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Sitagliptin


Mechanism of action:

Sitagliptin is a dipeptidyl peptidase-4 inhibitor (dipeptidyl peptidase-4 inhibitor). Dipeptidyl peptidase-4 (DPP-4) is an enzyme responsible for degrading incretins, such as glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide. When sitagliptin inhibits dipeptidyl peptidase-4, incretins are less readily degraded, so their blood concentration and duration of action are prolonged. This promotes insulin secretion from pancreatic beta cells and suppresses glucagon secretion from pancreatic alpha cells.

Reference(s):

1. Herman GA et al. (2005). Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses. Clin Pharmacol Ther. 


2. Herman GA et al. (2006). Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects. J Clin Pharmacol. 


3. Karasik A et al. (2008). Sitagliptin, a DPP-4 inhibitor for the treatment of patients with type 2 diabetes: a review of recent clinical trials. Curr Med Res Opin.

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