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

General Information of Drug (ID: DMTPB8A)

Drug Name

INT-777 Drug Info

Synonyms

TGR5 agonist (oral, metabolic disorder), Intercept

Indication

Disease Entry	ICD 11	Status	REF
Metabolic disorder	5C50-5D2Z	Investigative	[1]

Cross-matching ID

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Clinical Trial Drug(s)

Patented Agent(s)

Preclinical Drug(s)

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Drug(s) Targeting G-protein coupled bile acid receptor 1 (GPBAR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Sodium taurocholate	DM3GO0J	Type-2 diabetes	5A11	Phase 1/2	[3]
Bile acid	DM9UZD7	Discovery agent	N.A.	Phase 1	[4]
PMID29649907-Compound-INT767	DMA0RI8	N. A.	N. A.	Patented	[5]
PMID29649907-Compound-8	DMV2D5M	N. A.	N. A.	Patented	[5]
INT-767	DMRJ9P4	Hepatic fibrosis	DB93.0	Preclinical	[6]
XL475	DMD8TNK	Type-2 diabetes	5A11	Preclinical	[7]
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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
G-protein coupled bile acid receptor 1 (GPBAR1)	TTSDVTR	GPBAR_HUMAN	Agonist	[2]

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References

1	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7048).
2	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 37).
3	Bile acids and sphingosine-1-phosphate receptor 2 in hepatic lipid metabolism.Acta Pharmaceutica Sinica B Volume 5, Issue 2, March 2015, Pages 151-157.
4	Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5718-21.
5	Farnesoid X receptor modulators 2014-present: a patent review.Expert Opin Ther Pat. 2018 May;28(5):351-364.
6	FXR/TGR5 Dual Agonist Prevents Progression of Nephropathy in Diabetes and Obesity. J Am Soc Nephrol. 2018 Jan;29(1):118-137.
7	Clinical pipeline report, company report or official report of Exelixis (2011).