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PSN821 is an orally active small molecule that acts as a G-protein-coupled receptor 119 (GPR119) agonist. It was developed for the treatment of type 2 diabetes mellitus and obesity. The drug works by stimulating GPR119, which leads to glucose-dependent insulin secretion and may also increase incretin hormones such as glucagon-like peptide-1 (GLP-1), resulting in improved glycemic control and potential weight loss. Preclinical studies demonstrated effective glucose lowering and reductions in body weight. Clinical development reached Phase II for type 2 diabetes before being discontinued. The original developer was Prosidion, later acquired by Astellas Pharma; AstraZeneca had an option agreement to acquire the asset.
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