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Saxagliptin: A New Dipeptidyl Peptidase-4 Inhibitor for Type 2 Diabetes

Lam, Sum PharmD*†; Saad, Maha PharmD*‡

doi: 10.1097/CRD.0b013e3181daad5f
New Therapy Update

Type 2 diabetes mellitus is a common chronic disease that causes significant morbidity and mortality worldwide. The primary goal of treatment is to target glycemic control by maintaining the glycosylated hemoglobin (HbA1c) level near 6% to 7% without predisposing patients to hypoglycemia. Currently available antidiabetic agents work by different mechanisms to lower blood glucose levels. Unfortunately, each of them has its tolerability and safety concerns that limit use and dose titration. Dipeptidyl peptidase-4 enzyme inhibitors are novel drugs that prolong the action of incretins, and lead to increased insulin secretion and reduced hepatic glucose production. Saxagliptin is another dipeptidyl peptidase-4 (after sitagliptin) that is approved for the management of type 2 diabetes. It can be used alone or in combination with metformin, sulfonylurea, or thiazolidinedione (pioglitazone or rosiglitazone) when treatment with one drug alone provides inadequate glucose control. The usual adult dose is 2.5 to 5 mg once daily regardless of meals. A daily dose of 2.5 mg is recommended for patients with moderate to severe renal impairment or those who are taking potent CYP 3A4 inhibitors. In randomized clinical trials, saxagliptin alone lowered HbA1c levels by about 0.5%; with better efficacy seen when combined with other agents. It is well tolerated with the most common side effects being upper respiratory tract infection, headache, and urinary tract infection. In summary, saxagliptin is an option as an adjunct to lifestyle modifications and other antidiabetic agents to target glycemic control. It is also an alternative therapy for patients who have contraindications or intolerability to other antidiabetic agents.

From the *Department of Clinical Pharmacy Practice, College of Pharmacy and Allied Health Professions, St. John's University, Queens, NY; †Divisions of Geriatric Medicine and Pharmacy, Winthrop University Hospital, Mineola, NY; and ‡Department of Pharmacy, Long Island Jewish Medical Center, New Hyde Park, NY.

Correspondence: Sum Lam, PharmD, Department of Clinical Pharmacy Practice, College of Pharmacy and Allied Health Professions, St. John's University, St. Albert's Hall Room 114, 8000 Utopia Parkway, Queens, NY 11439. E-mail:

© 2010 Lippincott Williams & Wilkins, Inc.