Abstract: Farnesoid X receptor(FXR), a member of the nuclear receptor superfamily, plays an important role on the regulating bile acid, lipid and glucose homeostasis. FXR antagonist can stimulate the conversion of total cholesterol into bile acid by improving the activity of CYP7A1. It can also reduce the content of triglyceride, low-density lipoprotein and increase that of high-density lipoprotein by regulating the relevant target genes. Considering the above facts, FXR antagonist is expected to become a potential drug to treat hyperlipidemia. In recent years, great progress has been made in the research on FXR antagonists with their various structural types having been obtained. This article introduces natural and synthetic FXR antagonists reported in recent years.