JNJ-38431055

JNJ-38431055 (also known as APD597) is an orally available small molecule agonist of the G protein-coupled receptor 119 (GPR119), developed for the treatment of type 2 diabetes mellitus. Its mechanism of action involves stimulating GPR119, which increases postprandial levels of incretin hormones such as glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP), thereby enhancing glucose-dependent insulin secretion. Clinical studies demonstrated that while single-dose administration reduced glucose excursion during oral glucose tolerance tests and increased incretin hormone concentrations, multiple dosing did not significantly alter mean daily glucose levels or increase insulin secretion in patients with type 2 diabetes. The drug was well tolerated without significant hypoglycemia but showed limited efficacy in lowering blood glucose[1][5][6]. Development has been discontinued after phase I clinical trials[4][8].

Other names

isopropyl 4-((5-methoxy-6-((2-methyl-6-(methylsulfonyl)pyridin-3-yl)amino)pyrimidin-4-yl)oxy)piperidine-1-carboxylate