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ZYDG2 is a potent, selective small molecule agonist of the G protein-coupled receptor 40 (GPR40), also known as free fatty acid receptor 1. It was developed by Zydus Cadila Healthcare for the treatment of type 2 diabetes mellitus. GPR40 is predominantly expressed in pancreatic β-cells and mediates glucose-stimulated insulin secretion in response to free fatty acids. In preclinical studies, ZYDG2 demonstrated dose-dependent improvement in glucose tolerance and increased insulin secretion without tachyphylaxis or liver toxicity—an issue that led to discontinuation of the earlier GPR40 agonist fasiglifam. The compound showed high oral bioavailability across multiple species and a favorable safety profile with no observed adverse effects at doses up to 300 mg/kg over repeated administration[1][2].
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