Vildagliptin: a DPP-4 inhibitor for the treatment of Type 2 diabetes

Abstract

SUMMARY The key defect in Type 2 diabetes is islet dysfunction, which includes impaired insulin secretion, augmented glucagon secretion and reduced β-cell mass. The incretin hormone GLP-1 targets this islet dysfunction. GLP-1 is inactivated by DPP-4 and, consequently, DPP-4 inhibition has evolved as an efficient treatment of hyperglycemia in Type 2 diabetes since it increases the concentrations of intact GLP-1. Several DPP-4 inhibitors have been developed and all of them have been shown to be efficient in improving glycemia with a low risk for adverse events. This article reviews basic and clinical studies on one of the DPP-4 inhibitors, vildagliptin. It is a specific inhibitor of DPP-4 and improves glycemia both when used in monotherapy and when used as an add-on to metformin, sulfonylurea, thioazolidinedione or insulin in subjects with Type 2 diabetes. Clinical studies have shown that vildagliptin reduces HbA1c in association with a low risk of adverse events, including hypoglycemia, and no weight gain....