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. Preclinical data indicate that 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. This dual action is unique and may offer improved glucose homeostasis over existing diabetes therapies, with potential for weight loss and improved islet health. MBX-2982 has completed four Phase 1 studies and one Phase 2 study. In the 4-week Phase 2 study in diabetics, MBX-2982 lowered mean weighted glucose and postprandial glucose during an extended mixed-meal tolerance test (MMTT). 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. In all studies to date, MBX-2982 demonstrated dose-dependent increases in drug exposure with a profile supporting once daily oral dosing that was safe and well tolerated with no serious adverse events, adverse event trends or dose-limiting toxicities. These results provide clinical validation for the potential therapeutic benefits of MBX-2982 as a type 2 diabetes treatment.