Abstract: Pregnane X receptor (PXR), a member of the nuclear receptor subfamily of ligand-dependent regulatory target genes, regulates the expression of multiple drug metabolizing enzymes and transporters upon activation, thus affecting the efficacy and drug resistance of clinical medicines. PXR is involved in the pathogenesis and development liver diseases by regulating the metabolism of lipids and carbohydrates in the liver, emerging as a potential drug target for drug screening and treatment of liver diseases. The deep understanding of PXR and its regulatory mechanisms has great significance for predicting drug-drug interactions, avoiding or mitigating adverse drug reactions, designing and developing novel drugs targeting PXR. This article summarized the regulatory roles of PXR in liver diseases and the research progress in drug intervention for liver disease progression through PXR.