Drug intelligence / Profile preview

GW825964X

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

GW825964X is a potent and selective small molecule inhibitor of dipeptidyl peptidase 4 (DPP-IV), originally developed by GlaxoSmithKline (GSK) for the treatment of type 2 diabetes mellitus. By inhibiting DPP-IV, GW825964X prevents the enzymatic degradation of incretin hormones, such as glucagon-like peptide-1 (GLP-1), thereby prolonging their half-life and enhancing glucose-dependent insulin secretion. Preclinical studies in insulin-resistant rat models demonstrated that GW825964X significantly reduces the plasma insulin-to-glucose ratio without affecting tissue microcirculation or capillary permeability.

02

Targets

DPP-4 (Dipeptidyl Peptidase-IV)

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