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IDG-16177 is a potent, orally bioavailable small molecule agonist of G protein-coupled receptor 40 (GPR40), also known as free fatty acid receptor 1 (FFAR1), developed primarily for the treatment of type 2 diabetes mellitus. It acts by stimulating GPR40 on pancreatic β-cells, which enhances glucose-stimulated insulin secretion in a glucose-dependent manner. IDG-16177 has demonstrated higher potency and efficacy than fasiglifam (TAK-875) in preclinical studies, with favorable pharmacokinetic properties including high oral bioavailability across multiple species. Mechanistically, it stimulates both β-arrestin and gastrointestinal hormone pathways to promote insulin release and improve glucose tolerance. The drug is currently in phase I clinical trials for type 2 diabetes mellitus.
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