Vildagliptin is an inhibitor of dipeptidyl peptidase 4 (DPP-4, Ki = 0.003 µM). It is selective for DPP-4 over DPP-2, DPP-8, and DPP-9 (Kis = >500, 0.81, and 0.095 µM, respectively). Vildagliptin (3 mg/kg) decreases plasma glucose levels and increases plasma insulin levels during an oral glucose challenge in Zucker...

Inhibits the inactivation of GLP-1 and GIP by DPP-4, allowing GLP-1 and GIP to potentiate the secretion of insulin in the beta cells and suppress glucagon release by the alpha cells of the islets of Langerhans in the pancreas.