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Sitagliptin is a dipeptidyl peptidase-4 (DPP4) inhibitor [1].

DPP4 is an antigenic enzyme expressed on the surface of most cell types associated with immune regulation, signal transduction and apoptosis. DPP4 is an intrinsic membrane glycoprotein and a serine exopeptidase that cleaves X-proline dipeptides from the N-terminus of polypeptides [2].

In vitro: Sitagliptin was a potent inhibitor for DPP-4 with an IC50 of 18 nM [1]. Sitagliptin inhibited DPP-8 with an IC50 of 48 μM. Sitagliptin showed no effect on several related peptidases, including DPP-9, DPP-II, and amino peptidase P [1].

Clinical trials: In patients with type 2 diabetes, once-daily sitagliptin monotherapy improved glycemic control in the fasting and postprandial states, improved measures of β-cell function. Sitagliptin was well tolerated [3]. Sitagliptin did not increase the risk of major adverse cardiovascular events, hospitalization for heart failure, or other adverse events [4].

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