Abstract: Objective To outline the functions of and research progress in the nuclear receptor pregnane X receptor (PXR) and constitutive androstane receptor (CAR)-metabolic enzyme/transporter detoxification system. Methods The detoxification system of PXR/CAR-metabolic enzyme/transporter and its applications were reviewed in terms of the liver metabolic enzyme, liver and kidney transporter and PXR CAR-mediated drug detoxification. Results and Conclusion Drugs, as exogenous substances in the human body, may have toxicity and side effects, which is likely to cause injury when administrated improperly or with apparent toxicity. Drug metabolic enzymes and transporters are two pivotal factors in determining the process and exposure of drugs in vivo, making much difference to drug toxicity and detoxification. With the continuous deeping of research, PXR and CAR have been found to play a central regulatory role in metabolic enzymes and transporters related to drug detoxification. As a result, PXR and CAR can combine with their related drug metabolizing enzymes and transporters to constitute the most important defense detoxification system in vivo, the so-called PXR/CAR- metabolic enzymes/transporters detoxification system.

Key words: PXR, CAR, metabolic enzymes, transporter, drug detoxification system