Abstract: OBJECTIVE To summarize and analyze the metabolic drug interaction, the role of pregnane X receptor(PXR) in CYP3A4 modulation and its molecule mechanism. METHODS Related literatures in recent years were reviewed. RESULTS PXR was a key transcription factor that regulate CYP3A4 expression. CYP3A4 transcription could be activated by compound via PXR-mediated signaling pathway therefore results in changes of co-administered drug metabolism. CONCLUSION For clinical drug, caution should be taken when PXR agonist is used in combination with prescribed drugs metabolized by CYP3A4.