LY2922083

LY2922083 is an orally administered small molecule agonist of G protein-coupled receptor 40 (GPR40), also known as free fatty acid receptor 1 (FFAR1). It was developed by Eli Lilly for the treatment of type 2 diabetes mellitus. GPR40 is highly expressed in pancreatic β-cells and amplifies insulin secretion in response to elevated glucose levels, making it a promising target for glucose-lowering therapies. LY2922083 demonstrated potent, dose-dependent reductions in glucose levels and increased insulin and GLP-1 secretion during preclinical studies. In early clinical trials, it showed rapid absorption after oral administration with dose-proportional pharmacokinetics and no dose-limiting adverse events reported. The drug reached Phase 1 clinical development but has not advanced further or received regulatory approval[1][4][5][7].