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DAVID Q. PHAM, PHARM.D., BCPS, is Assistant Professor of Pharmacy Practice, College of Pharmacy and Health Sciences, Western University, Pomona, CA, and Research and Clinical Education Coordinator, Fountain Valley Regional Hospital and Medical Center, Fountain Valley, CA. ANNA NOGID, B.S., PHARM.D., BCPS, is Assistant Professor of Pharmacy Practice, Arnold & Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY, and Critical Care Specialist, Brookdale University Hospital and Medical Center, Brooklyn. RODA PLAKOGIANNIS, B.S., PHARM.D., BCPS, is Associate Professor of Pharmacy Practice, Arnold & Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, and Clinical Pharmacy Manager—Primary Care, Montefiore Medical Group, New York.

Address correspondence to Dr. Pham at the College of Pharmacy and Health Sciences, Western University, 309 East Second Street, Pomona, CA 91766-1854 (dqpham{at}westernu.edu).

Purpose. The pharmacologic, pharmacokinetic, safety, clinical efficacy, and role of sitagliptin in the management of type 2 diabetes mellitus are reviewed. Summary. Sitagliptin is a dipeptidyl-peptidase IV (DPP4) inhibitor that increases insulin release and decreases glucagon levels by preventing the activation of incretin hormones—glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide. The clinical trials reviewed provide evidence that sitagliptin, either alone or in combination with metformin or thiazolidinediones, is effective in reducing glycosylated hemoglobin (HbA1c), fasting plasma glucose, and two-hour postprandial glucose levels in patients with type 2 diabetes. Specifically, sitagliptin has a role in patients who have been compliant with their oral hypoglycemic agents but unable to attain target HbA1c values with monotherapy and lifestyle modifications. Sitagliptin is generally well tolerated, with the frequency of adverse events being similar to placebo and a low frequency of hypoglycemia. Sitagliptin does not appear to alter the pharmacokinetics of metformin, rosiglitazone, glyburide, simvastatin, warfarin, or oral contraceptives. The addition of sitagliptin to a patient’s oral antidiabetic regimen would necessitate close monitoring for adverse events and possible drug interactions. The sitagliptin dosage recommended by the manufacturer is 100 mg once daily as monotherapy or in combination with metformin or a thiazolidinedione. No formal pharmacoeconomic evaluations of sitagliptin therapy have been conducted. Conclusion. Sitagliptin, a DPP4 inhibitor, offers a novel treatment option for patients with type 2 diabetes mellitus. Index terms: Antidiabetic agents; Combined therapy; Diabetes mellitus; Dosage; Drug interactions; Mechanism of action; Metformin; Pharmacokinetics; Sitagliptin; Thiazolidinediones; Toxicity