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Overview
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Dipeptidyl peptidase IV (DPP-IV) inhibitor.
Vildagliptin, also known as LAF237, is a potent and selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin inhibits the inactivation of glucagon-like peptide-1 (GLP-1) and gastric inhibitory peptide (GIP) by DPP-IV, allowing GLP-1 and GIP to potentiate the secretion of insulin and suppress glucagon release in the pancreas. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity in type 2 diabetes.
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