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Vildagliptin: novel pharmacological approach to treat Type 2 diabetes

Bo Ahraain

Vildagliptin is an orally active inhibitor of the enzyme dipeptidyl peptidase-4. It prevents the inactivation of the gut hormone glucagon-like peptide-1, which results in increased endogenous levels of the hormone. This stimulates insulin secretion and inhibits glucagon secretion by increasing the glucose sensitivity of the pancreatic α- and β-cells. A large body of evidence shows that vildagliptin improves glycemic control in subjects with Type 2 diabetes. Thus, vildagliptin reduces hemoglobin (Hb)-A_1c by 0.8–1.1% from baseline levels of 7.7–8.5% as monotherapy in Type 2 diabetes. Furthermore, vildagliptin reduces HbA_1c when used in combination therapy with metformin, a thiazolidinedione, a sulfonylurea or insulin. Moreover, vildagliptin is well tolerated, the risk of hypoglycemia is low and body weight is not increased during the treatment. Therefore, vildagliptin represents a novel pharmacological therapy for Type 2 diabetes. Its main potential is as an add-on therapy to metformin in patients with insufficient glycemic control, as an add-on to sulfonylurea and as a first-line treatment as monotherapy in patients who are intolerant to or have contraindications for metformin.