GS-59728

GS-59728 (also referred to as GL59728) is a potent and selective small-molecule agonist of the G-protein coupled receptor 120 (GPR120), also known as free fatty acid receptor 4 (FFAR4). Developed by Gilead Sciences, the compound was primarily investigated for the treatment of metabolic disorders, including type 2 diabetes and obesity. GPR120 is highly expressed in adipose tissue and pro-inflammatory macrophages; its activation is associated with improved insulin sensitivity and anti-inflammatory effects. GS-59728 was designed to improve upon the potency and pharmacokinetic profiles of earlier GPR120 agonists. Clinical development reached Phase 1, but the compound is no longer listed in Gilead's active development pipeline and appears to have been discontinued.