 1	serotonin receptor antagonist	HTR6		
SB-297006	Preclinical	CC chemokine receptor antagonist	CCR3		
SB-328437	Preclinical	CCR antagonist			
SB-334867	Preclinical	orexin receptor antagonist	HCRTR1|HCRTR2		
SB-366791	Preclinical	TRPV antagonist	TRPV1		
SB-399885	Preclinical	serotonin receptor antagonist	HTR6		
SB-408124	Preclinical	orexin receptor antagonist	HCRTR1|HCRTR2		
SB-415286	Preclinical	glycogen synthase kinase inhibitor	GSK3A|GSK3B|RPS6KB1		
SB-431542	Preclinical	TGF beta receptor inhibitor	ACVR1C|TGFBR1		
SB-452533	Preclinical	TRPV antagonist	TRPV1		
SB-505124	Preclinical	ALK tyrosine kinase receptor inhibitor	TGFBR1		
SB-525334	Preclinical	TGF beta receptor inhibitor	TGFBR1		
SB-590885	Preclinical	RAF inhibitor	BRAF		
SB-612111	Preclinical	nociceptin/orphanin FQ receptor antagonist	OPRL1		
SB-649868	Phase 2	orexin receptor antagonist			
SB-657510	Preclinical	urotensin receptor antagonist	UTS2R		
SB-683698	Phase 1	integrin antagonist	ITGA4|ITGAV|ITGB1|ITGB7		
SB-705498	Phase 2	TRPV antagonist	TRPV1		
SB-706375	Preclinical	urotensin receptor antagonist	UTS2R		
SB-742457	Phase 3	serotonin receptor antagonist	HTR6		
SB-743921	Phase 1/Phase 2	kinesin-like spindle protein inhibitor	KIF11		
SB-747651A	Preclinical	kinase inhibitor	AKT1|AKT3|ROCK1|RPS6KA5|RPS6KB1		
SB-756050	Phase 1	G protein-coupled receptor agonist	GPBAR1		
SB-772077B	Preclinical	rho associated kinase inhibitor	ROCK1|ROCK2		
SB-939	Phase 3	HDAC inhibitor	HDAC1|HDAC10|HDAC2|HDAC3|HDAC4|HDAC5|HDAC6|HDAC9		
SBE-13	Preclinical	PLK inhibitor	PLK1		
SBHA	Preclinical	HDAC inhibitor	HDAC1|HDAC3		
SBI-115	Preclinical	G protein-coupled receptor antagonist			
SC-10	Preclinical	protein kinase activator	PRKCA		
SC-12267	Phase 2	dihydroorotate dehydrogenase inhibitor	IL17A		
SC-144	Preclinical	P glycoprotein inhibitor			
SC-19220	Preclinical	prostanoid receptor antagonist	PTGER1		
SC-236	Preclinical	cyclooxygenase inhibitor	PTGS2		
SC-51089	Preclinical	prostanoid receptor antagonist	PTGER1		
SC-560	Preclinical	cyclooxygenase inhibitor	PTGS1		
SC-9	Preclinical	protein tyrosine kinase activator	PRKCA		
scabertopin	Preclinical	anticancer agent			
SCH-202676	Preclinical	G protein-coupled receptor modulator	CHRM1|CHRM2|DRD1|DRD2		
SCH-221510	Preclinical	nociceptin/orphanin FQ receptor agonist	OPRL1		
SCH-23390	Preclinical	dopamine receptor antagonist	DRD1|DRD5|HTR2C|KCNJ4|KCNJ6		
SCH-28080	Phase 1	ATPase inhibitor	ATP4A		
SCH-51344	Preclinical	MTH1 inhibitor	NUDT1		
SCH-58261	Preclinical	adenosine receptor antagonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
SCH-900776	Phase 2	CHK inhibitor	CDK2|CHEK1		
schisandrin-B	Preclinical	antioxidant	ATR		
schisandrol-B	Phase 3	lipid peroxidase inhibitor			
sclareol	Preclinical				
sclareolide	Launched	other antifungal			
SCMC-Lys	Launched	mucolytic agent	GSTP1	pulmonary	chronic obstructive pulmonary disease (COPD)
scopine	Launched				
scopolamine	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|SI	neurology/psychiatry|gastroenterology	motion sickness|vomiting|nausea
scopolamine-N-oxide	Preclinical	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4		
SCP-1	Phase 1	analgesic agent			
scriptaid	Preclinical	HDAC inhibitor	HDAC1|HDAC2|HDAC3|HDAC4|HDAC5|HDAC6|HDAC7|HDAC8|HDAC9		
SCS	Preclinical				
SD-0006	Phase 2	p38 MAPK inhibitor			
SD-169	Preclinical	p38 MAPK inhibitor	MAPK14		
SD-208	Preclinical	TGF beta receptor inhibitor	TGFBR1		
SD-2590	Preclinical	matrix metalloprotease inhibitor	MMP1|MMP13|MMP2		
SDM25N	Preclinical	opioid receptor antagonist	OPRD1		
SDZ-NKT-343	Phase 1	tachykinin antagonist	TACR1		
SDZ-SER-082	Preclinical	serotonin receptor antagonist	HTR2A|HTR2B|HTR2C		
SDZ-WAG-994	Phase 2	adenosine receptor agonist	ADORA1		
SDZ-205-557	Preclinical	serotonin receptor antagonist	HTR3A|HTR3B		
SDZ-21009	Preclinical	adrenergic receptor antagonist|serotonin receptor antagonist	HTR1A|HTR1B		
SDZ-220-040	Preclinical	glutamate receptor antagonist	GRIN1		
SDZ-220-581	Preclinical	glutamate receptor antagonist	GRIN1		
Se-methylselenocysteine	Phase 2				
secalciferol	Launched	vitamin D receptor agonist	VDR	critical care	bone fracture
seclazone	Phase 1	anti-inflammatory agent			
seclidemstat	Phase 1	histone demethylase inhibitor			
secnidazole	Launched	acetylcholinesterase inhibitor|microtubule inhibitor		infectious disease	protozoan infection
secoisolariciresinol-(-)	Phase 2				
secoisolariciresinol-diglucoside	Phase 2	antioxidant			
securinine	Preclinical	GABA receptor antagonist|TP53 activator	GABRA1		
segesterone-acetate	Launched	progesterone receptor agonist	PGR		
seladelpar	Phase 3	PPAR receptor agonist			
selamectin	Launched	nematocide		infectious disease	flea control
selegiline	Launched	monoamine oxidase inhibitor	MAOA|MAOB	neurology/psychiatry	Parkinson's Disease
selenomethionine	Launched				
seletalisib	Preclinical	PI3K inhibitor			
selexipag	Launched	IP1 prostacyclin receptor agonist|platelet aggregation inhibitor	PTGIR	pulmonary	pulmonary arterial hypertension (PAH)
selfotel	Phase 3	glutamate receptor antagonist	GRIN2A|GRIN2B|GRIN2C|GRIN2D		
selinexor	Launched	exportin antagonist	XPO1	hematologic malignancy	multiple myeloma
selitrectinib	Phase 1/Phase 2	protein tyrosine kinase inhibitor			
selonsertib	Phase 2	MAP kinase activator			
selumetinib	Phase 3	MEK inhibitor	MAP2K1		
semagacestat	Phase 3	gamma secretase inhibitor	PSEN1		
semapimod	Phase 2	cytokine production inhibitor|p38 MAPK inhibitor	MAPK14		
semaxanib	Phase 3	VEGFR inhibitor	FGFR1|FLT1|KDR|KIT|PDGFRA|PDGFRB|RET		
semustine	Phase 3	DNA alkylating agent			
SEN-1269	Preclinical	beta amyloid inhibitor	APP		
senicapoc	Phase 3	intermediate conductance potassium channel blocker	KCNN4		
sennoside-A	Launched	glycoside agonist		gastroenterology	constipation
sennoside-protonated	Preclinical				
seocalcitol	Phase 3	vitamin D receptor agonist	VDR		
SEP-227900	Phase 1	D-amino acid oxidase Inhibitor	DAO		
seratrodast	Launched	prostanoid receptor antagonist	TBXA2R	pulmonary	asthma
serdemetan	Phase 1	MDM inhibitor	MDM2		
serotonin	Launched	growth factor receptor activator	DRD1|DRD5|HTR1A|HTR1B|HTR1D|HTR1E|HTR1F|HTR2A|HTR2B|HTR2C|HTR3A|HTR3B|HTR4|HTR5A|HTR6|HTR7|SLC36A1	neurology/psychiatry	anxiety|depression|sleeplessness
sertaconazole	Launched	sterol demethylase inhibitor		infectious disease	tinea pedis
sertindole	Withdrawn	dopamine receptor antagonist|serotonin receptor antagonist	ADRA1A|ADRA1B|ADRA1D|DRD2|DRD3|DRD4|HRH1|HTR1A|HTR1B|HTR1D|HTR1E|HTR1F|HTR2A|HTR2C|HTR6|KCNH2		
sertraline	Launched	selective serotonin reuptake inhibitor (SSRI)	SLC6A3|SLC6A4	neurology/psychiatry|obstetrics/gynecology	depression|obsessive compulsive disorder (OCD)|panic disorders|posttraumatic stress disorder|premenstrual syndrome|social anxiety disorder
sesamin	Preclinical	NFkB pathway inhibitor			
setipiprant	Phase 3	prostaglandin inhibitor	PTGDR2		
setiptiline	Launched	adrenergic receptor antagonist	HRH1|HTR2A|HTR2C	neurology/psychiatry	depression
setmelanotide	Phase 3	melanocortin receptor agonist			
sevoflurane	Launched	membrane integrity inhibitor	ATP2C1|ATP5D|GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ|GLRA1|GLRB|GRIA1|KCNA1|KCNK10|KCNK18|KCNK2|KCNK3|KCNK9|MT-ND1	neurology/psychiatry	anesthetic
SEW-2871	Preclinical	lysophospholipid receptor agonist	S1PR1		
SF-11	Preclinical	neuropeptide receptor antagonist	MCOLN3|NPY2R		
SGC-CBP30	Preclinical	bromodomain inhibitor	CREBBP|EP300		
SGC-0946	Preclinical	histone lysine methyltransferase inhibitor			
SGC-707	Preclinical	protein arginine N-methyltransferase inhibitor	PRMT3		
SGI-1027	Preclinical	DNA methyltransferase inhibitor	DNMT1|DNMT3A|DNMT3B		
SGI-1776	Phase 1	Pim kinase inhibitor	FLT3|PIM1|PIM2|PIM3		
SGS-742	Preclinical	GABA receptor antagonist	GABBR1|GABBR2		
SGX523	Phase 1	hepatocyte growth factor receptor inhibitor	MET		
SHA-68	Preclinical	neuropeptide receptor antagonist	NPSR1		
shikimic-acid	Preclinical				
SHP099	Preclinical	protein tyrosine kinase inhibitor	PTPN11		
SIB-1553A	Phase 2	acetylcholine receptor agonist	CHRNB4		
SIB-1757	Preclinical	glutamate receptor antagonist	GRM5		
SIB-1893	Preclinical	glutamate receptor antagonist	GRM4|GRM5		
SID-7969543	Preclinical	steroidogenic factor antagonist	NR5A1		
siguazodan	Phase 1	phosphodiesterase inhibitor	PDE3A		
sildenafil	Launched	phosphodiesterase inhibitor	PDE5A|PDE6G|PDE6H|SLCO1B1|SLCO1B3	urology	erectile dysfunction
silibinin	Launched	cytochrome P450 inhibitor	ALOX5	gastroenterology	hepatic cirrhosis
silodosin	Launched	adrenergic receptor antagonist	ADRA1A|ADRA1B|ADRA1D	urology	benign prostatic hyperplasia (BPH)
silver-sulfadiazine	Launched	PABA antagonist		critical care	sepsis
silymarin	Launched				
simeprevir	Launched	HCV inhibitor	CYP1A2|CYP3A4	infectious disease	hepatitis C
simurosertib	Preclinical	kinase inhibitor			
simvastatin	Launched	HMGCR inhibitor	HMGCR|ITGB2	endocrinology|cardiology|neurology/psychiatry	hypercholesterolemia|coronary heart disease|myocardial infarction|stroke|hyperlipidemia
sincalide	Preclinical	cholecystokinin agonist			
sinefungin	Preclinical	DNA methyltransferase inhibitor|RNA synthesis inhibitor	CARM1		
sinomenine	Preclinical	angiogenesis inhibitor			
sipatrigine	Phase 2	voltage-gated sodium channel blocker	CACNA1D|SCN10A|SCN1A|SCN3A|SCN4A|SCN5A|SCN9A		
siponimod	Launched	sphingosine 1-phosphate receptor modulator	S1PR1	neurology/psychiatry	multiple sclerosis
siramesine	Phase 2	sigma receptor antagonist	ADRA1A|ADRA1B|ADRA1D		
siremadlin	Preclinical	MDM inhibitor			
sirolimus	Launched	mTOR inhibitor	FKBP1A|MTOR	transplant|pulmonary	organ rejection|lymphangioleiomyomatosis
SirReal-2	Preclinical	SIRT inhibitor	SIRT2		
sirtinol	Preclinical	SIRT inhibitor	SIRT1|SIRT2		
sisomicin	Launched	protein synthesis inhibitor		ophthalmology	conjunctivitis|punctate keratitis
sisomicin-sulfate	Launched	bacterial 30S ribosomal subunit inhibitor		infectious disease	gram-negative bacterial infections
SIS3	Preclinical	serine/threonine kinase inhibitor	SMAD3|TGFBR1		
sitafloxacin	Launched	bacterial DNA gyrase inhibitor		infectious disease	buruli ulcer
sitagliptin	Launched	dipeptidyl peptidase inhibitor	DPP4	endocrinology	diabetes mellitus
sitaxentan	Withdrawn	endothelin receptor antagonist	EDNRA|EDNRB		
sitosterol	Preclinical				
sitravatinib	Phase 3	receptor tyrosine protein kinase inhibitor			
sivelestat	Launched	elastase inhibitor	CELA1|ELANE	pulmonary	acute lung injury
SJ-172550	Preclinical	MDM inhibitor	MDM4		
SJ-733	Phase 1	ATPase inhibitor			
SJG-136	Phase 2	DNA intercalating agent			
SK&F-10047-(+)	Phase 1	sigma receptor agonist	SIGMAR1		
SKA-31	Preclinical	potassium channel activator	KCNN4		
skepinone-L	Preclinical	p38 MAPK inhibitor	MAPK14		
SKF-38393	Preclinical	dopamine receptor agonist	CALY|DRD1|DRD5		
SKF-77434	Preclinical	dopamine receptor agonist	DRD1		
SKF-81297	Preclinical	dopamine receptor agonist	DRD1|DRD5		
SKF-83566	Preclinical	dopamine receptor antagonist	DRD1|DRD5		
SKF-86002	Preclinical	p38 MAPK inhibitor	ALOX5|MAPK14		
SKF-89976A	Preclinical	GABA uptake inhibitor	SLC6A1		
SKF-91488	Preclinical	histamine N-methyltransferase inhibitor	HNMT		
SKF-96365	Preclinical	calcium channel blocker	CYP3A4|PKD2|TRPC1|TRPC3|TRPC4|TRPC5|TRPV2		
SKI-II	Preclinical	sphingosine kinase inhibitor	SPHK1		
SKLB-1028	Preclinical	Abl kinase inhibitor|EGFR inhibitor|FLT3 inhibitor			
SKLB1002	Preclinical	VEGFR inhibitor	KDR		
SLV-319-(+/-)	Phase 2	cannabinoid receptor antagonist	CNR1|DRD2|HTR1A		
SLV-320	Phase 2	adenosine receptor antagonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
SM-108	Phase 2				
SM-164	Preclinical	XIAP inhibitor	BIRC2|BIRC3|XIAP		
SM-21	Preclinical	sigma receptor antagonist	PGRMC1		
SMER-28	Preclinical	autophagy inducer	SNCA		
SMI-4a	Preclinical	Pim kinase inhibitor	PIM1		
SN-2	Preclinical	transient receptor potential channel agonist	MCOLN3		
SN-38	Launched	topoisomerase inhibitor	TOP1	oncology	colorectal cancer
SN-6	Preclinical	sodium/calcium exchange inhibitor			
SNAP	Phase 2	nitric oxide donor	PTPN1		
SNAP-5089	Preclinical	adrenergic receptor antagonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|CACNA1C|CACNA1D		
SNAP-94847	Preclinical		ADRA1A|DRD2		
SNC-80	Preclinical		OPRD1		
SNG-1153	Preclinical	selective estrogen receptor modulator (SERM)	ESR1		
SNS-314	Phase 1	Aurora kinase inhibitor	AURKA|AURKB|AURKC		
SNX-2112	Phase 1	HSP inhibitor			
SNX-5422	Phase 1/Phase 2	HSP inhibitor	HSP90AA1|HSP90AB1		
sobetirome	Phase 1/Phase 2	thyroid hormone receptor agonist	THRA|THRB		
soblidotin	Phase 2	microtubule inhibitor			
sobrepin	Launched	mucolytic agent		pulmonary	chest congestion
sobuzoxane	Launched	topoisomerase inhibitor		hematologic malignancy	peripheral T-cell lymphoma (PTCL)
sodium-ascorbate	Launched				
sodium-butyrate	Phase 2	HDAC inhibitor	BCHE|FFAR2|FFAR3|HDAC1|HDAC2|HDAC3|HDAC8		
sodium-danshensu	Preclinical				
sodium-dodecyl-sulfate	Launched		ALB		
sodium-gluconate	Launched				
sodium-gualenate	Launched	antacid		gastroenterology|otolaryngology	peptic ulcer disease (PUD)|pharyngitis
sodium-monofluorophosphate	Launched		PYGM	dental	cavities
