孕烷X受体(PXR)对药物代谢途径的调控

Role of Pregnane X Receptor(PXR) in Drug Metabolism Modulation

目的从孕烷X受体(PXR)对药物代谢途径的调控入手,在代谢性药物相互作用、PXR在CYP3A4调控中的作用及其调控机制等方面作分析和阐述。方法结合近年来国内外相关文献进行评述。结果 PXR是CYP3A4的主要转录调控因子,药物通过PXR介导的信号通路调节CYP3A4的表达是影响药物体内代谢变化的重要途径。结论就临床药物而言,由PXR介导的CYP3A4酶蛋白表达的改变可造成合用药物药效的减弱甚至丧失,因此必须引起广大临床药师的足够重视。

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.