Drug intelligence / Profile preview

sitagliptin + mitiglinide

Development stage
Phase 1
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Sitagliptin + mitiglinide is a fixed-dose combination of two oral antidiabetic agents used in the management of type 2 diabetes mellitus. Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor that increases incretin levels, thereby enhancing glucose-dependent insulin secretion and suppressing glucagon release. Mitiglinide is a rapid-acting insulin secretagogue from the meglitinide class, which stimulates insulin secretion by blocking ATP-sensitive potassium channels on pancreatic beta cells. The combination provides additive postprandial glucose-lowering effects without significantly increasing the risk of hypoglycemia compared to monotherapy, though caution is advised in patients with renal impairment due to increased exposure and risk[1][2][6]. This combination targets both fasting and postprandial plasma glucose for improved glycemic control in adults with type 2 diabetes[1][3][6].

02

Targets

KATP channel (ATP-sensitive potassium channel)DPP-4 (Dipeptidyl Peptidase-IV)SUR1 (Sulfonylurea receptor 1)KCNJ10 (Kir4.1)PPARG (Peroxisome proliferator-activated receptor gamma)

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