sodium-nitrite	Launched	nitric oxide donor		critical care	poison antidote|cyanide poisoning
sodium-nitroprusside	Launched	nitric oxide donor		cardiology	hypertension|congestive heart failure
sodium-orthovanadate	Preclinical				
sodium-picosulfate	Launched			gastroenterology	constipation
sodium-stibogluconate	Launched	tyrosine phosphatase inhibitor	PTPN6	infectious disease	leishmaniasis
sodium-tanshinone-II-A-sulfonate	Phase 2	potassium channel activator			
sodium-tetradecyl-sulfate	Launched		PROC	dermatology	varicose veins
sofalcone	Launched	mucus protecting agent	CBR1	gastroenterology	peptic ulcer disease (PUD)
sofosbuvir	Launched	HCV inhibitor		infectious disease	hepatitis C|hepatitis C
sofosbuvir-impurity-m	Preclinical	antiviral			
sograzepide	Phase 2	gastrin inhibitor			
solamargine	Phase 3	apoptosis inhibitor			
solcitinib	Phase 1	JAK inhibitor	JAK1		
solifenacin-succinate	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5	urology	urinary incontinence|urinary frequency
solithromycin	Phase 3	protein synthesis inhibitor			
solriamfetol	Launched	dopamine reuptake inhibitor		neurology/psychiatry	narcolepsy
somantadine	Phase 1	antiviral			
somatostatin	Launched	somatostatin receptor agonist	OPRD1|OPRM1|SSTR1|SSTR2|SSTR3|SSTR4|SSTR5	hematology	hemorrhage
sonepiprazole	Phase 2	dopamine receptor antagonist			
sonidegib	Launched	smoothened receptor antagonist	SMO	oncology	basal cell carcinoma (BCC)
sophocarpine	Phase 3				
sorafenib	Launched	FLT3 inhibitor|KIT inhibitor|PDGFR tyrosine kinase receptor inhibitor|RAF inhibitor|RET tyrosine kinase inhibitor|VEGFR inhibitor	BRAF|DDR2|FGFR1|FLT1|FLT3|FLT4|KDR|KIT|PDGFRB|RAF1|RET	oncology	renal cell carcinoma (RCC)|thyroid cancer|hepatocellular carcinoma (HCC)
soraprazan	Preclinical	proton pump inhibitor			
sorbic-acid	Launched				
sorbinil	Phase 3	aldose reductase inhibitor	AKR1B1		
sorbitan-monostearate	Preclinical				
sorbitol	Launched	mucolytic agent		gastroenterology	constipation
sotagliflozin	Phase 3	sodium/glucose cotransporter inhibitor	SLC5A1|SLC5A2		
sotalol	Launched	adrenergic receptor antagonist	ADRB1|ADRB2|KCNH2	cardiology	atrial fibrillation (AF)|ventricular arrhythmias
sotrastaurin	Phase 2	PKC inhibitor	PRKCA|PRKCB|PRKCD|PRKCE|PRKCH|PRKCQ		
SP-100030	Preclinical	NFkB pathway inhibitor	JUN|NFKB1		
SP-141	Preclinical	ubiquitin ligase inhibitor	MDM2		
SP-420	Phase 1				
spaglumic-acid	Launched	glutamate receptor antagonist	GRM3	allergy	allergic conjunctivitis|allergic rhinitis
sparfloxacin	Withdrawn	bacterial DNA gyrase inhibitor	TOP2A		
sparfosate	Phase 3	aspartate carbamoyltransferase inhibitor	CA2|CA4		
sparsentan	Phase 3	angiotensin receptor antagonist			
sparteine-(+)	Launched				
sparteine-(-)	Launched				
sparteine-sulfate	Launched				
spautin-1	Preclinical	deubiquitinase inhibitor	USP10|USP13		
spectinomycin	Launched	bacterial 30S ribosomal subunit inhibitor		pulmonary	airsacculitis|chronic respiratory disease
spermidine	Preclinical	glutamate receptor modulator	KCNJ4|TXNRD1		
spermine	Preclinical		CA14|CA4|CA6|CA9|CASR|GRIN1|GRIN2A|KCNJ4|ODC1|SMOX|SMS|TRPM4|TRPM5		
sphingosylphosphorylcholine	Preclinical	gene expression stimulant	GPR12		
spiperone	Launched	dopamine receptor antagonist	ADRA1A|ADRA1B|ADRA1D|DRD1|DRD2|DRD3|DRD4|DRD5|HTR1A|HTR1D|HTR2A|HTR2B|HTR2C|HTR6|HTR7	neurology/psychiatry	schizophrenia
spiradoline	Phase 2	opioid receptor agonist	OPRK1		
spiramycin	Launched	bacterial 50S ribosomal subunit inhibitor		infectious disease	toxoplasmosis|soft tissue infection
spirobromin	Phase 1				
spironolactone	Launched	mineralocorticoid receptor antagonist	AR|CACNA1A|CACNA1B|CACNA1C|CACNA1D|CACNA1F|CACNA1G|CACNA1H|CACNA1I|CACNA1S|CACNA2D1|CACNA2D2|CACNA2D3|CACNB1|CACNB2|CACNB3|CACNB4|CACNG1|CYP11B2|NR3C1|NR3C2|PGR|SHBG	endocrinology|cardiology|gastroenterology|rheumatology	hyperaldosteronism|congestive heart failure|hepatic cirrhosis|nephrotic syndrome|hypertension|hypokalemia
spiroxatrine	Preclinical	serotonin receptor antagonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|HTR1A|HTR2B		
spizofurone	Withdrawn				
splitomycin	Preclinical	SIRT inhibitor	SIRT1		
SPP301	Phase 3	endothelin receptor antagonist	EDNRA		
SPP86	Preclinical	receptor tyrosine protein kinase inhibitor	RET		
SQ-109	Phase 3	bacterial cell wall synthesis inhibitor	FDFT1		
SQ-22536	Preclinical	adenylyl cyclase inhibitor	ADCY1		
squalamine	Phase 3	antiviral			
squaric-acid-dibutyl-ester	Preclinical	oxidative stress inducer			
SR-1078	Preclinical	retinoid receptor agonist	RORA|RORC		
SR-11302	Preclinical				
SR-140333	Phase 2	neurokinin receptor antagonist	TACR1		
SR-1664	Preclinical	PPAR receptor ligand	PPARG		
SR-2211	Preclinical	retinoid receptor inverse agonist	RORC		
SR-2640	Phase 2	leukotriene receptor antagonist	CYSLTR1		
SR-27897	Phase 2	CCK receptor antagonist	CCKAR		
SR-3306	Preclinical	JNK inhibitor	MAPK10|MAPK8|MAPK9		
SR-33805	Phase 1	calcium channel blocker			
SR-3576	Preclinical	JNK inhibitor	MAPK10		
SR-3677	Preclinical	rho associated kinase inhibitor	ROCK2		
SR-57227A	Phase 2	serotonin receptor agonist	HTR3A		
SR-59230A	Preclinical	adrenergic receptor antagonist	ADRB1|ADRB2|ADRB3		
SR-95639A	Preclinical	acetylcholine receptor agonist	CHRM1		
SRC-kinase-inhibitor-I	Preclinical	SRC inhibitor	CSK|LCK|RIPK2		
SRPIN340	Preclinical	serine arginine protein kinase inhibitor	SRPK1|SRPK2		
SRT1720	Preclinical	SIRT activator	SIRT1		
SRT2104	Phase 2	SIRT activator	SIRT1		
SRT3190	Preclinical	CC chemokine receptor antagonist			
SSR128129E	Preclinical				
SSR180711	Phase 2	acetylcholine receptor agonist	CHRNA7		
SSR240612	Preclinical	bradykinin receptor antagonist			
ST-1535	Preclinical	adenosine receptor antagonist			
ST-1859	Phase 1	antiamyloidogenic agent			
ST-2825	Preclinical	myeloid differentiation primary response inhibitor	MYD88		
ST-91	Preclinical	adrenergic receptor agonist			
STA-5326	Phase 2	interleukin synthesis inhibitor	IL12A		
statil	Preclinical	aldose reductase inhibitor			
stattic	Preclinical				
STAT3-inhibitor-VI	Preclinical	STAT inhibitor	STAT3		
stavudine	Launched	DNA directed DNA polymerase inhibitor|nucleoside reverse transcriptase inhibitor		infectious disease	human immunodeficiency virus (HIV-1)
stemregenin-1	Preclinical	aryl hydrocarbon receptor antagonist	AHR		
stepronin	Launched	mucolytic agent			
stetaderm	Launched				
STF-083010	Preclinical	serine/threonine kinase inhibitor	ERN1		
STF-118804	Preclinical	NAMPT inhibitor	NAMPT		
STF-31	Preclinical	NAMPT inhibitor	NAMPT|SLC2A1		
STF-62247	Preclinical	autophagy inducer			
stigmasterol	Preclinical				
stiripentol	Launched	GABA uptake inhibitor	GABRA3	neurology/psychiatry	epilepsy
stobadine	Phase 2	adrenergic receptor antagonist	ADRA1A		
streptomycin	Launched	bacterial 30S ribosomal subunit inhibitor		infectious disease	tuberculosis
streptozotocin	Launched	DNA alkylating agent		oncology	pancreatic cancer
strontium-ranelate	Launched	bone formation stimulant|bone resorption inhibitor	CASR	orthopedics|rheumatology	osteoporosis|osteoarthritis
strychnine	Preclinical	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|CHRNA10|CHRNA9|GLRA1|GLRA2|GLRA3|GLRB		
substance-P	Phase 1	neurokinin receptor antagonist	TACR1|TACR2|TACR3		
succinic-acid	Launched		ALDH5A1|ASPH|BBOX1|HSD17B6|OXCT1|OXCT2|P3H1|P3H2|P3H3|P4HA1|P4HA2|PLOD1|PLOD3|SDHA|SDHB|SDHC|SDHD|SLC13A1|SLC13A2|SLC13A3|SLC25A10|SUCLA2|SUCLG1|SUCLG2|SUCNR1|TMLHE		
succinobucol	Phase 2/Phase 3	antioxidant	VCAM1		
succinylcholine-chloride	Launched		CHRFAM7A|CHRM1|CHRM2|CHRM3|CHRNA1|CHRNA10	neurology/psychiatry	muscle relaxant
succinylsulfathiazole	Phase 2	dihydrofolate reductase inhibitor	DHFR		
sucralfate	Launched	antacid		gastroenterology	duodenal ulcer disease
sucralose	Launched				
sucrose	Launched		ACTA1|ATOX1|C22orf28|LYZ		
sucrose-octaacetate	Preclinical				
sudan-IV	Preclinical				
sufugolix	Preclinical	gonadotropin releasing factor hormone receptor antagonist			
sugammadex	Launched	neuromuscular blockade reversal agent			
sulbactam	Launched	beta lactamase inhibitor		infectious disease	skin infections|intra-abdominal infections|gynecologic infections
sulbactam-pivoxil	Launched	beta lactamase inhibitor		infectious disease	skin infections
sulbentine	Preclinical	other antifungal			
sulbutiamine	Launched	acetylcholine receptor antagonist		neurology/psychiatry	asthenia
sulconazole	Launched	sterol demethylase inhibitor		infectious disease	tinea pedis|tinea cruris|tinea corporis
sulfabenzamide	Launched	bacterial antifolate		infectious disease	gram-negative bacterial infections|gram-positive bacterial infections
sulfacarbamide	Withdrawn				
sulfacetamide	Launched	PABA antagonist		ophthalmology	conjunctivitis
sulfachlorpyridazine	Launched	bacterial antifolate		infectious disease	urinary tract infections
sulfadiazine	Launched	bacterial antifolate		infectious disease|ophthalmology	malaria|meningitis|urinary tract infections|conjunctivitis|trachoma|chancroid
sulfadoxine	Launched	dihydropteroate synthase inhibitor		infectious disease	malaria
sulfafurazole	Launched	bacterial antifolate		infectious disease	urinary tract infections
sulfaguanidine	Launched	bacterial antifolate		infectious disease	urinary tract infections
sulfamerazine	Launched	bacterial antifolate		infectious disease	coccidiosis|cholera
sulfameter	Launched	dihydrofolate reductase inhibitor	DHFR	infectious disease	urinary tract infections
sulfamethazine	Launched	PABA antagonist		gastroenterology	enteritis
sulfamethizole	Launched	bacterial antifolate		infectious disease	urinary tract infections
sulfamethoxazole	Launched	PABA antagonist		infectious disease|gastroenterology	pneumonia|enteritis|urinary tract infections
sulfamethoxypyridazine	Withdrawn	bacterial antifolate			
sulfametopyrazine	Launched	PABA antagonist		infectious disease	malaria|urinary tract infections|respiratory tract infections
sulfamonomethoxine	Launched	bacterial antifolate		infectious disease	urinary tract infections
sulfamoxole	Launched	PABA antagonist		infectious disease	urinary tract infections
sulfanilamide	Launched	carbonic anhydrase inhibitor	CYP2C19|CYP2C9|CYP2D6|CYP2E1|CYP3A4	infectious disease	vulvovaginal candidiasis
sulfanilate-zinc	Preclinical				
sulfanitran	Launched			infectious disease	coccidiosis
sulfaphenazole	Launched	dihydropteroate synthetase inhibitor	DHPS	infectious disease	urinary tract infections
sulfapyridine	Launched	PABA antagonist		infectious disease	gram-negative bacterial infections|gram-positive bacterial infections
sulfaquinoxaline	Launched	vitamin K antagonist		infectious disease	coccidiosis
sulfasalazine	Launched	cyclooxygenase inhibitor	ACAT1|ALOX5|CHUK|IKBKB|PLA2G1B|PPARG|PTGS1|PTGS2|SLC46A1|SLC7A11|TBXAS1	gastroenterology	ulcerative colitis
sulfathiazole	Launched	dihydropteroate synthase inhibitor		infectious disease	gram-negative bacterial infections|gram-positive bacterial infections
sulfatinib	Phase 1	tyrosine kinase inhibitor			
sulfinpyrazone	Launched	uricosuric blocker	ABCC1|FPR1|SLC22A12	rheumatology	gout
sulfisomidin	Preclinical	antibacterial			
sulfisoxazole-acetyl	Launched	folic acid antagonist		infectious disease|otolaryngology	meningitis|urinary tract infections|otitis|trachoma
sulforaphane	Phase 2	anticancer agent|aryl hydrocarbon receptor antagonist	NFE2L2		
sulindac	Launched	cyclooxygenase inhibitor	AKR1B1	rheumatology	osteoarthritis|rheumatoid arthritis|ankylosing spondylitis
sulisobenzone	Launched			dermatology	sunscreen lotion
sulmazole	Phase 1	adenosine receptor antagonist			
sulmetozine	Launched	gastrin inhibitor	GAST	gastroenterology	peptic ulcer disease (PUD)
suloctidil	Withdrawn	adrenergic receptor antagonist			
sulopenem	Phase 3	antibacterial			
sulphadimethoxine	Launched	dihydropteroate synthetase inhibitor		infectious disease	gram-negative bacterial infections|gram-positive bacterial infections
sulpiride	Launched	dopamine receptor antagonist		neurology/psychiatry	schizophrenia
sultamicillin	Launched	antibacterial 		infectious disease	gram-negative bacterial infections|gram-positive bacterial infections
sultiame	Phase 3	carbonic anhydrase inhibitor	CA2		
sultopride	Preclinical	dopamine receptor antagonist			
sumanirole	Phase 3	dopamine receptor agonist	DRD2		
sumatriptan	Launched	serotonin receptor agonist	HTR1A|HTR1B|HTR1D|HTR1E|HTR1F|HTR5A|HTR6|HTR7	neurology/psychiatry	migraine headache
SUN-B-8155	Preclinical	calcitonin agonist	CALCR		
SUN-11602	Preclinical	fibroblast growth factor mimetic	FGFR1		
sunitinib	Launched	FLT3 inhibitor|KIT inhibitor|PDGFR tyrosine kinase receptor inhibitor|RET tyrosine kinase inhibitor|VEGFR inhibitor	CSF1R|FGFR1|FLT1|FLT3|FLT4|KDR|KIT|PDGFRA|PDGFRB|RET	oncology	gastrointestinal stromal tumors (GIST)|renal cell carcinoma (RCC)|neuroendocrine tumors of pancreatic origin (PNET)
suplatast	Launched	histamine release inhibitor|immunoglobulin inhibitor		rheumatology	Kimura's disease
suprofen	Withdrawn	cyclooxygenase inhibitor	PTGS1|PTGS2		
suramin	Launched	DNA synthesis inhibitor	F2|FSHR|P2RY1|P2RY11|P2RY13|P2RY2|PLA2G2A|RYR1|RYR2|SIRT5	infectious disease	African trypanosomiasis|onchocerciasis
