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(s) Related to This Drug


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

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Farnesoid X-activated receptor (FXR) DTT NR1H4 9.173 5.722 7.333 6.967
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Primary sclerosing cholangitis
ICD Disease Classification DB96.2
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Farnesoid X-activated receptor (FXR) DTT NR1H4 5.72E-01 0.39 1.68
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

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.