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

General Information of Drug (ID: DM3XRUH)

Drug Name

LJN452 Drug Info

Synonyms

Tropifexor; 1383816-29-2; UNII-NMZ08KM76Z; NMZ08KM76Z; CPD1549; Tropifexor [INN]; GTPL9725; SCHEMBL19178329; SCHEMBL17848159; LJN-452; EX-A1934; CS-8153; compound 1 [PMID: 29148806]; ACN-053193; AC-30341; 2-[(1R,3r,5S)-3-({5-cyclopropyl-3-[2-(trifluoromethoxy)phenyl]-1,2-oxazol-4-yl}methoxy)-8-azabicyclo[3.2.1]octan-8-yl]-4-fluoro-1,3-benzothiazole-6-carboxylic acid; HY-107418; 2-((1R,5S)-3-((5-cyclopropyl-3-(2-(trifluoromethoxy)phenyl)isoxazol-4-yl)methoxy)-8-azabicyclo[3.2.1]octan-8-yl)-4-fluorob

Indication

Disease Entry	ICD 11	Status	REF
Primary biliary cholangitis	DB96.1	Phase 2	[1]

Cross-matching ID

PubChem CID: 121418176
CAS Number: CAS 1383816-29-2
TTD Drug ID: DM3XRUH

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	[3]
Guggulsterone	DMP7LK1	Osteoarthritis	FA00-FA05	Approved	[4]
obeticholic acid	DM3Q1SM	Primary biliary cholangitis	DB96.1	Approved	[5]
GS-9674	DM936V7	Primary sclerosing cholangitis	DB96.2	Phase 3	[6]
Apomine	DM6B9HP	Osteopetrosis	LD24.10	Phase 2	[7]
EYP001	DM5PBLM	Non-alcoholic steatohepatitis	DB92.1	Phase 2	[8]
EDP-305	DMGJYZ8	Non-alcoholic steatohepatitis	DB92.1	Phase 2	[9]
LMB763	DMQOXNL	Diabetic nephropathy	GB61.Z	Phase 2	[10]
MET409	DM89QXT	Non-alcoholic steatohepatitis	DB92.1	Phase 2	[11]
Turofexorate isopropyl	DM36ONA	Hyperlipidaemia	5C80	Phase 1	[12]
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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	[2]

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References

1	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2	FXR modulators for enterohepatic and metabolic diseases.Expert Opin Ther Pat. 2018 Nov;28(11):765-782.
3	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.
4	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.
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	Clinical pipeline report, company report or official report of ENYO Pharma.
9	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.
10	Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis. J Med Chem. 2020 Apr 23;63(8):3868-3880.
11	Clinical pipeline report, company report or official report of Metacrine.
12	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.