Article

Reappraisal of GPR40/FFAR1 as a Therapeutic Target for Type 2 Diabetes Mellitus: Systematic Cheminformatic Analysis of 2,637 Compounds in ChEMBL 36 Identifies Superior Candidates to Fasiglifam

2026-05-21

Abstract excerpt

<h4>ABSTRACT</h4> <h4>Background</h4> The discontinuation of Fasiglifam (TAK-875), a GPR40/FFAR1 full agonist, during Phase 3 clinical trials due to hepatotoxicity led to widespread abandonment of GPR40 as a viable therapeutic target for type 2 diabetes mellitus (T2DM). However, mechanistic evidence suggests that Fasiglifam’s hepatotoxicity arises from mitochondrial liability driven by high lipophilicity (aLogP...

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Literature Corpus work: 3f3fd087-1a05-5926-badf-acb433a6b136
DOI: 10.64898/2026.05.19.726272

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Reappraisal of GPR40/FFAR1 as a Therapeutic Target for Type 2 Diabetes Mellitus: Systematic Cheminformatic Analysis of 2,637 Compounds in ChEMBL 36 Identifies Superior Candidates to FasiglifamDOI 10.64898/2026.05.19.726272Read

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