Drug intelligence / Profile preview

HG043

Development stage
Preclinical
Lead developer
Hanmi Pharmaceutical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

HG043 is a novel, potent thienopyrimidine-based small molecule agonist of GPR119, a G protein-coupled receptor implicated in glucose homeostasis and energy balance. By activating GPR119, HG043 enhances glucose-stimulated insulin secretion and stimulates incretin (GLP-1) release from pancreatic β-cells. Preclinical studies demonstrate that HG043 has superior efficacy compared to MBX-2982 (another GPR119 agonist) and sibutramine (an appetite suppressant), resulting in significant improvements in diabetic parameters, body weight reduction, food intake suppression, and fat mass loss in both healthy and disease models. Additionally, HG043 shows synergistic glucose-lowering effects when combined with metformin or sitagliptin. These findings suggest its potential as a promising therapeutic agent for patients with type 2 diabetes who are also obese[1][2][4].

02

Targets

GPR119 (Glucose-dependent insulinotropic receptor)

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