MBX-2982

MBX-2982 is a potent selective orally-active GPR119 agonist that functions through a unique dual mechanism of action. First, it acts directly on the beta cell to increase insulin secretion. In addition, MBX-2982 stimulates release of the incretin GLP-1 from the gut. Treatment with MBX-2982 increased insulin, active GLP-1, and total GLP-1 during an extended MMTT. Treatment with MBX-2982 also tended to increase fasting insulin and c-peptide, and decrease fasting triglycerides. MBX-2982 is a potential first-in-class treatment for type 2 diabetes that targets G protein-coupled receptor 119 (GPR119), a receptor that interacts with bioactive lipids known to stimulate glucose-dependent insulin secretion.