Drug intelligence / Profile preview

sitagliptin + gliclazide

Development stage
Phase 4
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Sitagliptin + gliclazide is an oral combination therapy for type 2 diabetes mellitus (T2DM). Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that increases levels of incretin hormones, such as glucagon-like peptide-1 (GLP-1), thereby enhancing glucose-dependent insulin secretion and suppressing glucagon release. Gliclazide is a sulfonylurea that stimulates pancreatic beta cells to secrete more insulin, independent of blood glucose levels. The combination targets different mechanisms in glucose regulation—sitagliptin acts via incretin enhancement while gliclazide directly stimulates insulin secretion—providing additive glycemic control. This combination may be considered in patients with T2DM who require dual oral therapy for improved glycemic management when monotherapy is insufficient.

02

Targets

KCNJ11 (Atp-sensitive inward rectifier potassium channel 11)DPP-4 (Dipeptidyl Peptidase-IV)SUR1 (Sulfonylurea receptor 1)KATP channel (ATP-sensitive potassium channel)

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