GSK1292263 is primarily investigated for its potential in treating type 2 diabetes and obesity due to its action as a selective inhibitor of the apical sodium-dependent bile acid transporter (ASBT). By inhibiting ASBT, it reduces bile acid reabsorption in the ileum, leading to increased bile acid excretion. This triggers the liver to convert more cholesterol into bile acids, which can lower circulating cholesterol levels and improve glucose metabolism. The compound has shown promise in preclinical studies for enhancing insulin sensitivity and promoting weight loss, making it a candidate for metabolic disorder therapies. Research also suggests it may influence the gut-liver axis and modulate lipid homeostasis, supporting its development for cardiometabolic conditions.