Farnesoid X receptor agonists for primary biliary cirrhosis

This review will provide an overview of the role of nuclear receptors in bile acid homeostasis with a focus on the farnesoid X receptor (FXR) and its potential therapeutic use in cholestatic liver diseases.

Nuclear receptors have emerged as important mediators of a variety of metabolic and transport functions involving the liver. The role of FXR, in particular, has come to light because of its important role in bile acid homeostasis. The use of potent FXR ligands has recently been shown to offer potentially important therapeutic benefits in patients with primary biliary cirrhosis, an important cholestatic liver disease of adults. This recent finding has now opened the door for future therapeutic trials for use of FXR agonists such as obeticholic acid for the treatment of chronic cholestatic liver diseases.

Further understanding of the role of farnesoid X receptor agonists and the potential role of ligands in animal models of other forms of cholestasis will be important to set the stage for future applications to human disease.