Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM936V7)

Drug Name

GS-9674 Drug Info

Synonyms

Cilofexor; 1418274-28-8; UNII-YUN2306954; PX104; 1418274-28-8 (free acid); YUN2306954; 2-(3-(2-chloro-4-((5-cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl)methoxy)phenyl)-3-hydroxyazetidin-1-yl)isonicotinic acid; GS 9674; 2-[3-[2-chloro-4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-1,2-oxazol-4-yl]methoxy]phenyl]-3-hydroxyazetidin-1-yl]pyridine-4-carboxylic acid; Cilofexor [INN]; Cilofexor (GS(c)\\9674); CHEMBL4297613; SCHEMBL14641986; GTPL10644; BCP29283; BDBM50511109; GS9674; s6547; DB15168; example 13/9 [US10485795B2]; HY-109083; CS-0039260; 2-(3-(2-Chloro-4-((5-cyclopropyl-3-(2,6-dichlorophenyl)-4-isoxazolyl)methoxy)phenyl)-3-hydroxy-1-azetidinyl)-4-pyridinecarboxylic acid; 4-Pyridinecarboxylic acid, 2-(3-(2-chloro-4-((5-cyclopropyl-3-(2,6-dichlorophenyl)-4-isoxazolyl)methoxy)phenyl)-3-hydroxy-1-azetidinyl)-

Indication

Disease Entry	ICD 11	Status	REF
Primary sclerosing cholangitis	DB96.2	Phase 3	[1]
Non-alcoholic steatohepatitis	DB92.1	Phase 2	[2]

Cross-matching ID

PubChem CID: 71228883
CAS Number: CAS 1418274-28-8
TTD Drug ID: DM936V7

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

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Drug(s) Targeting Farnesoid X-activated receptor (FXR)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Chenodiol	DMQ8JIK	Cholelithiasis	DC11	Approved	[4]
Guggulsterone	DMP7LK1	Osteoarthritis	FA00-FA05	Approved	[5]
obeticholic acid	DM3Q1SM	Primary biliary cholangitis	DB96.1	Approved	[6]
Apomine	DM6B9HP	Osteopetrosis	LD24.10	Phase 2	[7]
LJN452	DM3XRUH	Primary biliary cholangitis	DB96.1	Phase 2	[8]
EYP001	DM5PBLM	Non-alcoholic steatohepatitis	DB92.1	Phase 2	[9]
EDP-305	DMGJYZ8	Non-alcoholic steatohepatitis	DB92.1	Phase 2	[10]
LMB763	DMQOXNL	Diabetic nephropathy	GB61.Z	Phase 2	[11]
MET409	DM89QXT	Non-alcoholic steatohepatitis	DB92.1	Phase 2	[12]
Turofexorate isopropyl	DM36ONA	Hyperlipidaemia	5C80	Phase 1	[13]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Farnesoid X-activated receptor (FXR)	TTS4UGC	NR1H4_HUMAN	Agonist	[3]

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References

1	ClinicalTrials.gov (NCT03890120) Safety, Tolerability, and Efficacy of Cilofexor in Non-Cirrhotic Adults With Primary Sclerosing Cholangitis (PRIMIS). U.S. National Institutes of Health.
2	ClinicalTrials.gov (NCT03449446) Study to Evaluate the Safety and Efficacy of Selonsertib, Firsocostat, Cilofexor, and Combinations in Participants With Bridging Fibrosis or Compensated Cirrhosis Due to Nonalcoholic Steatohepatitis (NASH) (ATLAS). U.S. National Institutes of Health.
3	The Nonsteroidal Farnesoid X Receptor Agonist Cilofexor (GS-9674) Improves Markers of Cholestasis and Liver Injury in Patients With Primary Sclerosing Cholangitis. Hepatology. 2019 Sep;70(3):788-801.
4	Lithocholic acid decreases expression of bile salt export pump through farnesoid X receptor antagonist activity. J Biol Chem. 2002 Aug 30;277(35):31441-7.
5	Effect of guggulsterone and cembranoids of Commiphora mukul on pancreatic phospholipase A(2): role in hypocholesterolemia. J Nat Prod. 2009 Jan;72(1):24-8.
6	2016 FDA drug approvals. Nat Rev Drug Discov. 2017 Feb 2;16(2):73-76.
7	The nuclear receptors FXR and LXRalpha: potential targets for the development of drugs affecting lipid metabolism and neoplastic diseases. Curr Pharm Des. 2001 Mar;7(4):231-59.
8	FXR modulators for enterohepatic and metabolic diseases.Expert Opin Ther Pat. 2018 Nov;28(11):765-782.
9	Clinical pipeline report, company report or official report of ENYO Pharma.
10	A novel non-bile acid FXR agonist EDP-305 potently suppresses liver injury and fibrosis without worsening of ductular reaction. Liver Int. 2020 Jul;40(7):1655-1669.
11	Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis. J Med Chem. 2020 Apr 23;63(8):3868-3880.
12	Clinical pipeline report, company report or official report of Metacrine.
13	A synthetic farnesoid X receptor (FXR) agonist promotes cholesterol lowering in models of dyslipidemia. Am J Physiol Gastrointest Liver Physiol. 2009 Mar;296(3):G543-52.