GSK3527497

GSK3527497, formerly known as ST810, is a potent and selective small-molecule agonist of the G protein-coupled receptor 35 (GPR35). Originally discovered by Sosei Heptares using its proprietary StaR® technology and structure-based drug design platform, the compound was subsequently licensed to GSK for global development. GPR35 is an orphan receptor highly expressed in the gastrointestinal tract, particularly in colonic epithelial cells and certain immune cells, where it is believed to play a critical role in maintaining intestinal homeostasis and promoting mucosal barrier repair. By activating GPR35, GSK3527497 is intended to enhance epithelial healing and modulate inflammatory responses in patients with inflammatory bowel diseases, such as ulcerative colitis. The drug has been evaluated in Phase 1 clinical trials to assess its safety, tolerability, and pharmacokinetics in both healthy volunteers and patients with ulcerative colitis.