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Carmegliptin is a potent, long-acting, selective, orally bioavailable small molecule inhibitor of dipeptidyl peptidase 4 (DPP-4), developed for the treatment of type 2 diabetes mellitus. As a pyrrolidinone-based DPP-4 inhibitor, it works by preventing the rapid inactivation of incretin hormones such as glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). These incretins are important for regulating blood glucose levels by stimulating insulin secretion, supporting β-cell mass, and inhibiting glucagon production. By prolonging the activity of GLP-1 and GIP through DPP-IV inhibition, carmegliptin enhances their antidiabetic effects. The drug has been studied as both monotherapy and in combination with other oral antihyperglycemic agents in phase 2 clinical trials but has not received regulatory approval[1][2][3][5][7].
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