Sitagliptin: The First in a New Class of DPP-4 Inhibitors for the Treatment of Type 2 Diabetes

Abstract

Background: Sitagliptin (JANUVIA®) is the first approved dipeptidyl peptidase-4 (DPP-4) inhibitor for the treatment of type 2 diabetes mellitus (T2DM) and is approved in more than 60 countries. It is a potent, highly selective, and reversible DPP-4 inhibitor with a half-life of approximately 12 hours, allowing once-daily dosing.

Methodology: A meta-analysis of studies evaluating sitagliptin in patients with type 2 diabetes mellitus was conducted.

Results: A single daily dose achieves 24-hour DPP-4 inhibition, reaching peak inhibition within 2–4 hours and maintaining at least 80% inhibition throughout the dosing interval. Food does not significantly affect its pharmacokinetics, and the drug exhibits low protein binding with no clinically important drug–drug interactions. Clinical trials demonstrated significant reductions in HbA1c, fasting plasma glucose, and postprandial glucose levels, improvement in β-cell function, weight neutrality, and a low incidence of hypoglycaemia compared with sulfonylureas.