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

General Information of DTT (ID: TTS4UGC)

• DTT Name: Farnesoid X-activated receptor (FXR) DTT Info
• UniProt ID: NR1H4_HUMAN
• Gene Name: NR1H4

Molecule-Related Drug & Molecule List

3 Approved Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Chenodiol	DMQ8JIK	Cholelithiasis	DC11	Approved	[1], [2]
Guggulsterone	DMP7LK1	Osteoarthritis	FA00-FA05	Approved	[3], [4]
Obeticholic acid	DM3Q1SM	Primary biliary cholangitis	DB96.1	Approved	[5]

11 Clinical Trial Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Bevacizumab + Trastuzumab	DM9CEI5	Breast cancer	2C60-2C65	Phase 3	[1]
GS-9674	DM936V7	Primary sclerosing cholangitis	DB96.2	Phase 3	[6]
Apomine	DM6B9HP	Osteopetrosis	LD24.10	Phase 2	[7]
EDP-305	DMGJYZ8	Non-alcoholic steatohepatitis	DB92.1	Phase 2	[8]
EYP001	DM5PBLM	Non-alcoholic steatohepatitis	DB92.1	Phase 2	[9]
LJN452	DM3XRUH	Primary biliary cholangitis	DB96.1	Phase 2	[10], [11]
LMB763	DMQOXNL	Diabetic nephropathy	GB61.Z	Phase 2	[12]
MET409	DM89QXT	Non-alcoholic steatohepatitis	DB92.1	Phase 2	[13]
AGN-242266	DMVHPOX	Non-alcoholic steatohepatitis	DB92.1	Phase 1	[14]
PX-102	DMWU682	Hepatic fibrosis	DB93.0	Phase 1	[15]
Turofexorate isopropyl	DM36ONA	Hyperlipidaemia	5C80	Phase 1	[16]

45 Patented Agent(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID29649907-Compound-1	DMDKT9X	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-10	DMNE9AX	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-11	DMSC9MH	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-12	DMBHT2E	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-13	DMLBQUS	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-14	DMQAV30	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-15	DMMIKFU	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-18	DMBVOZK	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-19	DMFL38V	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-2	DMM4TBH	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-20	DMGNW34	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-21	DMES0UY	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-22	DMXW108	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-23	DMW7T45	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-24	DMUHNS7	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-25	DMALOEW	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-26	DM6O78C	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-27	DMQDGZL	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-28	DMYMKZC	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-29	DMEVZIK	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-3	DMPVSG9	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-30	DM0SY7Q	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-31	DME6H8Q	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-32	DM7E9HA	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-33	DM39HCU	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-34	DMUDKE0	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-35	DMSWJPO	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-36	DMP5KEW	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-37	DM8WKYT	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-38	DMMP09F	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-39	DMI3ELU	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-4	DMO45VP	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-40	DMS6UD2	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-41	DM26IRH	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-42	DMSAD9B	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-44	DMBA2S3	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-5	DMDWSIE	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-8	DMV2D5M	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-9	DMA6H4W	N. A.	N. A.	Patented	[17]
PMID29649907-Compound-INT767	DMA0RI8	N. A.	N. A.	Patented	[17]
PMID30259754-Compound-INT-767	DME0RJ2	N. A.	N. A.	Patented	[10]
PMID30259754-Compound-LY2562175	DMZ5CDY	N. A.	N. A.	Patented	[10]
PMID30259754-Compound-Px-102	DM78IN5	N. A.	N. A.	Patented	[10]
PMID30259754-Compound-pyrrole[2,3-d]azepines	DMVP16K	N. A.	N. A.	Patented	[10]
PMID30259754-Compound-WAY-362450	DMDKSJQ	N. A.	N. A.	Patented	[10]

2 Discontinued Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
SB-756050	DMXFQS1	Type-2 diabetes	5A11	Discontinued in Phase 2	[18]
SKF-97426	DM40HTZ	Hyperlipidaemia	5C80	Discontinued in Phase 2	[19]

1 Preclinical Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
INT-767	DMRJ9P4	Hepatic fibrosis	DB93.0	Preclinical	[20]

8 Investigative Drug(s) Transported by This DTP

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
1,1-bisphosphonate esters	DMG362U	Discovery agent	N.A.	Investigative	[7]
12-O-deacetyl-12-epi-19-deoxy-21-hydroxyscalarin	DMKH0OC	Discovery agent	N.A.	Investigative	[4]
22R-hydroxycholesterol	DME8273	Discovery agent	N.A.	Investigative	[21]
AGN-34	DM5ECDM	Discovery agent	N.A.	Investigative	[22]
cholesten	DMKM3WJ	Discovery agent	N.A.	Investigative	[23]
Desmosterol	DMV8SUM	Discovery agent	N.A.	Investigative	[23]
Fexaramine	DMWCLQ5	Discovery agent	N.A.	Investigative	[24]
GW4065	DMFRP7H	Discovery agent	N.A.	Investigative	[1]

References

• [1] 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.
• [2] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [3] 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.
• [4] Scalarane sesterterpenes from a marine sponge of the genus Spongia and their FXR antagonistic activity. J Nat Prod. 2007 Nov;70(11):1691-5.
• [5] 2016 FDA drug approvals. Nat Rev Drug Discov. 2017 Feb 2;16(2):73-76.
• [6] 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.
• [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] 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.
• [9] Clinical pipeline report, company report or official report of ENYO Pharma.
• [10] FXR modulators for enterohepatic and metabolic diseases.Expert Opin Ther Pat. 2018 Nov;28(11):765-782.
• [11] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [12] Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis. J Med Chem. 2020 Apr 23;63(8):3868-3880.
• [13] Clinical pipeline report, company report or official report of Metacrine.
• [14] Clinical pipeline report, company report or official report of AbbVie.
• [15] An FXR Agonist Reduces Bile Acid Synthesis Independently of Increases in FGF19 in Healthy Volunteers. Gastroenterology. 2018 Oct;155(4):1012-1016.
• [16] 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.
• [17] Farnesoid X receptor modulators 2014-present: a patent review.Expert Opin Ther Pat. 2018 May;28(5):351-364.
• [18] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [19] SK&F 97426-A a more potent bile acid sequestrant and hypocholesterolaemic agent than cholestyramine in the hamster. Atherosclerosis. 1993 Jun;101(1):51-60.
• [20] FXR/TGR5 Dual Agonist Prevents Progression of Nephropathy in Diabetes and Obesity. J Am Soc Nephrol. 2018 Jan;29(1):118-137.
• [21] Oxysterol 22(R)-hydroxycholesterol induces the expression of the bile salt export pump through nuclear receptor farsenoid X receptor but not liver ... J Pharmacol Exp Ther. 2006 Apr;317(1):317-25.
• [22] Farnesoid X receptor: from structure to potential clinical applications. J Med Chem. 2005 Aug 25;48(17):5383-403.
• [23] Identification of farnesoid X receptor beta as a novel mammalian nuclear receptor sensing lanosterol. Mol Cell Biol. 2003 Feb;23(3):864-72.
• [24] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.