Sitagliptin: an oral agent for glucose control

Sitagliptin (Januvia™) is a new oral agent approved by the US FDA to treat Type 2 diabetes. This is the first approved agent in a new class of antihyperglycemics, dipeptidyl peptidase (DPP)-4 inhibitors. Sitagliptin selectively inhibits the action of DPP-4, the primary enzyme degrading the incretin hormones, allowing glucagon-like peptide-1 and glucose-dependent insulinotropic peptide to facilitate glucose regulation in response to a meal. Studies demonstrate that sitagliptin decreases hemaglobin A1c, postprandial glucose excursion and fasting plasma glucose. Sitagliptin presents some advantages over other drugs used in the management of diabetes. One advantage is its oral administration; another, is its low incidence of hypoglycemia, similar to that of a placebo. Sitagliptin has a low incidence of adverse events, consisting of stomach discomfort, diarrhea, upper respiratory infection, stuffy or runny nose, sore throat and headache. Unlike many other drugs used to treat diabetes, sitagliptin does not cause weight gain. Animal studies have shown that it can help prevent β-cell apoptosis and improve β-cell functioning; therefore, it may have a role in preventing diabetes, although human data are currently lacking.