CAJ | 학술논문

他克莫司（FK506）是一种新型免疫抑制剂，广泛应用于器官移植后排斥反应的预防，主要由细胞色素P450（CYP450）3A酶代谢，P-糖蛋白（P-gp）转运，CYP3A和多药耐药基因1（MDR1）的多态性可能会影响CYP3A酶及P-gp的表达水平和生物活性，进而影响FK506的药代动力学过程，最终可能影响其血药浓度。本文就CYP3A和MDR1基因多态性与FK506血药浓度的相关性进行综述，以期指导临床个体化合理用药。
타극막사（FK506）시일충신형면역억제제，엄범응용우기관이식후배척반응적예방，주요유세포색소P450（CYP450）3A매대사，P-당단백（P-gp）전운，CYP3A화다약내약기인1（MDR1）적다태성가능회영향CYP3A매급P-gp적표체수평화생물활성，진이영향FK506적약대동역학과정，최종가능영향기혈약농도。본문취CYP3A화MDR1기인다태성여FK506혈약농도적상관성진행종술，이기지도림상개체화합리용약。
As a novel immunosuppressant, tacrolimus (FK506) is widely applied to prevent rejections after organ transplants. FK506 is mainly metabolized by cytochrome P450 (CYP450) 3A and transported by P-glycoprotein (P-gp). Genetic polymorphisms of CYP3A and MDR1 probably influence the expressions and bioactivity of CYP3A and P-gp, and then affect FK506 pharmacokinetics and finally may affect the blood drug concentrations of FK506. This article summarized the correlation between genetic polymorphisms of CYP3A and MDR1 and the blood drug concentrations of FK506 to guide the rational and individualized medication in clinic.