DS-7309 + metformin

DS-7309 + metformin is an investigational combination therapy developed by Daiichi Sankyo for the treatment of type 2 diabetes mellitus (T2DM). DS-7309 is a small molecule agonist of the G protein-coupled receptor 119 (GPR119), which is primarily expressed in pancreatic beta cells and intestinal enteroendocrine cells. Activation of GPR119 promotes glucose-dependent insulin secretion and the release of incretins such as GLP-1 and GIP. Metformin is a biguanide and standard-of-care treatment for T2DM that reduces blood glucose levels by activating AMP-activated protein kinase (AMPK) and inhibiting mitochondrial complex I, thereby decreasing hepatic gluconeogenesis and improving peripheral insulin sensitivity. The combination was evaluated in a Phase 1 multiple ascending dose study (NCT01956305) to assess the safety, tolerability, and pharmacokinetics of DS-7309 when co-administered with escalating doses of metformin.