suritozole	Phase 2	GABA receptor inverse agonist	GABBR1		
sutezolid	Phase 2	protein synthesis inhibitor			
suxibuzone	Launched	cyclooxygenase inhibitor		rheumatology|neurology/psychiatry	joint pain|muscle pain
SU014813	Phase 2	PDGFR tyrosine kinase receptor inhibitor|VEGFR inhibitor	KDR		
SU11274	Preclinical	hepatocyte growth factor receptor inhibitor|tyrosine kinase inhibitor	MET		
SU16f	Preclinical	PDGFR tyrosine kinase receptor inhibitor	PDGFRB		
SU3327	Preclinical	JNK inhibitor	MAPK8		
SU4312	Preclinical	PDGFR tyrosine kinase receptor inhibitor|tyrosine kinase inhibitor|VEGFR inhibitor	KDR|PDGFRB		
SU9516	Preclinical	CDK inhibitor	CDK1|CDK2|CDK4|CDK5		
swainsonine	Phase 2	alpha mannosidase inhibitor	MAN2A1		
SX-011	Preclinical	MAP kinase inhibitor	MAPK14		
SY-640	Phase 2				
SYM-2081	Preclinical	kainate receptor antagonist	GRIK1|GRIK2|GRIK3|GRIK4|GRIK5|SLC1A2		
SYM-2206	Preclinical	glutamate receptor antagonist	GRIA1|GRIA2|GRIA3|GRIA4		
symclosene	Preclinical				
synephrine	Launched	adrenergic receptor agonist	ADRA1A	otolaryngology	sinusitis
S1P1-agonist-III	Preclinical	sphingosine kinase inhibitor	S1PR1		
S15535	Preclinical	serotonin receptor agonist			
S18986	Phase 2	glutamate receptor modulator	GRIA1|GRIA2|GRIA3|GRIA4		
S26948	Preclinical	PPAR receptor agonist	PPARG		
S4	Preclinical	carbonic anhydrase inhibitor	CA12|CA9		
S49076	Preclinical	tyrosine kinase inhibitor			
S63845	Preclinical	MCL1 inhibitor			
T-0070907	Preclinical	PPAR receptor antagonist	PPARG		
T-0156	Preclinical	phosphodiesterase inhibitor	PDE5A		
T-025	Preclinical	CLK inhibitor			
T-0901317	Preclinical	LXR agonist	NCOA1|NCOA2|NR1H2|NR1H3|NR1I2|RXRB		
T-1095	Preclinical	sodium/glucose cotransporter inhibitor			
T-5224	Phase 2	AP inhibitor	JUN		
T-5601640	Preclinical	LIM kinase inhibitor	LIMK2		
T-62	Phase 2	adenosine receptor modulator	ADORA2A		
T-807	Phase 2	PET radiotracer			
TA-01	Preclinical	casein kinase inhibitor|MAP kinase inhibitor	CSNK1D|CSNK1E|MAPK14		
tabimorelin	Phase 2	growth hormone secretagogue receptor agonist	GHSR		
tacalcitol	Launched	vitamin D receptor agonist	VDR	dermatology	psoriasis|chapped lips
tacedinaline	Phase 3	HDAC inhibitor	HDAC1		
tacrine	Launched	acetylcholinesterase inhibitor	ACHE|BCHE	neurology/psychiatry	Alzheimer's disease
tacrolimus	Launched	calcineurin inhibitor	FKBP1A	transplant	organ rejection
tadalafil	Launched	phosphodiesterase inhibitor	PDE11A|PDE5A	urology	erectile dysfunction
tafamidis-meglumine	Launched	transthyretin amyloid inhibitor	TTR	neurology/psychiatry	familial amyloid polyneuropathy (FAP)
tafenoquine	Launched	antimalarial agent		infectious disease	malaria
tafluprost	Launched	prostaglandin inhibitor	PTGFR	ophthalmology	glaucoma|ocular hypertension
tagatose	Launched	phosphorylase inhibitor	PYGL		
TAK-063	Phase 2	phosphodiesterase inhibitor	PDE10A		
TAK-220	Phase 1	CC chemokine receptor antagonist	CCR5		
TAK-243	Phase 1	ubiquitin activating enzyme inhibitor			
TAK-285	Phase 1	EGFR inhibitor	ERBB2		
TAK-593	Phase 1	VEGFR inhibitor	PDGFRA		
TAK-632	Preclinical	RAF inhibitor	BRAF		
TAK-659	Phase 2	spleen associated tyrosine kinase inhibitor			
TAK-715	Phase 2	p38 MAPK inhibitor	MAPK14		
TAK-733	Phase 1	MEK inhibitor	MAP2K1		
TAK-779	Preclinical	CC chemokine receptor antagonist			
TAK-875	Phase 3	insulin secretagogue	FFAR1		
TAK-901	Phase 1	Aurora kinase inhibitor	AURKB		
TAK-960	Phase 1	PLK inhibitor	PLK1		
talabostat	Phase 3	dipeptidyl peptidase inhibitor|fibroblast activation protein inhibitor	DPP4		
taladegib	Phase 2	smoothened receptor antagonist	DHH|IHH|SMO		
talampanel	Phase 2	glutamate receptor antagonist	GRIA1|GRIA2|GRIA3|GRIA4		
talaporfin	Phase 3	photosensitizing agent			
talarozole	Phase 2	cytochrome P450 inhibitor	CYP26A1		
talazoparib	Launched	PARP inhibitor	PARP2	oncology	breast cancer
talinolol	Launched	adrenergic receptor antagonist	ADRB1	cardiology	hypertension
talipexole	Launched	adrenergic receptor agonist|dopamine receptor agonist	ADRA2A|DRD2|HTR3A	infectious disease	genitial herpes
talmapimod	Phase 2	p38 MAPK inhibitor	IL1B|MAPK11|MAPK14|MT-CO2|TNF		
talnetant	Phase 2	tachykinin antagonist	TACR2|TACR3		
talniflumate	Launched	cyclooxygenase inhibitor	CLCA1	neurology/psychiatry	pain relief
talopram	Phase 2	adrenergic inhibitor	SLC6A2		
talsaclidine	Phase 2/Phase 3	acetylcholine receptor agonist			
taltirelin	Launched	thyrotropin releasing hormone receptor agonist	TRHR	neurology/psychiatry	spinocerebellar ataxia
taltobulin	Phase 1	tubulin polymerization inhibitor			
TAME	Preclinical				
tamibarotene	Launched	retinoid receptor agonist	RARA|RARB	hematologic malignancy	acute promyelocytic leukemia (APL)
taminadenant	Phase 1/Phase 2	adenosine receptor antagonist			
tamoxifen	Launched	estrogen receptor antagonist|selective estrogen receptor modulator (SERM)	EBP|ESR1|ESR2|GPER1|PRKCA|PRKCB|PRKCD|PRKCE|PRKCG|PRKCI|PRKCQ|PRKCZ	oncology	breast cancer
tamsulosin	Launched	adrenergic receptor antagonist	ADRA1A|ADRA1B|ADRA1D	urology	benign prostatic hyperplasia (BPH)
tanaproget	Phase 2	progesterone receptor agonist	PGR		
tandospirone	Launched	serotonin receptor agonist	HTR1A	neurology/psychiatry	generalized anxiety disorder (GAD)|dysthymic disorder
tandutinib	Phase 2	FLT3 inhibitor|KIT inhibitor|PDGFR tyrosine kinase receptor inhibitor	CSF1R|FLT3|KIT|PDGFD|PDGFRB		
tanespimycin	Phase 3	HSP inhibitor	HSP90AA1		
tangeritin	Preclinical	cell cycle inhibitor			
tannic-acid	Launched	PARG inhibitor	ANO1	gastroenterology	constipation
tanshinone-I	Phase 2	AP inhibitor	IFNG		
tanshinone-IIA	Phase 2/Phase 3	anti-inflammatory agent|interleukin inhibitor	IL1B|NR1I2|TNF		
tapinarof	Phase 3	aryl hydrocarbon receptor agonist			
taprenepag	Phase 2	prostaglandin receptor agonist	PTGER2		
tarafenacin	Phase 2	acetylcholine receptor antagonist	CHRM3		
taranabant	Phase 3	cannabinoid receptor inverse agonist	CNR1		
targinine	Phase 3	nitric oxide synthase inhibitor	NOS3		
tariquidar	Phase 3	P glycoprotein inhibitor	ABCB1		
tartaric-acid	Launched	antioxidant			
TAS-103	Phase 1	topoisomerase inhibitor	TOP1		
taselisib	Phase 3	PI3K inhibitor	PIK3CA		
tasimelteon	Launched	melatonin receptor agonist	MTNR1A|MTNR1B	neurology/psychiatry	Non-24-Hour Sleep-Wake Disorder
tasisulam	Phase 3	apoptosis stimulant			
tasquinimod	Phase 3	angiogenesis inhibitor|S100A9 inhibitor	HDAC4		
tasuldine	Phase 3	mucolytic agent			
taurine	Launched	antioxidant		neurology/psychiatry	anxiety|irritability|sleeplessness
taurocholate	Phase 1	G protein-coupled receptor agonist	CEL|FABP6|SLCO1C1		
tauroglycocholate	Preclinical	membrane permeability enhancer			
taurolidine	Launched	apoptosis stimulant		infectious disease	catheter-related bloodstream infection
tavaborole	Launched	leucyl-tRNA synthetase inhibitor		infectious disease	onychomycosis
tavilermide	Phase 3	tyrosine kinase partial agonist			
taxifolin	Phase 2	opioid receptor antagonist	ADIPOR2		
tazarotene	Launched	retinoid receptor agonist	RARA|RARB|RARG|RXRB	dermatology	cosmetic|sunscreen lotion
tazemetostat	Launched	histone lysine methyltransferase inhibitor	EZH2		
tazobactam	Launched	beta lactamase inhibitor		infectious disease	pneumonia
TBA-354	Phase 1				
TBOA-(DL)	Preclinical	excitatory amino acid transporter inhibitor	SLC1A1|SLC1A2|SLC1A3|SLC1A6|SLC1A7		
TC-A-2317	Preclinical	Aurora kinase inhibitor	AURKA		
TC-ASK-10	Preclinical	MAP kinase inhibitor	MAP3K5|MAP3K6		
TC-E-5002	Preclinical	histone demethylase inhibitor	KDM2A|KDM4A|KDM4C|KDM5A|KDM6A|KDM7A|PHF8		
TC-E-5006	Preclinical	gamma secretase modulator	APP		
TC-F-2	Preclinical	FAAH inhibitor	FAAH		
TC-FPR-43	Preclinical	formyl peptide receptor agonist	FPR2		
TC-G-1000	Preclinical	adrenergic receptor agonist	ADRA2A|ADRA2B|ADRA2C		
TC-G-1004	Preclinical	adenosine receptor antagonist	ADORA2A		
TC-G-1005	Preclinical	G protein-coupled receptor agonist	GPBAR1		
TC-G-1008	Preclinical	G protein-coupled receptor agonist	GPR39		
TC-H-106	Preclinical	HDAC inhibitor	HDAC1|HDAC2|HDAC3|HDAC8		
TC-I-15	Preclinical	integrin inhibitor	ITGA2|ITGB1		
TC-I-2000	Preclinical	transient receptor potential channel antagonist	TRPM8		
TC-I-2014	Preclinical	transient receptor potential channel antagonist	TRPM8		
TC-LPA5-4	Preclinical	lysophosphatidic acid receptor antagonist	LPAR5		
TC-Mps1-12	Preclinical	monopolar spindle 1 kinase inhibitor	TTK		
TC-N-1752	Preclinical	sodium channel blocker	SCN9A		
TC-NTR1-17	Preclinical	neurotensin agonist	NTSR1		
TC-O-9311	Preclinical	G protein-coupled receptor agonist	GPR139		
TC-OT-39	Preclinical	oxytocin receptor agonist|vasopressin receptor agonist	AVPR1A|OXT		
TC-S-7003	Preclinical	SRC inhibitor	LCK		
TC-S-7004	Preclinical	DYRK inhibitor	DYRK1A|DYRK1B		
TC-S-7005	Preclinical	PLK inhibitor	PLK2		
TC-S-7006	Preclinical	MAP kinase inhibitor	MAP3K8		
TC-S-7009	Preclinical	hypoxia inducible factor inhibitor	EPAS1		
TC-SP-14	Preclinical	sphingosine 1-phosphate receptor agonist	S1PR1		
TCID	Preclinical				
TCN201	Preclinical	glutamate receptor antagonist	GRIN2A		
TCN238	Preclinical	glutamate receptor positive allosteric modulator	GRM4		
TCS-HDAC6-20b	Preclinical	HDAC inhibitor	HDAC6		
TCS-OX2-29	Preclinical	orexin receptor antagonist	HCRTR2		
TCS-PIM-1-1	Preclinical	Pim kinase inhibitor	PIM1		
TCS-2002	Preclinical	glycogen synthase kinase inhibitor	GSK3B		
TCS-21311	Preclinical	JAK inhibitor	JAK3		
TCS-2210	Preclinical	neural stem cell inducer			
TCS-2314	Preclinical	integrin inhibitor	ITGA4|ITGB1		
TCS-3035	Preclinical	G protein-coupled receptor agonist	GPR35		
TCS-359	Preclinical	FLT3 inhibitor	FLT3		
TCS-5861528	Preclinical	transient receptor potential channel antagonist	TRPA1		
TCV-309	Preclinical	platelet activating factor receptor antagonist			
TC1	Preclinical	beta-secretase inhibitor	BACE1		
TC2559	Preclinical	acetylcholine receptor agonist	CHRNA4		
TD139	Phase 2	anti-inflammatory agent			
tebipenem	Launched	bacterial cell wall synthesis inhibitor	CNR1	infectious disease|otolaryngology	pneumonia|otitis
tecadenoson	Phase 2	adenosine receptor agonist	ADORA1		
tecalcet	Phase 2	calcium-sensing receptor agonist	CASR		
tecastemizole	Phase 3	histamine receptor antagonist	KCNH2		
tecovirimat	Launched	orthopoxvirus egress inhibitor		infectious disease	smallpox
tedizolid	Launched	bacterial 50S ribosomal subunit inhibitor		infectious disease	skin infections
tedizolid-phosphate	Launched	protein synthesis inhibitor		infectious disease	skin infections
tegaserod	Withdrawn	serotonin receptor partial agonist	HTR2A|HTR2B|HTR2C|HTR4		
tegobuvir	Phase 3	HCV inhibitor|protease inhibitor			
teicoplanin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-positive bacterial infections
teicoplanin-A2-1	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-positive bacterial infections
teicoplanin-A2-3	Launched	bacterial cell wall synthesis inhibitor		infectious disease	gram-positive bacterial infections
teijin-compound-1	Preclinical	CC chemokine receptor antagonist	CCR2		
telaprevir	Launched	HCV inhibitor	CTSA|PGR	infectious disease	hepatitis C
telatinib	Phase 2	KIT inhibitor|PDGFR tyrosine kinase receptor inhibitor|VEGFR inhibitor	KDR		
telbivudine	Launched	DNA polymerase inhibitor		infectious disease	hepatitis B
telcagepant	Phase 3	calcitonin antagonist	CALCRL|RAMP1		
telenzepine	Phase 3	acetylcholine receptor antagonist	CHRM1		
telithromycin	Launched	bacterial 30S ribosomal subunit inhibitor|bacterial 50S ribosomal subunit inhibitor	CYP1A2|CYP2D6|CYP3A4|CYP3A5|CYP3A7	infectious disease	pneumonia
telmesteine	Launched	mucolytic agent		pulmonary	cough suppressant
telmisartan	Launched	angiotensin receptor antagonist	AGTR1|PPARG	cardiology	hypertension
telotristat	Launched	tryptophan hydroxylase inhibitor	TPH1	gastroenterology	diarrhea
telotristat-ethyl	Launched	tryptophan hydroxylase inhibitor	TPH1	gastroenterology	diarrhea
telratolimod	Preclinical	toll-like receptor agonist			
temanogrel	Preclinical	serotonin receptor antagonist			
temefos	Launched	cholinesterase inhibitor			
temocapril	Launched	angiotensin converting enzyme inhibitor	ACE	cardiology|nephrology	hypertension|congestive heart failure|diabetic nephropathy|coronary artery disease (CAD)
temoporfin	Launched	radical formation stimulant		oncology	head and neck squamous cell carcinoma (HNSCC)
temozolomide	Launched	DNA alkylating agent	MGMT	oncology	glioblastoma|astrocytoma
tempol	Phase 2	free radical scavenger			
temsirolimus	Launched	mTOR inhibitor	MTOR	oncology	renal cell carcinoma (RCC)
TEN-010	Preclinical	bromodomain inhibitor			
tenalisib	Phase 2	PI3K inhibitor			
tenapanor	Launched	sodium/hydrogen exchanger inhibitor			
tenatoprazole	Phase 2	ATPase inhibitor	IDO1		
teneligliptin	Launched	dipeptidyl peptidase inhibitor	DPP4	endocrinology	diabetes mellitus
tenidap	Phase 3	cyclooxygenase inhibitor	KCNJ4|PTGS1		
tenilsetam	Phase 3	AGE inhibitor			
teniposide	Launched	topoisomerase inhibitor	TOP2A|TOP2B	hematologic malignancy	acute lymphoblastic leukemia (ALL)
tenofovir	Launched	HIV integrase inhibitor|nucleoside reverse transcriptase inhibitor		infectious disease	human immunodeficiency virus (HIV-1)|hepatitis B
