Drug Information

Drug General Information
Drug ID
D0M0WV
Former ID
DIB002820
Drug Name
Fasiglifam hemihydrate
Drug Type
Small molecular drug
Indication Type 2 diabetes [ICD9: 250; ICD10:E11] Phase 3 [524575]
Company
Apollo Scientific
Structure
Download
2D MOL

3D MOL
Formula
C58H66O15S2
Canonical SMILES
CC1=CC(=CC(=C1C2=CC(=CC=C2)COC3=CC4=C(C=C3)C(CO4)CC(=O)<br />O)C)OCCCS(=O)(=O)C.CC1=CC(=CC(=C1C2=CC(=CC=C2)COC3=CC4=<br />C(C=C3)C(CO4)CC(=O)O)C)OCCCS(=O)(=O)C.O
InChI
1S/2C29H32O7S.H2O/c2*1-19-12-25(34-10-5-11-37(3,32)33)13-20(2)29(19)22-7-4-6-21(14-22)17-35-24-8-9-26-23(15-28(30)31)18-36-27(26)16-24;/h2*4,6-9,12-14,16,23H,5,10-11,15,17-18H2,1-3H3,(H,30,31);1H2/t2*23-;/m11./s1
InChIKey
OJXYMYYDAVXPIK-IWKNALKQSA-N
PubChem Compound ID
57339446
PubChem Substance ID
136350037, 162109076, 198965579, 226087965
Target and Pathway
Target(s) GPR40 Target Info Modulator [532423], [532513]
KEGG Pathway Insulin secretion
Reactome G alpha (q) signalling events
Fatty Acids bound to GPR40 (FFAR1) regulate insulin secretion
WikiPathways GPCRs, Class A Rhodopsin-like
Incretin Synthesis, Secretion, and Inactivation
Gastrin-CREB signalling pathway via PKC and MAPK
Integration of energy metabolism
GPCR ligand binding
GPCR downstream signaling
References
Ref 524575ClinicalTrials.gov (NCT02015780) Fasiglifam in Type 2 Diabetic Subjects With Chronic Kidney Disease Stage 4 or 5 on Hemodialysis. U.S. National Institutes of Health.
Ref 532423TAK-875, a GPR40/FFAR1 agonist, in combination with metformin prevents progression of diabetes and beta-cell dysfunction in Zucker diabetic fatty rats. Br J Pharmacol. 2013 Oct;170(3):568-80.
Ref 532513A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1. PLoS One. 2013 Oct 10;8(10):e76280.

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