Abstract: Cholestatic liver injury is usually accompanied by disordered homeostasis of bile acid, and the accumulation of bile acid is the direct cause of liver injury. Bile acid transporters and nuclear receptors maintain bile acid homeostasis by regulating the level of bile acid. This article systematically introduced the latest progress in the therapeutic drugs for cholestatic liver diseases from the perspectives of bile acid transporters and nuclear receptor, so as to provide reference for the development of related therapeutic drugs.