tenofovir-alafenamide	Launched	nucleoside reverse transcriptase inhibitor		infectious disease	hepatitis B
tenofovir-disoproxil	Launched	nucleoside reverse transcriptase inhibitor	CYP1A2	infectious disease	human immunodeficiency virus (HIV-1)|hepatitis B
tenovin-1	Preclinical	SIRT inhibitor|TP53 activator	SIRT1		
tenovin-6	Preclinical	SIRT inhibitor	SIRT1|SIRT2|SIRT3		
tenoxicam	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	rheumatology|orthopedics	rheumatoid arthritis|osteoarthritis|ankylosing spondylitis|tendinitis|bursitis|periarthritis
tenylidone	Preclinical				
tepoxalin	Launched	cyclooxygenase inhibitor|lipoxygenase inhibitor	ALOX5	rheumatology|orthopedics	rheumatoid arthritis|hip dysplasia
TEPP-46	Preclinical	pyruvate kinase isozyme activator	PKM		
teprenone	Launched	mucus protecting agent		dermatology	cosmetic
terameprocol	Phase 1/Phase 2	lipoxygenase inhibitor	BIRC5|CDK1		
terazosin	Launched	adrenergic receptor antagonist	ADRA1A|ADRA1B|ADRA1D	urology|cardiology	benign prostatic hyperplasia (BPH)|hypertension
terbinafine	Launched	fungal squalene epoxidase inhibitor	SQLE	infectious disease	tinea pedis|tinea cruris|tinea corporis
terbutaline	Launched	adrenergic receptor agonist	ADRB2	pulmonary	bronchospasm|bronchitis|emphysema
terciprazine	Phase 1				
terconazole	Launched	sterol demethylase inhibitor		infectious disease	vulvovaginal candidiasis
terfenadine	Withdrawn	histamine receptor antagonist	HRH1|KCNH1|KCNH2		
terguride	Launched	dopamine receptor agonist|serotonin receptor antagonist	ADRA1A|ADRA2A|ADRA2B|ADRA2C|DRD2|DRD3|DRD4|HTR1A|HTR1B|HTR1D|HTR2A|HTR2B|HTR2C	neurology/psychiatry	Parkinson's Disease
teriflunomide	Launched	dihydroorotate dehydrogenase inhibitor	DHODH	neurology/psychiatry	multiple sclerosis
terlipressin	Launched	vasopressin receptor agonist	AVPR1A	cardiology	hypotension
terodiline	Withdrawn	cholinergic receptor antagonist			
teroxirone	Phase 1	DNA inhibitor			
terpene	Preclinical				
terreic-acid-(-)	Preclinical	Bruton's tyrosine kinase (BTK) inhibitor	BTK		
terutroban	Phase 3	prostanoid receptor antagonist	TBXA2R		
tesaglitazar	Phase 3	insulin sensitizer|PPAR receptor agonist	PPARA|PPARG		
tetomilast	Phase 2	phosphodiesterase inhibitor	PDE4D		
tetrabenazine	Launched	vesicular monoamine transporter inhibitor	SLC18A1|SLC18A2	infectious disease|neurology/psychiatry	cholera|Huntington's disease
tetracaine	Launched	membrane integrity inhibitor	SCN10A|SCN11A|SCN1A|SCN2A|SCN3A|SCN4A|SCN5A|SCN7A|SCN8A|SCN9A	neurology/psychiatry	anesthetic
tetracycline	Launched	bacterial 30S ribosomal subunit inhibitor		infectious disease|dermatology	respiratory tract infections|pneumonia|skin infections|urinary tract infections|acne vulgaris (AV)|plague|psittacosis
tetradecylthioacetic-acid	Phase 2	lipid peroxidase inhibitor			
tetraethylenepentamine	Phase 2/Phase 3	superoxide dismutase inhibitor	SOD1|SOD2		
tetrahydrofolic-acid	Launched		FOLR2		
tetrahydropapaverine	Preclinical				
tetrahydrouridine	Phase 2	cytidine deaminase inhibitor	CDA		
tetrahydrozoline	Launched	adrenergic receptor agonist		ophthalmology	eye irritation
tetramethylthiuram-monosulfide	Preclinical				
tetramisole	Launched	immunostimulant	ALPPL2|CHRNA3	infectious disease	gastrointestinal parasites
tetrandrine	Preclinical	calcium channel blocker	SLC6A3		
tetrazol-5-yl-glycine-(RS)	Preclinical	glutamate receptor agonist	GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D		
tetrindole	Phase 3	monoamine oxidase inhibitor	MAOA		
tetroquinone	Preclinical				
tezacaftor	Launched	CFTR channel agonist		pulmonary	cystic fibrosis
TFC-007	Preclinical	prostaglandin inhibitor	HPGDS		
TG-003	Preclinical	CLK inhibitor	CLK1|CLK4|DYRK1A|DYRK1B		
TG-02	Phase 1/Phase 2	CDK inhibitor|FLT3 inhibitor|JAK inhibitor	CDK1|CDK2|CDK7|CDK9|FLT3|JAK2		
TG-100572	Preclinical	SRC inhibitor|VEGFR inhibitor	KDR|SRC		
TG-100713	Preclinical	PI3K inhibitor			
TG-100801	Phase 2	SRC inhibitor|VEGFR inhibitor	CSK|FGFR1|FLT1|FLT4|KDR|SRC		
TG-101209	Preclinical	JAK inhibitor	JAK2|JAK3		
TGR-1202	Phase 3	PI3K inhibitor			
TGX-221	Preclinical	PI3K inhibitor	PIK3CB|PIK3CD		
TG100-115	Phase 1/Phase 2	PI3K inhibitor	PIK3CA|PIK3CB|PIK3CD|PIK3CG		
TH-302	Phase 3	DNA alkylating agent			
TH-588	Preclinical	MTH1 inhibitor	NUDT1		
thaliblastine	Phase 2	DNA inhibitor			
thalidomide	Launched	tumor necrosis factor production inhibitor	TNF	oncology	myeloma
theaflavin	Preclinical	antiviral			
theobromine	Launched	phosphodiesterase inhibitor	ADORA1|ADORA2A|PDE4B		
thiamet-g	Preclinical	GLCNAC phosphotransferase inhibitor	MGEA5		
thiamine	Launched	vitamin B	SLC19A2|SLC19A3|TPK1	metabolism	thiamine deficiency
thiamine-pyrophosphate	Launched			hematology	anemia
thiamphenicol	Launched	bacterial 50S ribosomal subunit inhibitor		infectious disease	pelvic inflammatory disease
thiamylal	Launched	glutamate receptor antagonist	GABRA1	neurology/psychiatry	sedative
thiazovivin	Preclinical	rho associated kinase inhibitor			
thiethylperazine	Launched	dopamine receptor antagonist	DRD1|DRD2|DRD4	gastroenterology	nausea
thiocolchicoside	Launched	GABA receptor antagonist	GABRA1|GABRB2|GABRG2|GLRA1|GLRB	neurology/psychiatry	muscle relaxant
thioctic-acid	Launched	reducing agent	ACHE|PTGS2	nephrology	diabetic nephropathy
thiodiglycol	Preclinical				
thioguanine	Launched	purine antagonist	IMPDH1|IMPDH2	hematologic malignancy	acute myeloid leukemia (AML)
thiomersal	Launched	other antibiotic	OXCT1	infectious disease	preservative
thiopental	Launched	GABA receptor antagonist	FAAH	neurology/psychiatry	anesthetic
thioperamide	Preclinical	histamine receptor antagonist	HRH3|HRH4		
thiophanate	Preclinical				
thioproperazine	Launched	dopamine receptor antagonist	ADRA1A|ADRA1B|DRD1|DRD2|HTR1A|HTR2A	neurology/psychiatry	schizophrenia
thioridazine	Withdrawn	dopamine receptor antagonist	DRD1|DRD2|DRD3|DRD4|DRD5|HRH1|HTR1A|HTR2A|HTR2C|HTR6|HTR7		
thiorphan	Phase 1	membrane metalloendopeptidase inhibitor	MME		
thiostrepton	Launched	FOXM1 inhibitor|protein synthesis inhibitor	FOXM1	obstetrics/gynecology	mastitis
thiotepa	Launched	cytochrome P450 inhibitor	CYP2B6|CYP3A4	oncology	breast cancer|ovarian cancer|bladder cancer
thiothixene	Launched	dopamine receptor antagonist	DRD1|DRD2|HRH1|HTR2A	neurology/psychiatry	schizophrenia
thiram	Launched		JAK2	ophthalmology	contact dermatitis
THK5351	Phase 2	PET radiotracer 			
thonzonium	Launched	ATPase inhibitor		infectious disease	ear infections
thonzylamine	Launched	antihistamine		neurology/psychiatry	itching
threo-2-methylisocitrate-(DL)	Preclinical	isocitrate lyase substrate			
thymalfasin	Launched	immune response modulator		infectious disease	hepatitis B|hepatitis C
thymol	Launched	GABA receptor positive allosteric modulator	TRPA1	infectious disease	ringworm|antiseptic
thymol-iodide	Preclinical				
thymopentin	Launched	immune response stimulator			
THZ1	Preclinical	CDK inhibitor	CDK7		
THZ1-R	Preclinical	CDK inhibitor	CDK7		
THZ2	Preclinical	CDK inhibitor	CDK7		
tiabendazole	Launched	angiogenesis inhibitor		infectious disease	gastrointestinal roundworms|hookworm
tiagabine	Launched	GABA uptake inhibitor	SLC6A1	neurology/psychiatry	seizures
tianeptine	Launched	selective serotonin reuptake enhancer (SSRE)	OPRD1|OPRK1|OPRM1	neurology/psychiatry|pulmonary|gastroenterology	depression|asthma|irritable bowel syndrome
tiapride	Launched	dopamine receptor antagonist	DRD2|DRD3	neurology/psychiatry	dyskinesia|abstinence from alcohol|psychosis
tiaprofenic-acid	Launched	cyclooxygenase inhibitor	PTGS2	rheumatology	rheumatoid arthritis
tiaramide	Launched	anti-inflammatory agent		pulmonary	asthma
tibolone	Launched	androgen receptor agonist|estrogen receptor agonist|progesterone receptor agonist	ESR1	obstetrics/gynecology	endometriosis
ticagrelor	Launched	purinergic receptor antagonist	P2RY12	cardiology	acute coronary syndrome (ACS)|myocardial infarction
ticarcillin	Launched	lactamase inhibitor		infectious disease	gram-negative bacterial infections
ticlopidine	Launched	purinergic receptor antagonist	P2RY12	hematology|neurology/psychiatry	thrombosis|stroke
TIC10	Phase 2	AKT inhibitor|TRAIL modulator	AKT1|MAPK1		
tideglusib	Phase 2	glycogen synthase kinase inhibitor	GSK3B		
tienilic-acid	Withdrawn	cytochrome P450 inhibitor|sodium/potassium/chloride transporter inhibitor	CYP2C9|SLC12A1		
tie2-kinase-inhibitor	Preclinical	TIE tyrosine kinase inhibitor	KDR|MAPK14		
tifenazoxide	Phase 1	ATP-sensitive potassium channel agonist	ABCC8|KCNJ11		
tigecycline	Launched	bacterial 30S ribosomal subunit inhibitor		infectious disease	skin infections|pneumonia|intra-abdominal infections
tilmicosin	Launched	bacterial 50S ribosomal subunit inhibitor		pulmonary	bovine respiratory disease (BRD)
tilorone	Launched	interferon inducer		infectious disease|gastroenterology|neurology/psychiatry	influenza A virus infection|diarrhea|hepatitis B|multiple sclerosis|urinary tract infections|virus herpes simplex (HSV)|hepatitis C
tiludronate	Launched	bone resorption inhibitor|osteoclast inhibitor	ATP6V1A|MMP2|PTPN1	orthopedics	navicular syndrome
timofibrate	Phase 2	cholesterol inhibitor|lipase clearing factor inhibitor	LPL		
timolol	Launched	adrenergic receptor antagonist	ADRB1|ADRB2	ophthalmology	ocular hypertension|glaucoma
timonacic	Launched	antioxidant			
tinazoline	Launched	adrenergic receptor agonist			
tinidazole	Launched	antiprotozoal agent		infectious disease|obstetrics/gynecology	giardiasis|amebiasis|bacterial vaginosis|trichomoniasis
tinoridine	Launched	anti-inflammatory agent		neurology/psychiatry	pain relief
tioconazole	Launched	sterol demethylase inhibitor		infectious disease	yeast infection
tioguanine	Launched	purine antagonist		hematologic malignancy	acute myeloid leukemia (AML)|acute lymphoblastic leukemia (ALL)|chronic myeloid leukemia (CML)
tiopronin	Launched	chelating agent|reducing agent		urology	kidney stones
tiotidine	Phase 2	histamine receptor antagonist	HRH2		
tiotropium	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3	pulmonary	chronic obstructive pulmonary disease (COPD)|bronchitis|emphysema
tioxolone	Preclinical	carbonic anhydrase inhibitor	CA2		
tipelukast	Phase 2	leukotriene receptor antagonist			
tipifarnib	Phase 3	farnesyltransferase inhibitor	FNTA|FNTB		
tipiracil	Launched	thymidine phosphorylase inhibitor		oncology	colorectal cancer
tiplaxtinin	Phase 1	plasminogen activator inhibitor	SERPINE1		
tipranavir	Launched	HIV protease inhibitor		infectious disease	human immunodeficiency virus (HIV-1)
tiprenolol	Phase 2	adrenergic receptor antagonist	ADRB1|ADRB2|ADRB3		
tiquizium	Launched	acetylcholine receptor antagonist		neurology/psychiatry	spasms
tiracizine	Withdrawn	sodium channel blocker	SCN5A		
tirapazamine	Phase 3	DNA inhibitor			
tirasemtiv	Phase 2	troponin activator			
tiratricol	Launched	thyroid hormone stimulant	THRA|THRB	endocrinology	Refetoff syndrome
tirofiban	Launched	platelet aggregation inhibitor|structural glycoprotein antagonist	ITGA2B|ITGB3	cardiology	myocardial infarction|refactory angina
titanocene-dichloride	Phase 2	apoptosis stimulant			
tivantinib	Phase 3	tyrosine kinase inhibitor	MET		
tivozanib	Launched	VEGFR inhibitor	FLT1|FLT4|KDR|KIT|PDGFRA|PDGFRB	oncology	renal cell carcinoma (RCC)
tizanidine	Launched	adrenergic receptor agonist	ADRA2A|ADRA2B|ADRA2C|NISCH	neurology/psychiatry	spasms
TMC-353121	Phase 2	RSV fusion inhibitor			
TMC647055	Phase 2	RNA polymerase inhibitor			
TMN-355	Preclinical	cyclophilin inhibitor	PPIA		
TMPH	Preclinical				
TMS	Preclinical				
TNP-470	Phase 2	methionine aminopeptidase inhibitor	METAP2		
tobramycin	Launched	bacterial 30S ribosomal subunit inhibitor		infectious disease	bacterial septicemia|respiratory tract infections|meningitis|skin infections|urinary tract infections
tocainide	Launched	sodium channel blocker	SCN5A	cardiology	cardiac arrythmia
toceranib	Launched	protein tyrosine kinase inhibitor	FLT1|FLT3|KDR|PDGFRA|PDGFRB	oncology	cutaneous mast cell tumors
tocofersolan	Launched	antioxidant		cardiology	cerebral cholesterosis
todralazine	Launched	antihypertensive agent		cardiology	hypertension
tofacitinib	Launched	JAK inhibitor	JAK1|JAK2|JAK3	rheumatology	rheumatoid arthritis
tofisopam	Launched	cytochrome P450 inhibitor|phosphodiesterase inhibitor	CYP3A4	neurology/psychiatry	anxiety|abstinence from alcohol
tofogliflozin	Launched	sodium/glucose cotransporter inhibitor	GCK	endocrinology	diabetes mellitus
tolamolol	Phase 3	adrenergic receptor antagonist	ADRB1|ADRB2|ADRB3		
tolazamide	Launched	ATP channel blocker	ABCC8|KCNJ1|KCNJ10|KCNJ11	endocrinology	diabetes mellitus
tolazoline	Launched	adrenergic receptor antagonist	ADRA1A|ADRA2A|ADRA2B|ADRA2C|HRH1|HRH2	neurology/psychiatry	reverse sedative
tolbutamide	Launched	ATP channel blocker	ABCC8|KCNJ1|KCNJ11|KCNJ8	endocrinology	diabetes mellitus
tolcapone	Withdrawn	catechol O methyltransferase inhibitor	COMT		
tolfenamic-acid	Launched	cyclooxygenase inhibitor|prostanoid receptor antagonist		neurology/psychiatry	migraine headache
tolimidone	Phase 2	SRC activator	LYN|SRC		
