linafexor

Linafexor (CS0159) is a potent, selective, small-molecule agonist of the farnesoid X receptor (FXR), developed by Cascade Pharmaceuticals (Cascade Technologies). FXR is a nuclear receptor that serves as a master regulator of bile acid synthesis, transport, and metabolism, while also influencing lipid and glucose homeostasis. By activating FXR, linafexor reduces the production of toxic bile acids and enhances their clearance, making it a promising therapeutic candidate for cholestatic liver diseases and metabolic disorders. It is currently in Phase 3 development for primary biliary cholangitis (PBC) and Phase 2 for metabolic dysfunction-associated steatohepatitis (MASH) and primary sclerosing cholangitis (PSC). Additionally, it is being explored in combination with GLP-1 receptor agonists for the treatment of obesity and type 2 diabetes.

Brand names

利耐舒

Other names

Linafexor