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Fasiglifam is an orally available small molecule drug developed as a selective agonist and ago-allosteric modulator of the free fatty acid receptor 1 (FFAR1, also known as G-protein–coupled receptor 40 or GPR40). It was investigated primarily for the treatment of type 2 diabetes mellitus, where it demonstrated potent glucose-lowering effects by potentiating glucose-stimulated insulin secretion in a glucose-dependent manner. This mechanism offered advantages over sulfonylureas by reducing the risk of hypoglycemia. Fasiglifam reached phase III clinical trials for type 2 diabetes but its development was terminated due to concerns about liver safety. The drug was developed by Takeda[1][3][4][6][7][8].
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