tolmetin	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	rheumatology	rheumatoid arthritis|osteoarthritis
tolnaftate	Launched	fungal squalene epoxidase inhibitor		infectious disease	tinea pedis|tinea corporis
tolonidine	Launched	adrenergic receptor antagonist	ADRA2A		
tolonium	Launched			hematology	methemoglobinemia
toloxatone	Launched	monoamine oxidase inhibitor	MAOA|MAOB	neurology/psychiatry	depression
tolperisone	Launched	voltage-gated sodium channel blocker	CYP2C19|CYP2D6	neurology/psychiatry|infectious disease|rheumatology|cardiology	muscle relaxant|multiple sclerosis|encephalomyelitis|ankylosing spondylitis|atherosclerosis|Raynaud's disease
tolrestat	Withdrawn	aldose reductase inhibitor	AKR1A1|AKR1B1|AKR1B10		
tolterodine	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5	urology	urinary incontinence|urinary frequency
toltrazuril	Launched	antiprotozoal agent		infectious disease	coccidiosis
tolvaptan	Launched	vasopressin receptor antagonist	AVPR1A|AVPR2	endocrinology|cardiology|gastroenterology	hyponatremia|congestive heart failure|hepatic cirrhosis
tomeglovir	Preclinical	antiviral			
tomelukast	Phase 3	leukotriene receptor antagonist	CYSLTR1		
tomivosertib	Phase 2	MAPK-interacting kinase inhibitor			
tonabersat	Phase 2	gap junction modulator|nitric oxide production inhibitor			
topilutamide	Preclinical	androgen receptor antagonist			
topiramate	Launched	carbonic anhydrase inhibitor|glutamate receptor antagonist|kainate receptor antagonist	CA1|CA12|CA2|CA4|CA7|GABRA1|GABRA2|GABRA3|GABRA4|GABRA5|GABRA6|GABRB1|GABRB2|GABRB3|GABRD|GABRE|GABRG1|GABRG2|GABRG3|GABRP|GABRQ|GRIA1|GRIA2|GRIA3|GRIA4|GRIK1|GRIK2|GRIK3|GRIK4|GRIK5|SCN10A|SCN11A|SCN1A|SCN2A|SCN3A|SCN4A|SCN5A|SCN7A|SCN8A|SCN9A	neurology/psychiatry	epilepsy|migraine headache
topiroxostat	Launched	xanthine oxidase inhibitor	XDH	rheumatology|nephrology	gout|hyperuricemia
topotecan	Launched	topoisomerase inhibitor	TOP1|TOP1MT	oncology	small cell lung cancer|cervical cancer
torasemide	Launched	electrolyte reabsorption inhibitor|thromboxane receptor antagonist	SLC12A1	cardiology	edema|congestive heart failure|hypertension
torcetrapib	Phase 3	cholesteryl ester transfer protein inhibitor	CETP		
torcitabine	Phase 2	DNA polymerase inhibitor	DCK|TK2		
toremifene	Launched	estrogen receptor antagonist|selective estrogen receptor modulator (SERM)	ESR1	oncology	breast cancer
torin-1	Preclinical	mTOR inhibitor	MTOR		
torin-2	Preclinical	mTOR inhibitor	MTOR		
tosedostat	Phase 2	peptidase inhibitor	ANPEP|LAP3|NPEPPS		
tosufloxacin	Launched	bacterial DNA gyrase inhibitor		infectious disease	gram-negative bacterial infections
toyocamycin	Phase 1	serine/threonine kinase inhibitor	ERN1		
tozadenant	Phase 3	adenosine receptor antagonist	ADORA2A		
tozasertib	Phase 2	Aurora kinase inhibitor|Bcr-Abl kinase inhibitor|FLT3 inhibitor|JAK inhibitor	AURKA|AURKB|AURKC|LCK		
TP-003	Preclinical	GABA receptor inverse agonist	GABRA1|GABRA2|GABRA3|GABRA5		
TP-0903	Phase 1/Phase 2	AXL kinase inhibitor	AXL		
TP-3654	Phase 1	"1,4,5-trisphosphate inhibitor"			
TPCA-1	Preclinical	IKK inhibitor	IKBKB		
TPPS4	Phase 1				
trabectedin	Phase 3	antitumor agent			
trabodenoson	Phase 3	adenosine receptor agonist			
tracazolate	Phase 2	GABA receptor modulator	GABRA1		
tradipitant	Phase 3	neurokinin receptor antagonist			
TRAM-34	Preclinical	potassium channel antagonist	KCNN4		
TRAM-39	Preclinical	calcium-activated potassium channel activator	KCNN4		
trametinib	Launched	MEK inhibitor	MAP2K1|MAP2K2	oncology	melanoma
tramiprosate	Phase 3	beta amyloid protein neurotoxicity inhibitor	APP		
trandolapril	Launched	angiotensin converting enzyme inhibitor	ACE	cardiology	hypertension|myocardial infarction
tranexamic-acid	Launched	antifibrinolytic|plasminogen activator inhibitor	PLG	hematology	hemophilia
tranilast	Launched	angiogenesis inhibitor	HPGDS|HRH1	pulmonary	asthma
"trans-10,cis-12-conjugated-linoleic-acid"	Launched				
trans-2-undecenoic-acid	Preclinical				
"trans-4-[8-(3-fluorophenyl)-1,7-naphthyridin-6-yl]cyclohexanecarboxylic-acid"	Preclinical				
trans-4-hydroxycrotonic-acid	Preclinical	gamma hydroxybutyric acid ligand			
trans-4-methoxycinnamic-acid	Preclinical				
transcrocetinate	Preclinical	glutamate receptor antagonist			
tranylcypromine	Launched	monoamine oxidase inhibitor	KDM1A|MAOA|MAOB	neurology/psychiatry	depression
trap-101	Preclinical	nociceptin/orphanin FQ receptor antagonist|opioid receptor antagonist	OPRL1		
trapidil	Launched	PDGFR tyrosine kinase receptor inhibitor	PDGFRA	cardiology	coronary artery disease (CAD)
travoprost	Launched	prostanoid receptor agonist	PTGFR	ophthalmology	ocular hypertension|glaucoma
traxoprodil	Phase 2	glutamate receptor antagonist	GRIN2B		
trazodone	Launched	adrenergic receptor antagonist|serotonin receptor antagonist|serotonin reuptake inhibitor	ADRA1A|ADRA2A|HRH1|HTR1A|HTR2A|HTR2B|HTR2C|SLC6A4	neurology/psychiatry	depression
trebenzomine	Phase 2				
trelagliptin	Launched	dipeptidyl peptidase inhibitor	DPP4	endocrinology	diabetes mellitus
tremorine	Preclinical	acetylcholine receptor agonist			
treosulfan	Launched	DNA synthesis inhibitor		oncology	ovarian cancer
trepibutone	Launched	cholinergic receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4	gastroenterology	irritable bowel syndrome
treprostinil	Launched	prostanoid receptor agonist	P2RY12|PPARD|PTGIR	pulmonary	pulmonary arterial hypertension (PAH)
trequinsin	Phase 1	phosphodiesterase inhibitor	PDE5A		
tretazicar	Phase 2	DNA replication inhibitor	NQO2		
tretinoin	Launched	retinoid receptor agonist|retinoid receptor ligand	ALDH1A1|ALDH1A2|GPRC5A|NR0B1|NR2C2|PPARD|RARA|RARB|RARG|RARRES1|RORB|RORC|RXRB|RXRG	hematologic malignancy	acute promyelocytic leukemia (APL)
triacetin	Launched				
triamcinolone	Launched	glucocorticoid receptor agonist	NR3C1	dermatology	corticosteroid-responsive dermatoses
triamcinolone-acetonide	Launched	glucocorticoid receptor agonist|immunosuppressant	NR3C1|SERPINA6	dermatology	corticosteroid-responsive dermatoses
triamcinolone-hexacetonide	Launched	anti-inflammatory agent			
triamterene	Launched	sodium channel blocker	SCNN1A|SCNN1B|SCNN1D|SCNN1G	endocrinology|cardiology	hypokalemia|hypertension|edema
triapine	Phase 2	ribonucleotide reductase inhibitor	RRM1|RRM2		
tribenoside	Launched	anti-inflammatory agent|capillary stabilizing agent			
tribomsalan	Preclinical				
tribromoethanol	Preclinical	analgesic agent			
tributyrin	Phase 1	HDAC inhibitor			
tricaprylin	Launched			dermatology	cosmetic
trichlormethiazide	Launched	chloride channel blocker	PTGS1|PTGS2|SLC12A1	cardiology	hypertension|edema
trichloroacetic-acid	Launched			dermatology	warts
trichloroethylene	Preclinical				
trichostatin-a	Phase 1	HDAC inhibitor	HDAC1|HDAC10|HDAC2|HDAC3|HDAC4|HDAC5|HDAC6|HDAC7|HDAC8|HDAC9		
triciribine	Phase 1/Phase 2	AKT inhibitor	AKT1|AKT2|AKT3		
triciribine-phosphate	Phase 1/Phase 2	AKT inhibitor			
triclabendazole	Launched	microtubule inhibitor	DNMT1	infectious disease	tapeworm
triclocarban	Launched	other antibiotic		infectious disease	first-aid antiseptic
triclosan	Launched	antibacterial agent	DNMT1	infectious disease	first-aid antiseptic
tridihexethyl	Launched	acetylcholine receptor antagonist		gastroenterology|ophthalmology	peptic ulcer disease (PUD)|nystagmus
trientine	Launched	chelating agent	CA14	metabolism	Wilson's disease
trifloxystrobin	Preclinical	mitochondrial electron transport inhibitor			
trifluoperazine	Launched	dopamine receptor antagonist	ADRA1A|CALM1|CALY|DRD2|DRD4|HRH1|HTR2A|HTR2C|S100A4|TNNC1	neurology/psychiatry	schizophrenia
triflupromazine	Launched	dopamine receptor antagonist	CHRM1|CHRM2|DRD1|DRD2|HTR2B	neurology/psychiatry|gastroenterology	psychosis|nausea|vomiting
trifluridine	Launched	DNA directed DNA polymerase inhibitor|thymidylate synthase inhibitor	TYMS	infectious disease	virus herpes simplex (HSV)
triflusal	Launched	cyclooxygenase inhibitor|platelet aggregation inhibitor|thromboxane synthase inhibitor	NFKB1|NOS2|PDE10A|PTGS1	neurology/psychiatry|cardiology	stroke|myocardial infarction|atrial fibrillation (AF)
trigonelline	Phase 1				
trihexyphenidyl	Launched	acetylcholine receptor antagonist	CHRM1	neurology/psychiatry	parkinsonism
trilaciclib	Phase 2	CDK inhibitor			
trilostane	Launched	3beta-hydroxy-delta5-steroid dehydrogenase inhibitor		endocrinology	Cushing's syndrome
TRIM	Preclinical				
trimebutine	Launched	opioid receptor agonist	OPRD1|OPRK1|OPRM1	gastroenterology	irritable bowel syndrome
trimetazidine	Launched	3-ketoacyl CoA thiolase inhibitor	ACAA2	cardiology	angina pectoris
trimethadione	Launched	oxazolidine antiepileptic	CACNA1G|CACNA1H|CACNA1I	neurology/psychiatry	seizures
trimethobenzamide	Launched	histamine receptor antagonist	DRD2	gastroenterology	vomiting|nausea|gastroenteritis
trimethoprim	Launched	dihydrofolate reductase inhibitor	DHFR|TYMS	infectious disease|gastroenterology	urinary tract infections|ear infections|diarrhea
trimethoquinol	Launched	adrenergic receptor antagonist	ADRB2|ADRB3	pulmonary	asthma
trimethylolpropane-triacrylate	Preclinical				
trimetozine	Launched	sedative		neurology/psychiatry	sedative
trimetrexate	Phase 3	dihydrofolate reductase inhibitor	DHFR		
trimipramine	Launched	norepinephrine reputake inhibitor|tricyclic antidepressant	SLC6A2|SLC6A3|SLC6A4	neurology/psychiatry	depression
trioxsalen	Launched	DNA synthesis inhibitor		dermatology	vitiligo|eczema
tripelennamine	Launched	histamine receptor antagonist	HRH1	pulmonary|allergy	asthma|allergic rhinitis|urticaria
triprolidine	Launched	histamine receptor antagonist	HRH1	allergy	allergic rhinitis
triptan	Phase 1	serotonin receptor agonist	HTR1B|HTR1D		
triptolide	Phase 3	RNA polymerase inhibitor	RELA		
triptorelin	Launched	gonadotropin releasing factor hormone receptor agonist	GNRHR	oncology|endocrinology|obstetrics/gynecology	prostate cancer|breast cancer|precocious puberty|endometriosis|myoma|gender dysphoria
troclosene	Launched				
trodusquemine	Phase 1	tyrosine phosphatase inhibitor			
trofinetide	Phase 2	cytokine production inhibitor	IFNG|IL6|TNF		
trofosfamide	Launched	DNA alkylating agent		oncology	medulloblastoma
troglitazone	Withdrawn	insulin sensitizer|PPAR receptor agonist	CYP2C8|PPARG|TRPM3		
troleandomycin	Launched	protein synthesis inhibitor		infectious disease|pulmonary|otolaryngology	pneumonia|bronchitis|tonsillitis|sinusitis
trolox	Launched	antioxidant			
tromaril	Launched	prostanoid receptor antagonist		ophthalmology	eye inflammation
trometamol	Launched		AMD1|CANT1|DCN|NEIL1|VEGFA		
"tropanyl-3,5-dimethylbenzoate"	Preclinical	serotonin receptor antagonist	HTR3A|HTR3B		
tropesin	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2		
tropicamide	Launched	acetylcholine receptor antagonist	CHRM3|CHRM4	ophthalmology	mydriasis diagnostic|cycloplegia diagnostic
tropifexor	Phase 2	FXR agonist			
tropisetron	Launched	serotonin receptor antagonist	GLRA1|GLRA2|GLRB|HTR3A|HTR4	gastroenterology	nausea|vomiting
trospium	Launched	acetylcholine receptor antagonist	CHRM1	urology	urinary incontinence|urinary frequency
trovafloxacin	Withdrawn	bacterial DNA gyrase inhibitor	TOP2A		
troventol	Phase 1				
trovirdine	Phase 1	non-nucleoside reverse transcriptase inhibitor			
troxerutin	Launched	antioxidant			
troxipide	Launched	glucosamine synthetase stimulant		gastroenterology	gastroesophageal reflux disease (GERD)
TRV130	Phase 3	opioid receptor agonist	OPRM1		
tryptanthrin	Preclinical	cyclooxygenase inhibitor	IDO1		
tryptophan	Launched	serotonin receptor partial agonist	CASR|IDO1|SLC36A1|WARS|WARS2	neurology/psychiatry|gastroenterology	anxiety|bloating|constipation|fatigue|sleeplessness
TS-011	Preclinical	delayed vasospasm antagonist			
TTNPB	Phase 1	retinoid receptor agonist	RARA|RARB|RARG		
TTP-22	Preclinical	casein kinase inhibitor	CSNK2A1		
TU-2100	Phase 2				
tuaminoheptane	Launched			otolaryngology	nasal congestion
tubastatin-A	Preclinical	HDAC inhibitor	HDAC6		
tubocurarine	Launched	acetylcholine receptor antagonist	ACHE|CHRNA2|HTR3A|HTR3B|KCNN1|KCNN2|KCNN3|ZACN	neurology/psychiatry	anesthetic
tucatinib	Phase 3	EGFR inhibitor	ERBB2		
tucidinostat	Phase 3	HDAC inhibitor			
tuftsin	Preclinical	macrophage activator			
TUG-770	Preclinical	free fatty acid receptor agonist	FFAR1		
TUG-891	Preclinical	free fatty acid receptor agonist	FFAR4		
tulobuterol	Launched	adrenergic receptor agonist	ADRB2	pulmonary	asthma
tulrampator	Phase 2	antidepressant 			
TW-37	Preclinical	BCL inhibitor	BCL2|BCL2L1|MCL1		
TWS-119	Preclinical	glycogen synthase kinase inhibitor	GSK3B|JUN|MYC		
TXA127	Phase 2	angiotensin receptor agonist			
TY-52156	Preclinical	sphingosine 1-phosphate receptor antagonist	S1PR3		
tylosin	Launched	protein synthesis inhibitor		infectious disease|gastroenterology	gram-positive bacterial infections|colitis
tymazoline	Launched			allergy	allergic rhinitis
tyrphostin-AG-1296	Preclinical	FLT3 inhibitor	FLT3		
tyrphostin-AG-1478	Preclinical	EGFR inhibitor	EGFR|MAPK14		
tyrphostin-AG-18	Preclinical	EGFR inhibitor|tyrosine kinase inhibitor	EGFR		
tyrphostin-AG-494	Preclinical	EGFR inhibitor	EGFR		
