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Garglicin (XZP-5695) is an orally bioavailable small molecule agonist of the G-protein coupled receptor 119 (GPR119), currently under development by Xuanzhu Biopharmaceutical (a subsidiary of Sihuan Pharmaceutical) for the treatment of type 2 diabetes mellitus. GPR119 is primarily expressed in pancreatic beta cells and intestinal enteroendocrine cells (L-cells and K-cells). Activation of this receptor by garglicin stimulates glucose-dependent insulin secretion and promotes the release of incretin hormones, such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). This dual mechanism of action aims to improve glycemic control and potentially preserve beta-cell function. Clinical development has progressed through Phase 1 studies in China, including safety, pharmacokinetic, and mass balance evaluations using radiolabeled [14C]-garglicin.
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