firuglipel

Firuglipel (DS-8500a) is an orally available, potent, and selective small molecule agonist of G-protein coupled receptor 119 (GPR119). Developed by Daiichi Sankyo for the treatment of type 2 diabetes mellitus, it targets GPR119 receptors highly expressed in pancreatic β-cells and intestinal L-cells. Activation of these receptors increases intracellular cAMP levels, stimulating glucose-dependent insulin secretion (GSIS) and the release of glucagon-like peptide-1 (GLP-1). Despite reaching Phase 2 clinical trials in Japan, where it was evaluated for its effects on pancreatic beta-cell function and insulin secretory capacity, its development has been discontinued.

Other names

firuglipel