tyrphostin-AG-825	Preclinical	protein tyrosine kinase inhibitor	ERBB2		
tyrphostin-AG-835	Preclinical	protein tyrosine kinase inhibitor	EGFR		
tyrphostin-AG-879	Preclinical	tyrosine kinase inhibitor	ERBB2|KDR|NTRK1		
tyrphostin-AG-99	Preclinical	tyrosine kinase inhibitor	EGFR		
tyrphostin-A9	Preclinical	protein tyrosine kinase inhibitor|tyrosine kinase inhibitor			
U-0124	Preclinical	MEK inhibitor			
U-0126	Preclinical	MEK inhibitor	AKT1|CHEK1|GSK3B|LCK|MAP2K1|MAP2K2|MAP2K7|MAPK1|MAPK11|MAPK12|MAPK14|MAPK8|PRKCA|RAF1|ROCK1|RPS6KB1|SGK1		
U-0521	Preclinical	catechol O methyltransferase inhibitor	COMT		
U-104	Phase 1/Phase 2	carbonic anhydrase inhibitor	CA1|CA12|CA2|CA9		
U-18666A	Preclinical	oxidosqualene cyclase inhibitor			
U-50488-(-)	Preclinical	opioid receptor agonist	OPRK1		
U-54494A	Preclinical	opioid receptor agonist	OPRK1		
U-75799E	Phase 1	growth hormone releasing factor agonist	GHSR		
U-99194	Preclinical	dopamine receptor antagonist	DRD3		
UAMC-00039	Preclinical	dipeptidyl peptidase inhibitor	DPP4|DPP7		
UB-165	Preclinical	acetylcholine receptor agonist	CHRNA3|CHRNA4|CHRNB2		
ubenimex	Launched	leukotriene synthesis inhibitor	LTA4H|RNPEP	hematologic malignancy	acute myeloid leukemia (AML)
UBP-296	Preclinical	glutamate receptor antagonist	GRIK1		
UBP-302	Preclinical	glutamate receptor antagonist	GRIK1		
UBP-310	Preclinical	glutamate receptor antagonist	GRIK1|GRIK5		
UC-112	Preclinical	XIAP inhibitor	XIAP		
UCL-2077	Preclinical	slow afterhyperpolarization channel blocker			
udenafil	Launched	phosphodiesterase inhibitor		urology	erectile dysfunction
UF-010	Preclinical	HDAC inhibitor	HDAC1|HDAC2|HDAC3|HDAC8		
ufenamate	Launched	cyclooxygenase inhibitor	PTGS1|PTGS2	dermatology	eczema|dermatitis
UH-232-(+)	Preclinical	dopamine receptor antagonist	DRD2|DRD3|DRD4|HTR1A		
UK-356618	Preclinical	metalloproteinase inhibitor	MMP13|MMP14|MMP2|MMP3|MMP9		
UK-383367	Phase 1	procollagen C-endopeptidase inhibitor	BMP1		
UK-5099	Preclinical	monocarboxylate transporter inhibitor	SLC16A1		
uki-1	Preclinical	urokinase inhibitor			
ulifloxacin	Launched			infectious disease	gram-negative bacterial infections|gram-positive bacterial infections
ulipristal	Launched	progesterone receptor antagonist	PGR	endocrinology	contraceptive
umeclidinium	Launched	acetylcholine receptor antagonist	CHRM1|CHRM2|CHRM3	pulmonary	chronic obstructive pulmonary disease (COPD)|bronchitis|emphysema
unbs-5162	Phase 1	CC chemokine receptor antagonist			
UNC0224	Preclinical	histone lysine methyltransferase inhibitor	EHMT1|EHMT2		
UNC0321	Preclinical	histone lysine methyltransferase inhibitor	EHMT2		
UNC0631	Preclinical	histone lysine methyltransferase inhibitor	EHMT2		
UNC0638	Preclinical	histone lysine methyltransferase inhibitor	EHMT1|EHMT2		
UNC0642	Preclinical	histone lysine methyltransferase inhibitor	EHMT1|EHMT2		
UNC0646	Preclinical	histone lysine methyltransferase inhibitor	EHMT2		
UNC0737	Preclinical	histone lysine methyltransferase inhibitor	EHMT1|EHMT2		
UNC1215	Preclinical	L3MBTL antagonist	L3MBTL3		
UNC1999	Preclinical	histone lysine methyltransferase inhibitor	EZH2		
UNC2025	Preclinical	FLT3 inhibitor|MER tyrosine kinase inhibitor	FLT3|MERTK		
UNC2250	Preclinical	MER tyrosine kinase inhibitor	MERTK		
UNC2327	Preclinical	protein arginine N-methyltransferase inhibitor	PRMT3		
UNC3230	Preclinical	phosphatidyl-inositol activator	PIP5K1C		
UNC669	Preclinical	L3MBTL antagonist	L3MBTL1		
UNC926	Preclinical	MBT inhibitor	L3MBTL1		
undecylenic-acid	Launched	other antifungal		infectious disease	tinea pedis|tinea corporis
upadacitinib	Launched	JAK inhibitor			
upamostat	Phase 2	serine protease inhibitor			
UPF-1069	Preclinical	PARP inhibitor	PARP2		
uprifosbuvir	Preclinical	antiviral			
uprosertib	Phase 2	AKT inhibitor	AKT1|AKT2|AKT3		
uracil	Launched		DPYD|UCKL1		
uracil-mustard	Launched	DNA synthesis inhibitor		hematologic malignancy	non-Hodgkin lymphoma (NHL)
urapidil	Launched	adrenergic receptor antagonist	HTR1A	cardiology	hypertension
URB597	Phase 1	FAAH inhibitor	FAAH|FAAH2|TRPA1		
urea	Launched	hydroxy radical formation stimulant	ARG1|CA2|CTNNB1	dermatology	psoriasis|xerosis cutis|ichthyosis vulgaris|eczema|keratosis|dermatitis
urethane	Preclinical	local anesthetic			
uric-acid	Phase 3		PYGL		
uridine	Phase 2	dopamine receptor agonist	LSM6|TYMP		
uridine-triacetate	Launched			nephrology	orotic aciduria
uridine-5'-triphosphate	Launched	purinergic receptor activator	P2RY11|P2RY2|P2RY4|P2RY6|UCK2		
URMC-099	Preclinical	mixed lineage kinase inhibitor	CDKL2|DAPK3|FLT3|LRRK2|MAP3K10|MAP3K11|MAP3K2|MAP3K9|SRPK2		
urolithin-A	Phase 3	antioxidant			
ursodeoxycholyltaurine	Phase 3	cholesterol inhibitor			
ursodiol	Launched	nuclear factor erythroid derived|like (NRF2) activator	AKR1C2|NR1H4	gastroenterology	gallstones
ursolic-acid	Phase 2/Phase 3	ATPase inhibitor|NFkB pathway inhibitor|STAT inhibitor	HSD11B1|PLA2G1B|PTPN1|PYGM		
usniacin-(+)	Preclinical	MAP kinase activator	PTPN1		
V-51	Phase 1	adrenergic receptor antagonist			
vaborbactam	Launched	beta lactamase inhibitor			
vadadustat	Phase 3	hypoxia inducible factor prolyl hydroxylase inhibitor			
val-tyr	Preclinical	angiotensin converting enzyme inhibitor			
valaciclovir	Launched	DNA polymerase inhibitor		infectious disease	shingles|virus herpes simplex (HSV)
valbenazine	Launched	vesicular monoamine transporter inhibitor		neurology/psychiatry	dyskinesia
valdecoxib	Withdrawn	cyclooxygenase inhibitor	CA12|PTGS2		
valethamate	Launched	acetylcholine receptor antagonist	CHRM1|CHRM4|CHRM5	obstetrics/gynecology	labor induction
valganciclovir	Launched	DNA synthesis inhibitor		infectious disease	cytomegalovirus (CMV)
valnemulin	Launched	bacterial 50S ribosomal subunit inhibitor		infectious disease|gastroenterology	dysentry|colitis|pneumonia
valnoctamide	Launched	arachidonic acid acylation inhibitor|benzodiazepine receptor agonist		neurology/psychiatry	sleeplessness
valproic-acid	Launched	benzodiazepine receptor agonist|HDAC inhibitor	ABAT|ACADSB|ALDH5A1|HDAC1|HDAC2|HDAC9|OGDH|SCN10A|SCN11A|SCN1A|SCN1B|SCN2A|SCN2B|SCN3A|SCN3B|SCN4A|SCN4B|SCN5A|SCN7A|SCN8A|SCN9A	neurology/psychiatry	epilepsy|seizures|seizures
valpromide	Launched	epoxide hydolase inhibitor		neurology/psychiatry	epilepsy
valrocemide	Phase 2				
valrubicin	Launched	DNA inhibitor|topoisomerase inhibitor	TOP2A	oncology	bladder cancer
valsartan	Launched	angiotensin receptor antagonist	AGTR1	cardiology	hypertension|congestive heart failure|congestive heart failure
valspodar	Phase 3	P glycoprotein inhibitor	ABCB1		
vancomycin	Launched	bacterial cell wall synthesis inhibitor		infectious disease	endocarditis
vandetanib	Launched	EGFR inhibitor|RET tyrosine kinase inhibitor|VEGFR inhibitor	EGFR|EPHA1|EPHA10|EPHA2|EPHA3|EPHA4|EPHA5|EPHA6|EPHA7|EPHA8|EPHB1|EPHB2|EPHB3|EPHB4|EPHB6|ERBB2|ERBB3|ERBB4|FLT1|FLT4|KDR|PTK6|RET|SRC|TEK|VEGFA	oncology	medullary thyroid cancer (MTC)
vanillin	Preclinical		ABAT|ALDH5A1		
vanillylacetone	Preclinical				
vaniprevir	Phase 3	serine protease inhibitor			
vanitiolide	Preclinical				
vanoxerine	Phase 3	dopamine reuptake inhibitor	SLC6A3		
vapendavir	Phase 2	antiviral			
vardenafil	Launched	phosphodiesterase inhibitor	PDE5A|PDE6G|PDE6H	urology	erectile dysfunction
varenicline	Launched	acetylcholine receptor agonist	CHRNA3|CHRNA4|CHRNA6|CHRNA7	neurology/psychiatry	smoking cessation
varespladib	Phase 3	secretory phospholipase inhibitor	PLA2G2A		
vasopressin	Launched	vasopressin receptor agonist	AVPR1A|AVPR1B|AVPR2|OXTR	gastroenterology	abdominal distension
vatalanib	Phase 3	KIT inhibitor|PDGFR tyrosine kinase receptor inhibitor|VEGFR inhibitor	EGFR|FLT1|FLT4|KDR|PDGFRB		
vatinoxan	Preclinical	adrenergic receptor antagonist			
VBY-825	Preclinical	cathepsin inhibitor	CTSB|CTSL|CTSS		
VCH-916	Phase 1	HCV inhibitor			
VE-821	Preclinical	ATR kinase inhibitor	ATR		
VE-822	Phase 2	ATR kinase inhibitor	ATM|ATR|MTOR|PIK3CG		
vecabrutinib	Phase 1/Phase 2	Bruton's tyrosine kinase (BTK) inhibitor			
vecuronium	Launched	acetylcholine receptor antagonist	CHRNA2	neurology/psychiatry	muscle relaxant
vedaprofen	Launched	anti-inflammatory agent	PTGS2	neurology/psychiatry|endocrinology	pain relief|fever
velaresol	Preclinical				
veledimex	Phase 2	cytochrome P450 inhibitor			
veliflapon	Phase 3	leukotriene synthesis inhibitor	ALOX5AP		
veliparib	Phase 3	PARP inhibitor	PARP1|PARP2		
velneperit	Phase 2	neuropeptide receptor antagonist	NPY5R		
velpatasvir	Launched	antiviral		infectious disease	hepatitis C
vemurafenib	Launched	RAF inhibitor	BRAF|RAF1	oncology	melanoma
venetoclax	Launched	BCL inhibitor	BCL2	hematologic malignancy	chronic lymphocytic leukemia (CLL)
venlafaxine	Launched	adrenergic inhibitor|norepinephrine reuptake inhibitor|serotonin–norepinephrine reuptake inhibitor (SNRI)	SLC6A2|SLC6A4	neurology/psychiatry	depression|generalized anxiety disorder (GAD)|panic disorders|social anxiety disorder
VER-155008	Preclinical	HSP inhibitor	HSPA1A		
VER-49009	Preclinical	HSP inhibitor	HSP90AA1		
veralipride	Preclinical	dopamine receptor antagonist			
verapamil	Launched	calcium channel blocker	CACNA1A|CACNA1B|CACNA1C|CACNA1D|CACNA1F|CACNA1G|CACNA1I|CACNA1S|CACNB1|CACNB2|CACNB3|CACNB4|CYP3A4|KCNA10|KCNA7|KCNH2|KCNJ11|NALCN|SCN5A|SLC29A4|SLC6A4	cardiology	hypertension
verbascoside	Phase 2/Phase 3	NFkB pathway inhibitor|PKC inhibitor			
vercirnon	Phase 3	CC chemokine receptor antagonist	CCR9		
verdinexor	Preclinical	exportin antagonist			
verdiperstat	Phase 3	myeloperoxidase inhibitor			
vericiguat	Phase 3	guanylate cyclase stimulant			
verinurad	Phase 2	urate transporter inhibitor	SLC22A12		
vernakalant	Launched	potassium channel blocker	KCNA5	cardiology	atrial fibrillation (AF)
verteporfin	Launched	photosensitizing agent		ophthalmology	macular degeneration
verubecestat	Phase 3	beta secretase inhibitor			
verubulin	Phase 2	tubulin polymerization inhibitor	TUBB		
verucerfont	Phase 2	corticotropin releasing factor receptor antagonist			
vesamicol	Preclinical	acetylcholinesterase inhibitor	SLC18A3		
vesnarinone	Launched	phosphodiesterase inhibitor	KCNH2|PDE3A	cardiology	congestive heart failure
VGX-1027	Phase 1	tumor necrosis factor receptor antagonist	TLR4		
vicriviroc	Phase 3	CC chemokine receptor antagonist	CCR5		
vidarabine	Launched	antiviral	ADA	infectious disease	virus herpes simplex (HSV)|varicella-zoster virus (VZV)
vigabatrin	Launched	GABA aminotransferase inhibitor	ABAT|SLC32A1	neurology/psychiatry	seizures|spasms
vilanterol	Launched	adrenergic receptor agonist	ADRB2	pulmonary	chronic obstructive pulmonary disease (COPD)
vilazodone	Launched	serotonin reuptake inhibitor	DRD2|DRD3|HRH1|HTR1A|HTR4|SLC6A4	neurology/psychiatry	depression
vildagliptin	Launched	dipeptidyl peptidase inhibitor	DPP4	endocrinology	diabetes mellitus
viloxazine	Launched	norepinephrine reuptake inhibitor	SLC6A2	neurology/psychiatry	depression
vinblastine	Launched	microtubule inhibitor|tubulin polymerization inhibitor	JUN|TUBA1A|TUBB|TUBD1|TUBE1|TUBG1	hematologic malignancy|infectious disease|oncology	Hodgkin's lymphoma|true histiocytic lymphoma (THL)|mycosis|small lymphocytic lymphoma (SLL)|testicular carcinoma|Kaposi sarcoma
vinburnine	Launched	adrenergic receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4	neurology/psychiatry	stroke
vincamine	Withdrawn	adrenergic receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4		
vincristine	Launched	tubulin polymerization inhibitor	TUBA4A|TUBB	hematologic malignancy	acute lymphoblastic leukemia (ALL)
vindesine	Launched	tubulin polymerization inhibitor	TUBB|TUBB1	oncology	breast cancer|non-small cell lung cancer (NSCLC)|melanoma
vinflunine	Launched	microtubule inhibitor		oncology	bladder cancer
vinorelbine	Launched	tubulin polymerization inhibitor	TUBA1A|TUBA1B|TUBA1C|TUBA3C|TUBA3D|TUBA3E|TUBA4A|TUBB|TUBB1|TUBB2A|TUBB2B|TUBB3|TUBB4A|TUBB4B|TUBB6|TUBB8	oncology	non-small cell lung cancer (NSCLC)
vinpocetine	Launched	phosphodiesterase inhibitor|sodium channel blocker	PDE1A|PDE1C	neurology/psychiatry	stroke|senile dementia
viomycin	Launched	protein synthesis inhibitor		infectious disease	tuberculosis
vipadenant	Phase 1	adenosine receptor antagonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
vismodegib	Launched	hedgehog pathway inhibitor|smoothened receptor antagonist	SMO	oncology	basal cell carcinoma (BCC)
visomitin	Preclinical	antioxidant			
vitamin-B12	Launched			hematology	megaloblastic anemia
vitamin-E	Launched	LDL oxidation inhibitor|PKC inhibitor	ALOX5|DGKA|NR1I2|PPP2CA|PPP2CB|PRKCA|PRKCB|SEC14L2|SEC14L3|SEC14L4		
vixotrigine	Phase 2	sodium channel blocker			
VLX1570	Phase 1/Phase 2	deubiquitinase inhibitor			
VLX600	Phase 1	antitumor agent|ubiquitin C-terminal hydrolase inhibitor	TP53|USP14		
VL285	Preclinical	PROTAC			
voclosporin	Phase 3	calcineurin inhibitor			
voglibose	Launched	glucosidase inhibitor	MGAM	endocrinology	diabetes mellitus|hyperglycemia
volasertib	Phase 3	PLK inhibitor	PLK1		
volinanserin	Phase 3	serotonin receptor antagonist	HTR2A|HTR2B|HTR2C|KCNH2		
vonoprazan	Launched	potassium-competitive acid antagonist	ATP4A	gastroenterology	peptic ulcer disease (PUD)
