Carmegliptin is a potent, long-acting, selective, orally bioavailable, pyrrolidinone-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. ). DPP-IV is a proline-specific serine protease enzyme that is known to rapidly inactivate two incretin hormones released during food ingestion, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). Incretins are essential for regulating both fasting and postprandial plasma glucose by stimulating insulin secretion, supporting β-cell mass, and inhibiting glucagon production by the α-cells to reduce glucose production by the liver. By selectively inhibiting DPP-IV, carmegliptin prolongs the activity of circulating GLP-1 and GIP and improves their potential to prolong the antidiabetic actions. Carmegliptin is indicated for use as monotherapy or in combination with other oral antihyperglycemic agents for the treatment of Type 2 diabetes.