Initial Combination Therapy With Sitagliptin, a Dipeptidyl Peptidase-4 Inhibitor, and Metformin for Patients With Type 2 Diabetes Mellitus

Tina Vilsbøll


Expert Rev Endocrinol Metab. 2008;3(1):13-19. 

In This Article


As a new class of OADs, DPP-4 inhibitors have many important advantages over other currently available antidiabetic drugs. Compared with currently available insulin secretagogues, DPP-4 inhibitors, by enhancing biologically active (intact) GLP-1, increase insulin secretion and suppress glucagon secretion in a glucose-dependent manner. As a result, DPP-4 inhibitors induce less risk of hypoglycemia than observed with insulin, sulfonylureas or meglitinides. Second, unlike the weight gain typically observed with all currently available drugs - except metformin - treatment with DPP-4 inhibitors produce no weight gain, in spite of the improvement in glycemic control.

Initial combination therapy of sitagliptin, a once-daily, orally active, potent selective and reversible DPP-4 inhibitor and metformin (Janumet), demonstrates a substantial, additive and sustained efficacy on glycemic control in patients with T2DM.[38] Concomitantly, the initial combination therapy is associated with a low incidence of hypoglycemia, despite marked improvements in glycemic control, which is consistent with the glucose dependency of the incretin hormones. The gastrointestinal AEs of the combination therapy with sitagliptin and metformin were similar to that of metformin monotherapy. The dosage of Janumet should be individualized on the basis of the patient's current regimen, effectiveness and tolerability while not exceeding the maximum recommended daily dose of sitagliptin 100 mg and metformin 2000 mg. Janumet should generally be administered twice daily with meals, with gradual dose escalation, in order to reduce the gastrointestinal side effects due to metformin, but the starting dose of Janumet should be based on the patient's current regimen.


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