vorapaxar	Launched	thrombin inhibitor	F2R	cardiology	myocardial infarction|peripheral artery disease (PAD)
vorasidenib	Preclinical	isocitrate dehydrogenase inhibitor			
voreloxin	Phase 3	topoisomerase inhibitor	TOP2A		
voriconazole	Launched	cytochrome P450 inhibitor	CYP2C19|CYP2C9|CYP3A4|CYP3A5|PTGS1	infectious disease	esophageal candidiasis|aspergillosis|skin infections
vorinostat	Launched	HDAC inhibitor	HDAC1|HDAC10|HDAC11|HDAC2|HDAC3|HDAC5|HDAC6|HDAC8|HDAC9	hematologic malignancy	cutaneous T-cell lymphoma (CTCL)
vortioxetine	Launched	serotonin receptor agonist|serotonin receptor antagonist	HTR1A|HTR1B|HTR2A|HTR2C|HTR3A|HTR5A|HTR6|HTR7|SLC6A4	neurology/psychiatry	depression
voruciclib	Phase 1	CDK9 inhibitor			
voxelotor	Launched	hemoglobin modulator			
voxtalisib	Phase 2	mTOR inhibitor|PI3K inhibitor	MTOR|PIK3CA		
VP-20629	Phase 1	beta amyloid antagonist	PLA2G2E|SLC36A1		
VS-4718	Phase 1	focal adhesion kinase inhibitor			
VT-464	Phase 2	cytochrome P450 inhibitor	CYP17A1		
VTP-27999	Phase 1	renin inhibitor	REN		
VUF10166	Preclinical	serotonin receptor antagonist	HTR3A|HTR3B		
VUF10460	Preclinical	histamine receptor agonist	HRH4		
VUF11207	Preclinical	CC chemokine receptor agonist	ACKR3		
VU0155069	Preclinical	phospholipase inhibitor	PLD1		
VU0238429	Preclinical	acetylcholine receptor allosteric modulator	CHRM5		
VU0240551	Preclinical	potassium/chloride cotransporter inhibitor	SLC12A5		
VU0357121	Preclinical	glutamate receptor positive allosteric modulator	GRM5		
VU0360172	Preclinical	glutamate receptor positive allosteric modulator	GRM5		
VU0361737	Preclinical	glutamate receptor positive allosteric modulator	GRM4		
VU0364439	Preclinical	glutamate receptor positive allosteric modulator	GRM4		
VU0364739	Preclinical	phospholipase inhibitor	PLD2		
VU0364770	Preclinical	glutamate receptor positive allosteric modulator	GRM4		
VU0422288	Preclinical	glutamate receptor positive allosteric modulator	GRM3		
VU10010	Preclinical	acetylcholine receptor allosteric modulator	CHRM4		
VU152100	Preclinical	acetylcholine receptor allosteric modulator	CHRM4		
VU1545	Preclinical	glutamate receptor positive allosteric modulator	GRM5		
VU29	Preclinical	glutamate receptor potentiator	GRM5		
VU591	Preclinical	potassium channel blocker	KCNJ1		
VX-11e	Preclinical	MAP kinase inhibitor	MAPK1		
VX-222	Phase 2	HCV inhibitor			
VX-702	Phase 2	p38 MAPK inhibitor	IL1B|IL6|MAPK11|MAPK12|MAPK14|TNF		
VX-745	Phase 2	p38 MAPK inhibitor	MAPK11|MAPK12|MAPK14		
VX-765	Phase 2	caspase inhibitor	CASP1		
W-54011	Preclinical	anaphylatoxin chemotactic receptor antagonist	C5AR1		
walrycin-B	Preclinical	transcriptional regulatory protein WalR			
warfarin	Launched	vitamin K antagonist	VKORC1	hematology|cardiology	deep vein thrombosis (DVT)|pulmonary embolism (PE)|atrial fibrillation (AF)|myocardial infarction
WAY-100635	Phase 1	serotonin receptor antagonist	HTR1A		
WAY-161503	Preclinical	serotonin receptor agonist	HTR2C		
WAY-170523	Preclinical	metalloproteinase inhibitor	MMP13		
WAY-200070	Preclinical	estrogen receptor agonist	ERBB2|ERBB3|ERBB4|ESR2		
WAY-207024	Preclinical	gonadotropin releasing factor hormone receptor antagonist	GNRHR|HRH2|TACR2		
WAY-208466	Preclinical	serotonin receptor agonist	DRD2|HTR2A|HTR2C|HTR6|HTR7		
WAY-213613	Preclinical	glutamate inhibitor	SLC1A2		
WAY-255348	Preclinical	progesterone receptor antagonist			
WAY-316606	Preclinical	secreted frizzled related protein inhibitor	SFRP1		
WAY-362450	Phase 1	FXR agonist	NR1H4		
WAY-600	Preclinical	mTOR inhibitor	MTOR		
WAY-629	Preclinical	serotonin receptor agonist	HTR2C		
WB-4101	Preclinical	adrenergic receptor antagonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C|HTR1A		
WDR5-0103	Preclinical	histone lysine methyltransferase inhibitor	WDR5		
WEHI-345-analog	Preclinical	SRC inhibitor			
WH-4-023	Preclinical	SRC inhibitor	LCK|SRC		
WHI-P154	Preclinical	JAK inhibitor	EGFR|JAK1|JAK2|JAK3		
WIKI4	Preclinical	tankyrase inhibitor|WNT pathway inhibitor	TNKS2		
WIN-18446	Preclinical	aldehyde dehydrogenase inhibitor	ALDH1A2		
WIN-64338	Preclinical	bradykinin receptor antagonist	BDKRB2		
wiskostatin	Preclinical	actin related protein inhibitor|neural Wiskott-Aldrich syndrome protein inhibitor	WASL		
wnt-c59	Preclinical	porcupine inhibitor	PORCN		
wortmannin	Preclinical	PI3K inhibitor	PI4KA|PI4KB|PIK3CA|PIK3CD|PIK3CG|PIK3R1|PLK1|PRKDC		
WP1066	Phase 1	STAT inhibitor	STAT3		
WP1130	Preclinical	deubiquitinase inhibitor	JAK2|UCHL5|USP14|USP9X		
WP921	Preclinical				
WR99210	Preclinical	dihydrofolate reductase inhibitor	TYMS	infectious disease	malaria
WWL-113	Preclinical	carboxylesterase inhibitor	CES3		
WWL-123	Preclinical	monoacylglycerol lipase inhibitor	ABHD6		
WY-16922	Phase 1	histamine release inhibitor			
WYE-125132	Preclinical	mTOR inhibitor	MTOR		
WYE-354	Preclinical	mTOR inhibitor	MTOR		
WYE-687	Preclinical	mTOR inhibitor	MTOR		
WZ-3146	Preclinical	EGFR inhibitor	EGFR		
WZ-4002	Preclinical	EGFR inhibitor	EGFR|ERBB2		
WZ4003	Preclinical	AMPK inhibitor	NUAK1|NUAK2		
WZ8040	Preclinical	EGFR inhibitor	EGFR		
WZ811	Preclinical	CC chemokine receptor antagonist	CXCR4		
xaliproden	Phase 3	serotonin receptor agonist	HTR1A		
xamoterol	Phase 3	adrenergic receptor agonist	ADRB1		
xanomeline	Phase 3	acetylcholine receptor agonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|HTR1A|HTR1B|HTR1D|HTR1E|HTR1F|HTR2A|HTR2B|HTR2C|HTR6|HTR7		
xanthone	Preclinical	antimalarial agent			
XAV-939	Preclinical	tankyrase inhibitor	TNKS|TNKS2		
XBD173	Phase 2	benzodiazepine receptor ligand	TSPO		
XD-14	Preclinical	bromodomain inhibitor	BRD2|BRD3|BRD4|BRDT		
XE-991	Preclinical	potassium channel blocker	KCNQ1|KCNQ2|KCNQ3|KCNQ4|KCNQ5		
xenalipin	Phase 2				
xibenolol	Phase 3	adrenergic receptor antagonist			
xilobam	Phase 1				
xipamide	Launched	carbonic anhydrase inhibitor	SLC12A3	cardiology	edema|hypertension
XL019	Phase 1	JAK inhibitor	JAK1|JAK2|JAK3		
XL041	Preclinical	LXR agonist			
XL147	Phase 2	PI3K inhibitor	PIK3CA|PIK3CD|PIK3CG		
XL228	Phase 1	Abl kinase inhibitor|insulin growth factor receptor inhibitor|SRC inhibitor	IGF1R|SRC		
XL388	Preclinical	mTOR inhibitor	MTOR		
XL647	Phase 3	EGFR inhibitor|VEGFR inhibitor	EGFR|EPHB4|ERBB2|FLT4|KDR		
XL888	Phase 1	HSP inhibitor			
XMD17-109	Preclinical	MAP kinase inhibitor	MAPK7		
XMD8-92	Preclinical	MAP kinase inhibitor	DCLK2|MAPK7|PLK4|TNK1		
xylazine	Launched	adrenergic receptor agonist	ADRA2A|ADRA2B|ADRA2C	neurology/psychiatry	anesthetic
xylometazoline	Launched	adrenergic receptor agonist	ADRA1A|ADRA1B|ADRA1D|ADRA2A|ADRA2B|ADRA2C	otolaryngology|allergy	nasal congestion|allergic rhinitis
xylose	Launched				
Y-11	Preclinical	focal adhesion kinase inhibitor	PTK2		
Y-134	Preclinical	estrogen receptor antagonist	ESR1|ESR2		
Y-26763	Phase 1	potassium channel activator	KCNJ8		
Y-27152	Phase 1	potassium channel activator	KCNJ8		
Y-27632	Preclinical	rho associated kinase inhibitor	PKIA|PKN2|PRKACA|PRKCE|ROCK1|ROCK2		
Y-29794	Preclinical	prolyl endopeptidase inhibitor	PREP		
Y-320	Preclinical	interleukin inhibitor	IL17A		
Y-39983	Phase 2	rho associated kinase inhibitor	ROCK1|ROCK2		
YC-1	Preclinical	guanylyl cyclase activator	GUCY1A2|GUCY1A3|GUCY1B3|HIF1A		
YIL-781	Preclinical	ghrelin receptor antagonist	GHSR		
YK-4-279	Preclinical	apoptosis inhibitor	EWSR1|FLI1		
YL0919	Preclinical	selective serotonin reuptake inhibitor (SSRI)			
YM-022	Phase 2	CCK receptor antagonist	CCKBR		
YM-155	Phase 2	survivin inhibitor	BIRC5		
YM-201636	Preclinical	PI3K inhibitor			
YM-244769	Preclinical	sodium/calcium exchange inhibitor			
YM-298198	Preclinical	glutamate receptor antagonist	GRM1		
YM-298198-desmethyl	Preclinical	glutamate receptor antagonist	GRM1		
YM-511	Phase 2	aromatase inhibitor	CYP19A1		
YM-58483	Preclinical	calcium channel blocker	TRPC3|TRPC5|TRPM4		
YM-750	Phase 1	ACAT inhibitor	SOAT1		
YM-90709	Preclinical	IL5 inhibitor	CSF2RB|IL5RA		
YM-976	Phase 1	phosphodiesterase inhibitor	PDE4A		
YO-01027	Preclinical	gamma secretase inhibitor			
yoda-1	Preclinical	piezo channel activator	PIEZO1		
yohimbine	Launched	adrenergic receptor antagonist	ADRA2A|ADRA2B|ADRA2C|DRD2|DRD3|HTR1A|HTR1B|HTR1D|HTR1E|HTR1F|HTR2A|HTR2B|HTR2C|HTR5A|HTR7|KCNJ1|KCNJ10|KCNJ11|KCNJ12|KCNJ14|KCNJ15|KCNJ8	cardiology	cardiac arrythmia|bradycardia
YS-035	Preclinical	calcium channel blocker			
YS-201	Preclinical	calcium receptor antagonist			
YZ9	Preclinical	phosphofructokinase inhibitor	MIF|PFKFB3		
Y16	Preclinical	rho associated kinase inhibitor	RHOA		
zacopride	Phase 2	serotonin receptor antagonist	HTR3A|HTR3B|HTR4|HTR5A		
zafirlukast	Launched	leukotriene receptor antagonist	CYSLTR1|CYSLTR2	pulmonary	asthma
zalcitabine	Launched	nucleoside reverse transcriptase inhibitor		infectious disease	human immunodeficiency virus (HIV-1)
zaldaride	Phase 3	calmodulin antagonist	CALM1		
zaltidine	Phase 3	histamine receptor antagonist	HRH2		
zaltoprofen	Launched	cyclooxygenase inhibitor		endocrinology|neurology/psychiatry	fever|pain relief
ZAMI-633	Phase 3	urease inhibitor			
zamifenacin	Phase 3	acetylcholine receptor antagonist	CHRM3		
zanamivir	Launched	neuraminidase inhibitor	NEU2	infectious disease	influenza A virus infection
zanubrutinib	Launched	Bruton's tyrosine kinase (BTK) inhibitor			
ZAPA	Preclinical				
zaprinast	Phase 2	phosphodiesterase inhibitor	GPR35|PDE1A|PDE4D|PDE5A|PDE9A		
zardaverine	Phase 2	phosphodiesterase inhibitor	PDE4D		
zatebradine	Phase 3	HCN channel blocker	HCN1|HCN2|HCN3|HCN4		
ZCL-278	Preclinical	CDC inhibitor	CDC42		
ZD-0947	Preclinical	potassium channel activator			
ZD-2079	Phase 2	adrenergic receptor agonist	ADRB3		
ZD-7114	Phase 1	adrenergic receptor agonist	ADRB3		
ZD-7155	Preclinical	angiotensin receptor antagonist	AGTR1		
ZD-7288	Phase 2	HCN channel blocker	HCN1|HCN2|HCN3|HCN4		
zeatin	Phase 1				
zebularine	Preclinical	DNA methyltransferase inhibitor	CDA|DNMT1		
zibotentan	Phase 3	endothelin receptor antagonist	EDNRA		
zidovudine	Launched	nucleoside reverse transcriptase inhibitor	TERT	infectious disease	human immunodeficiency virus (HIV-1)|acquired immunodeficiency syndrome (AIDS)
zileuton	Launched	leukotriene synthesis inhibitor|lipoxygenase inhibitor	ALOX5	pulmonary	asthma
zilpaterol	Launched	adrenergic receptor agonist	ADRB2	endocrinology	weight-gain aid
zimelidine	Withdrawn	selective serotonin reuptake inhibitor (SSRI)	MAOA|MAOB|SLC6A4		
zinc-undecylenate	Launched	other antifungal		infectious disease	tinea pedis
zindotrine	Phase 2	phosphodiesterase inhibitor			
ziprasidone	Launched	dopamine receptor antagonist|serotonin receptor antagonist	ADRA1A|ADRA1B|ADRA2A|ADRA2B|ADRA2C|CHRM1|CHRM2|CHRM3|CHRM4|CHRM5|DRD1|DRD2|DRD3|DRD4|DRD5|HRH1|HTR1A|HTR1B|HTR1D|HTR1E|HTR2A|HTR2C|HTR3A|HTR6|HTR7|SLC6A4	neurology/psychiatry	schizophrenia|bipolar disorder
ziritaxestat	Phase 3	autotaxin inhibitor			
ZK-164015	Preclinical	estrogen receptor antagonist	ESR1|ESR2		
ZK-200775	Phase 2	kainate receptor antagonist			
ZK-811752	Phase 2	CC chemokine receptor antagonist	CCR1		
ZK-93423	Phase 3	benzodiazepine receptor agonist	GABRA1|GABRA2|GABRA3|GABRA5|GABRB2|GABRG2		
ZK-93426	Phase 1	benzodiazepine receptor antagonist	GABRA1|GABRA2|GABRA3|GABRA5		
ZLN005	Preclinical				
ZLN024	Preclinical	AMPK activator	PRKAA1|PRKAB1|PRKAG1		
ZM-226600	Preclinical	Kir6 channel (KATP) activator			
ZM-241385	Preclinical	adenosine receptor antagonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
ZM-306416	Preclinical	Abl kinase inhibitor|SRC inhibitor|VEGFR inhibitor	EGFR|FLT1|FLT4|KDR		
ZM-323881	Preclinical	VEGFR inhibitor	KDR		
ZM-336372	Preclinical	RAF inhibitor	BRAF|LCK|MAPK14|RAF1		
ZM-39923	Preclinical	JAK inhibitor	JAK1|JAK3		
ZM-447439	Preclinical	Aurora kinase inhibitor	AURKA|AURKB		
zofenopril-calcium	Launched	angiotensin converting enzyme inhibitor	ACE	cardiology	hypertension
zolantidine	Preclinical	histamine receptor antagonist			
zoledronic-acid	Launched	bone resorption inhibitor	FDPS|GGPS1	endocrinology	Paget's disease
zoliflodacin	Phase 3	antibacterial 			
zolimidine	Launched	mucus protecting agent		gastroenterology	peptic ulcer disease (PUD)|gastroesophageal reflux disease (GERD)
zolmitriptan	Launched	serotonin receptor agonist	HTR1A|HTR1B|HTR1D|HTR1E|HTR1F	neurology/psychiatry	migraine headache
zomepirac	Withdrawn	prostaglandin synthesis inhibitor	PTGDR2		
zometapine	Phase 2				
zoniporide	Phase 3	sodium/hydrogen exchanger inhibitor	SLC9A1		
zonisamide	Launched	sodium channel blocker|T-type calcium channel blocker	CA1|CA10|CA11|CA12|CA13|CA14|CA2|CA3|CA4|CA5A|CA5B|CA6|CA7|CA8|CA9|CACNA1G|CACNA1H|CACNA1I|MAOA|MAOB|SCN10A|SCN11A|SCN1A|SCN1B|SCN2A|SCN2B|SCN3A|SCN3B|SCN4A|SCN4B|SCN5A|SCN7A|SCN8A|SCN9A	neurology/psychiatry	seizures|epilepsy
zopolrestat	Phase 2		AKR1B1|AKR1B10		
zosuquidar	Phase 3	P glycoprotein inhibitor	ABCB1|ABCB4		
zotarolimus	Launched	mTOR inhibitor	FKBP1A	cardiology	coronary artery restenosis
zotepine	Launched	dopamine receptor antagonist|serotonin receptor antagonist	ADRA2B|DRD2|DRD3|DRD4|HRH1|HTR1A|HTR1B|HTR1D|HTR1E|HTR2A|HTR2C|HTR6|HTR7|SLC6A2|SLC6A4	neurology/psychiatry	schizophrenia
zoxazolamine	Phase 2	myorelaxant			
