Abstract: Farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily. It has extensive physiological functions in maintaining homeostasis of bile acids, lipids, and glucose. It also participates in the development of various tumors. Therefore, regulation of its transcriptional activity is accepted as an important strategy for treatment of many diseases, and various FXR agonists have been developed. In recent years, it has been found that inhibition of FXR transcriptional activity also shows beneficial effects on various diseases, therefore several FXR antagonists have been developed and their pharmacological activities have been tested in preclinical animal models. This article provides an update review on FXR antagonists and their pharmacological activities.

Key words: farnesoid X receptor, antagonist, pharmacological activity