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Denagliptin is an orally active, selective inhibitor of dipeptidyl peptidase-4 (DPP-4), an enzyme responsible for the degradation of incretin hormones such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). By inhibiting DPP-4, denagliptin increases the levels of active incretins, which stimulates insulin secretion and suppresses glucagon release in a glucose-dependent manner, thereby improving glycemic control in patients with type 2 diabetes mellitus. Developed by GSK, the compound reached Phase 2 clinical trials but development was ultimately discontinued.
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