Drug intelligence / Profile preview

MK0626

Development stage
Preclinical
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

MK0626 is a selective small molecule inhibitor of dipeptidyl peptidase-4 (DPP-4), developed as an antidiabetic agent for the treatment of type 2 diabetes and for its potential to ameliorate metabolic complications such as hepatic steatosis and pancreatic islet injury. Its mechanism of action involves inhibition of DPP-4, leading to enhanced endogenous glucagon-like peptide-1 (GLP-1) signaling, increased AMP-activated protein kinase (AMPK) activity, improved beta-cell function, anti-oxidative effects, and anti-apoptotic actions in preclinical models. MK0626 is structurally and mechanistically related to other DPP-4 inhibitors such as sitagliptin and has been shown in animal models to reduce hepatic lipid accumulation, improve insulin sensitivity, attenuate hyperglycemia, restore pancreatic islet morphology and function following injury (e.g., after tacrolimus administration), and exert protective effects against oxidative stress[1][2][3][5][7][8][9].

02

Targets

DPP-4 (Dipeptidyl Peptidase-IV)

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