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

Bo Ahren

The key defect in Type 2 diabetes is islet dysfunction, which includes impaired insulin secretion, augmented glucagon secretion and reduced b-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. Vildagliptin is also efficient in elderly patients and in patients with renal impairment. Its main place in therapy is as add-on to ongoing therapy with metformin in patients in whom metformin alone is insufficient for reaching the glycemic target. Vildagliptin may also be used as monotherapy in patients in whom metformin cannot be used and as an add-on to sulfonylurea or thiazolidinedione. In the future, it may also be used as an add-on to insulin therapy. There is, at present, an extensive experience with the use of vildagliptin for at least 5 years in many countries. However, long-term surveillance of its effects and safety is still of importance.