APD668

APD668 is a synthetic, orally active small molecule that acts as a potent agonist of the G protein-coupled receptor 119 (GPR119), also referred to as the glucose-dependent insulinotropic receptor (GDIR)[1][2][7]. It was developed to stimulate insulin release from pancreatic beta cells in response to elevated blood glucose levels, thereby reducing the risk of hypoglycemia compared to traditional agents like sulfonylureas[1][5]. In preclinical and early clinical studies, APD668 demonstrated efficacy in lowering blood glucose and glycated hemoglobin (HbA1c) levels without causing desensitization or hypoglycemia[3][6]. Additionally, it has shown effects on incretin secretion and inhibition of intestinal triglyceride absorption, suggesting potential benefits for dyslipidemia and non-alcoholic steatohepatitis[4][7]. Despite promising results in animal models and initial human trials for type 2 diabetes mellitus, clinical development was terminated in favor of more potent follow-up compounds[5][7].

Other names

isopropyl 4-((1-(2-fluoro-4-(methylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)oxy)piperidine-1-carboxylate