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COLLEEN D. LAUSTER, PHARM.D., CDE, is Assistant Professor, School of Pharmacy, University of Pittsburgh (UP), and Internal Medicine Pharmacist, UP Medical Center, Pittsburgh, PA. TERESA P. MCKAVENEY, B.S., is Research Assistant, School of Pharmacy, UP. SARAH V. MUENCH, PHARM.D., CDE, is Ambulatory Care Specialist, William Beaumont Hospital, Royal Oak, MI.

Address correspondence to Dr. Lauster at the Department of Pharmacy and Therapeutics, School of Pharmacy, University of Pittsburgh, 302 Scaife Hall, 200 Lothrop Street, Pittsburgh, PA 15261 (laustercd{at}upmc.edu).

Purpose. The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, drug interactions, and role in therapy of vildagliptin for the treatment of type 2 diabetes mellitus were reviewed. Summary. Vildagliptin is an agent in a new class of medications called dipeptidyl peptidase IV (DPP4) inhibitors. By inhibiting DPP4, vildagliptin causes an increase in glucagon like peptide-1 (GLP-1), an intestinal hormone that aids in glucose homeostasis and insulin secretion. The manufacturer of vildagliptin received an approvable letter from the Food and Drug Administration in late February 2007. Vildagliptin has a halflife of about 90 minutes; however, 50% of DPP4 inhibition continues for more than 10 hours, allowing for once- or twice-daily dosing. Clinical trials have shown that vildagliptin is effective in significantly lowering glycosylated hemoglobin (HbA1c), fasting plasma glucose, and prandial glucose levels. Beta-cell function may also be improved. The most common adverse effects in patients receiving vildagliptin included headache, nasopharyngitis, cough, constipation, dizziness, and increased sweating. In most studies, the rate of hypoglycemia appeared to be similar to that of placebo. Conclusion. In clinical trials of patients with type 2 diabetes mellitus, vildagliptin has been shown to reduce HbA1c, fasting plasma glucose levels, prandial glucose levels, and prandial glucagon secretion and to improve ß-cell function. If vildagliptin is approved for marketing, it will add to the available treatment options for diabetes and will provide patients and health care providers with another noninjectable therapy option. Index terms: Antidiabetic agents; Diabetes mellitus; Dosage schedules; Drug interactions; Duration of action; Half-life; Mechanism of action; Pharmacokinetics; Toxicity; Vildagliptin