ZSET1446	Preclinical	nicotinic receptor agonist			
ZSTK-474	Phase 1/Phase 2	PI3K inhibitor	PIK3CB|PIK3CD|PIK3CG		
zuclopenthixol	Launched	dopamine receptor antagonist	ADRA1A|ADRA2A|DRD1|DRD2|DRD5|HRH1|HTR2A	neurology/psychiatry	schizophrenia|bipolar disorder
zuranolone	Phase 3	GABA receptor agonist			
Z160	Phase 2	N-type calcium channel blocker	CACNA2D1		
"1,12-Besm"	Phase 2	polyamine biosynthesis inhibitor			
"1,2,3,4,5,6-hexabromocyclohexane"	Preclinical	JAK inhibitor	JAK2		
"1,3-dipropyl-8-phenylxanthine"	Preclinical	adenosine receptor antagonist			
"1,4-butanediol"	Phase 1	benzodiazepine receptor agonist|gamma hydroxybutyric acid agonist	MAN1B1|PLA2G2A|PLA2G2E		
"1,5-dicaffeoylquinic-acid"	Phase 1				
"1-((Z)-3-chloroallyl)-1,3,5,7-tetraazaadamantan-1-ium"	Preclinical				
"1-(1,2-diphenylethyl)piperidine-(+/-)"	Preclinical	glutamate receptor antagonist			
1-(2-chloro-5-methylphenoxy)-3-(isopropylamino)-2-propanol	Preclinical				
1-acetyl-4-methylpiperazine	Preclinical	acetylcholine receptor agonist			
1-azakenpaullone	Preclinical	glycogen synthase kinase inhibitor	CCNB1|CDK1|CDK5|GSK3B		
1-deoxymannojirimycin	Preclinical	alpha mannosidase inhibitor	MAN2A1		
1-EBIO	Preclinical	potassium channel activator	KCNN1|KCNN2|KCNN3|KCNN4		
1-ethyl-2-pyrrolidone	Preclinical	transdermal absorption-enhancing compound			
1-hexadecanal	Preclinical	sphingosine 1-phosphate receptor substrate	DBI|RHO		
1-hexadecanol	Launched			dermatology	cosmetic
1-naphthyl-PP1	Preclinical	SRC inhibitor	SRC		
1-octacosanol	Phase 2				
1-octanol	Phase 2		GJA1|GJA10|GJA3|GJA4|GJA5|GJA8|GJA9|GJB1|GJB2|GJB3|GJB4|GJB5|GJB6|GJB7|GJC1|GJC2|GJC3|GJD2|GJD3|GJD4|GJE1		
1-phenylbiguanide	Preclinical	serotonin receptor agonist	HTR3A|HTR3B		
1E-1-(2-hydroxy-5-methylphenyl)-1-dodecanone-oxime	Preclinical				
"1S,2R-phenylpropanolamine"	Withdrawn	adrenergic receptor agonist			
10-deacetylbaccatin	Preclinical	antitumor agent			
10-DEBC	Preclinical	AKT inhibitor	PIM1		
10-hydroxycamptothecin	Preclinical	topoisomerase inhibitor	TOP1		
10058-F4	Preclinical	c-Myc inhibitor			
12-O-tetradecanoylphorbol-13-acetate	Phase 2	PKC activator	KCNT2|TRPV4		
1400W	Preclinical	nitric oxide synthase inhibitor	NOS1|NOS2|NOS3		
"16,16-dimethylprostaglandin-e2"	Phase 2	prostanoid receptor agonist	HPGD		
17-hydroxyprogesterone-caproate	Launched	progesterone receptor agonist	AR|ESR1|ESR2|NR1H4|NR1I2|NR3C1|PGR	obstetrics/gynecology	spontaneous preterm birth
17-PA	Preclinical	glucocorticoid receptor agonist			
2'-C-methylguanosine	Preclinical	HCV inhibitor			
2'-MeCCPA	Preclinical	adenosine receptor agonist	ADORA1		
"2,3-cis/exo-camphanediol"	Phase 1				
"2,3-cis/exo-pinanediol"	Phase 1				
"2,3-DCPE"	Preclinical	BCL-XL downregulator	BCL2L1		
"2,4-dinitrochlorobenzene"	Phase 2	thioredoxin inhibitor	TXN		
"2,4-dinitrophenol"	Preclinical	ATP synthase inhibitor	APP		
"2,5-furandimethanol"	Phase 2	hemoglobin modulator	HBB		
"2,6-dimethylpiperidine"	Preclinical				
"2-(chloromethyl)-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4(3H)-one"	Preclinical				
2-(1-adamantylamino)benzoic-acid	Preclinical				
2-(3-mercaptopropyl)pentanedioic-acid	Phase 1	glutamate carboxypeptidase inhibitor	FOLH1		
2-[1-(4-piperonyl)piperazinyl]benzothiazole	Preclinical	serotonin receptor agonist	HTR4		
2-aminobenzenesulfonamide	Preclinical	carbonic anhydrase inhibitor	CA12|CA14|CA2|CA6|CA9		
2-APB	Preclinical	"1,4,5-trisphosphate inhibitor"	TRPC1|TRPC3|TRPC4|TRPC5|TRPC6|TRPC7|TRPM2|TRPM3|TRPM6|TRPV1|TRPV6		
2-BFI	Preclinical	imidazoline receptor ligand	ADRA2A|ADRA2B|ADRA2C|MAOA|MAOB		
2-chloro-N6-cyclopentyladenosine	Preclinical	adenosine receptor agonist	ADORA1|ADORA2A|ADORA2B|ADORA3		
2-chloroadenosine	Preclinical	adenosine receptor agonist	ADORA1|ADORA2A|ADORA2B		
2-chloropyrazine	Preclinical				
2-CMDO	Preclinical	dopamine receptor antagonist	DRD2|DRD4		
2-deoxy-2-([methyl(nitroso)carbamoyl]amino)hexose	Preclinical			oncology|endocrinology	pancreatic cancer|hypoglycemia
2-deoxyglucose	Phase 2	glycolysis inhibitor	SLC2A1|SLC2A2|SLC2A3|SLC2A4		
2-ethoxybenzoic-acid	Phase 1	analgesic agent			
"2-ethyl-1,3-hexanediol"	Preclinical				
2-fluoro-2-deoxy-D-galactose	Phase 1		LCT		
2-fluorofucose	Phase 1				
"2-hydroxy-4-((E)-3-(4-hydroxyphenyl)acryloyl)-2-((2R,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)-6-((2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)cyclohexane-1,3,5-trione"	Preclinical				
2-hydroxyethyl-salicylate	Launched			neurology/psychiatry	pain relief
2-hydroxyflutamide	Phase 2	androgen receptor antagonist	AR		
2-hydroxysaclofen	Preclinical	GABA receptor antagonist	GABBR1|GABBR2		
2-iminobiotin	Phase 2	nitric oxide synthase inhibitor	NOS1|NOS2		
2-iodohippuric-acid	Preclinical				
2-iodomelatonin	Preclinical	melatonin receptor agonist	MTNR1A|MTNR1B|NQO2		
2-methoxyestradiol	Phase 2	hypoxia inducible factor inhibitor	COMT|CYP19A1|CYP1A1|CYP1B1|HIF1A|TUBB		
2-methyl-5-hydroxytryptamine	Preclinical	serotonin receptor agonist	HTR1B|HTR1D|HTR1E|HTR1F|HTR3A|HTR3B|HTR6		
2-methyl-5-nitrophenol	Preclinical				
2-methylimidazole	Preclinical	cholesterol inhibitor			
2-octyldodecan-1-ol	Preclinical				
2-oleoylglycerol	Phase 1	glucose dependent insulinotropic receptor ligand	GPR119		
2-oxoglutaric-acid	Preclinical		OXGR1		
2-oxopropanoate	Preclinical	pyruvate dehydrogenase kinase inhibitor	ABAT		
2-phenylmelatonin	Preclinical	melatonin receptor agonist	MTNR1A|MTNR1B		
2-PMDQ	Preclinical	adrenergic receptor antagonist	ADRA1A		
2-pyridylethylamine	Preclinical	histamine receptor agonist	HRH1		
2-TEDC	Preclinical	lipoxygenase inhibitor	ALOX12		
2-thiouracil	Preclinical				
20-HETE	Preclinical	ion channel antagonist			
20-hydroxyecdysone	Phase 2	ecdysone receptor modulator			
3'-fluorobenzylspiperone	Preclinical	dopamine receptor ligand	DRD2		
"3,3'-dichlorobenzaldazine"	Preclinical	glutamate receptor modulator	GRM5		
"3,3'-diindolylmethane"	Phase 3	"CHK inhibitor|cytochrome P450 activator|indoleamine 2,3-dioxygenase inhibitor"	AR|HIF1A|IFNG|PI3		
"3,4-DCPG-(+/-)"	Preclinical	glutamate receptor agonist	GRM8		
"3,4-DCPG-(R)"	Preclinical	glutamate receptor antagonist			
"3,4-DCPG-(S)"	Preclinical	glutamate receptor agonist	GRM8		
"3,4-methylenedioxy-beta-nitrostyrene"	Preclinical	SRC inhibitor|SYK inhibitor	SRC|SYK		
"3,5-DHPG-(S)"	Preclinical	glutamate receptor agonist	GRM1		
3-(4-methylbenzylidene)camphor	Launched	endocrine disruptor		dermatology	sunscreen lotion
3-alpha-bis-(4-fluorophenyl)-methoxytropane	Preclinical	dopamine uptake inhibitor	CHRM1|SLC6A2|SLC6A3|SLC6A4		
3-alpha-hydroxy-5-beta-androstan-17-one	Preclinical		HSD17B11|IGHG2|SULT2A1		
3-amino-benzamide	Phase 2	PARP inhibitor	PARP1		
3-anilinopropan-1-ol	Preclinical				
3-AQC	Preclinical	serotonin receptor agonist	HTR3A		
3-bromo-7-nitroindazole	Preclinical	nitric oxide synthase inhibitor	NOS1|NOS2|NOS3		
3-bromocamphor	Launched				
3-bromopyruvate	Preclinical	hexokinase inhibitor	HK2		
3-carboxy-4-hydroxyphenylglycine-(R)	Preclinical	glutamate receptor antagonist	GRIN1|GRIN2A|GRIN2B|GRIN2C		
3-carboxy-4-hydroxyphenylglycine-(S)	Preclinical	glutamate receptor antagonist	GRM1|GRM5		
3-CPMT	Preclinical	dopamine reuptake inhibitor			
3-deazaadenosine	Phase 2	adenosylhomocysteinase inhibitor	AHCY		
3-deazaneplanocin-A	Preclinical	histone lysine methyltransferase inhibitor	EZH2		
3-deazauridine	Preclinical	cytidine deaminase inhibitor			
3-hydroxy-3-phenylpentanamide	Phase 1	GABA receptor modulator			
3-indolebutyric-acid	Preclinical		B2M|HLA-A|TRAC|TRBC1		
3-MATIDA	Preclinical	glutamate receptor antagonist	GRM1		
3-methyl-GABA	Preclinical	GABA aminotransferase activator	ABAT		
3-methyladenine	Preclinical	PI3K inhibitor	PI3		
3-MPPI	Preclinical	adrenergic receptor ligand	ADRA1A		
3PO	Preclinical	phosphofructokinase inhibitor	PFKFB3		
"4,4'-DDT"	Preclinical				
"4,4-pentamethylenepiperidine"	Preclinical	M2 channel blocker			
"4,5,6,7-tetrabromobenzotriazole"	Preclinical	casein kinase inhibitor	AKT1|CHEK1|CSNK2A1|GSK3B|LCK|MAP2K1|MAPK1|MAPK11|MAPK12|MAPK14|MAPK8|PRKCA|ROCK1|RPS6KB1|SGK1		
4-(aminomethyl)benzoic-acid	Preclinical	hemostatic agent			
4-(4-fluorobenzoyl)-1-(4-phenylbutyl)-piperidine	Preclinical	serotonin receptor antagonist	HTR2A		
"4-acetyl-1,1-dimethylpiperazinium"	Preclinical	acetylcholine receptor agonist			
4-aminohippuric-acid	Launched		SLC22A6	nephrology	renal diagnostic agent
4-carboxy-3-hydroxyphenylglycine-(RS)	Preclinical	glutamate receptor agonist|glutamate receptor antagonist	GRM1		
4-carboxy-3-hydroxyphenylglycine-(S)	Preclinical	glutamate receptor agonist|glutamate receptor antagonist	GRM1|GRM2		
4-chlorophenylguanidine	Preclinical	urokinase inhibitor	PLAUR		
4-CMTB	Preclinical	free fatty acid receptor agonist	FFAR2		
4-DAMP	Preclinical	cholinergic receptor antagonist	CHRM1|CHRM2|CHRM3|CHRM4|CHRM5		
4-galactosyllactose	Preclinical				
4-HQN	Preclinical	PARP inhibitor	PARP1		
4-hydroxy-phenazone	Preclinical				
4-IBP	Preclinical	sigma receptor agonist	SIGMAR1		
4-iodo-L-phenylalanine	Preclinical		DPP4		
4-iodo-6-phenylpyrimidine	Preclinical	macrophage migration inhibiting factor inhibitor	MIF		
4-methylgenistein	Preclinical	protein tyrosine kinase inhibitor	CYP19A1|ESRRA|ESRRB|ESRRG|FASN		
4-methylhistamine	Preclinical	histamine receptor agonist	HRH4		
4-mu-8C	Preclinical	IRE1 inhibitor	ERN1		
4-P-PDOT	Preclinical	melatonin receptor antagonist	MTNR1A|MTNR1B		
4-phenolsulfonic-acid	Preclinical				
"4-phenyl-1,2,3,4-tetrahydroisoquinoline"	Preclinical	dopamine release inhibitor			
4-PPBP	Preclinical	sigma receptor ligand	SIGMAR1		
4-propylbenzoic-acid	Preclinical				
4-pyrimidinecarbonitrile	Preclinical				
4-tert-butylphenol	Preclinical				
4BP-TQS	Preclinical	nicotinic receptor agonist	CHRNA7		
4EGI-1	Preclinical	protein synthesis inhibitor	EIF4E		
4E1RCat	Preclinical	protein synthesis inhibitor	EIF4E|EIF4G1		
4SC-202	Phase 1	HDAC inhibitor	HDAC1		
5'-chloro-5'-deoxy-ENBA-(+/-)	Preclinical	adenosine receptor agonist	ADORA1		
"5,7-dichlorokynurenic-acid"	Preclinical	glutamate receptor antagonist	GLRA2|GRIN1|GRIN2A|GRIN2B|GRIN2C|GRIN2D		
"5-(4chlorophenyl)-4-ethyl-2,4-dihydro-3H-1,2,4-triazol-3-one"	Preclinical				
"5-amino-3-D-ribofuranosylthiazolo[4,5-d]pyrimidin-2,7(3H,6H)-dione"	Preclinical		TLR7		
5-aminolevulinic-acid	Launched	oxidizing agent	ALAD	oncology|dermatology	glioma|actinic keratosis (AK)
5-BDBD	Preclinical	purinergic receptor antagonist	P2RX4		
5-carboxamidotryptamine	Preclinical	serotonin receptor agonist	HTR1A|HTR1B|HTR1D|HTR1E|HTR1F|HTR2A|HTR2B|HTR2C|HTR5A|HTR6|HTR7		
5-fluoro-3-pyridyl-methanol	Preclinical				
5-fluoropyrimidine	Phase 3	kinase inhibitor			
5-fluorouracil	Launched	thymidylate synthase inhibitor	DPYD|TYMS	oncology	colorectal cancer|breast cancer|pancreatic cancer|gastric adenocarcinoma
5-FP	Phase 1	thymidylate synthase inhibitor	TYMS		
5-HMF	Phase 2				
5-hydroxydecanoic-acid	Preclinical				
5-hydroxyectoine	Preclinical				
5-hydroxymethyl-tolterodine	Phase 1	acetylcholine receptor antagonist	CHRM3		
5-hydroxytryptophan	Launched	neurotransmitter	SLC36A1|SLC36A2	neurology/psychiatry	insomnia
5-iodo-A-85380	Phase 2	acetylcholine receptor agonist			
5-methylfurmethiodide	Preclinical	acetylcholine receptor agonist	CHRM1|CHRM2|CHRM3|CHRM4		
5-methylhydantoin-(D)	Preclinical				
5-methylhydantoin-(L)	Preclinical				
5-octanoylsalicylic-acid	Preclinical	protein kinase activator			
"6,7-dehydro-17-acetoxy-progesterone"	Preclinical	steroidal progestin			
6-aminochrysene	Phase 2	transferase inhibitor			
6-aminopenicillanic-acid	Preclinical				
6-benzylaminopurine	Preclinical	purinergic receptor activator			
6-chloromelatonin	Preclinical	melatonin receptor agonist	MTNR1A|MTNR1B		
6-diazo-5-oxo-L-norleucine	Preclinical	glutamate receptor antagonist|glutaminase inhibitor			
6-iodo-nordihydrocapsaicin	Preclinical	TRPV antagonist	TRPV1		
"7,8,9,10-tetrahydroazepino[2,1-b]quinazolin-12(6H)-one"	Preclinical				
7-aminocephalosporanic-acid	Preclinical	beta lactamase inhibitor			
7-chlorokynurenic-acid	Preclinical	glutamate receptor antagonist	GRIN1|GRIN2A|GRIN2B|GRIN2C		
7-hydroxy-DPAT	Preclinical	dopamine receptor agonist	DRD2|DRD3		
7-hydroxy-PIPAT	Preclinical	dopamine receptor ligand	DRD3		
7-hydroxystaurosporine	Phase 2	CDK inhibitor|CHK inhibitor|PKC inhibitor	CDK1|CHEK1|CHEK2|GSK3B|LCK|MAPK14|MARK1|MARK3|PDPK1|PRKCA|PRKCB|PRKCD|PRKCE|PRKCG		
7-keto-DHEA	Launched	steroid			
7-methoxytacrine	Phase 2	acetylcholinesterase inhibitor	ACHE		
7-methylxanthine	Phase 2	adenosine receptor antagonist			
7-nitroindazole	Preclinical	nitric oxide synthase inhibitor	NOS1|NOS2|NOS3		
8-bromo-cAMP	Preclinical	PKA activator			
8-bromo-cGMP	Preclinical	PKA activator	PRKG1		
8-hydroxy-DPAT	Preclinical	serotonin receptor agonist	HTR5A|HTR7		
8-hydroxy-PIPAT	Preclinical	dopamine receptor ligand	DRD2|DRD3		
8-M-PDOT	Preclinical	melatonin receptor agonist	MTNR1A|MTNR1B		
80841-78-7	Preclinical				
9-aminoacridine	Preclinical				
9-aminocamptothecin	Phase 2	topoisomerase inhibitor	TOP1		
9-anthracenecarboxylic-acid	Preclinical		ANO1|CLCN1