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HO-03-03 is an investigational, orally bioavailable small molecule agonist of the G protein-coupled receptor 119 (GPR119), currently under development by Haisco Pharmaceutical Group. It is primarily being evaluated for the treatment of type 2 diabetes mellitus. GPR119 is a receptor predominantly expressed in pancreatic beta cells and enteroendocrine cells (L-cells) of the gastrointestinal tract. Activation of GPR119 by HO-03-03 stimulates the glucose-dependent secretion of insulin and promotes the release of incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). This dual mechanism of action helps to regulate blood glucose levels effectively while minimizing the risk of hypoglycemia, as the insulinotropic effect is contingent upon elevated glucose concentrations.
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