Ciclosporin A (CsA), an immunosuppressive macrolide antibiotics, is widely applied to prevent rejections after organ transplants. CsA is mainly transported by P-glycoprotein (P-gp) and metabolized by cytochrome P450 (CYP450) 3A.Genetic polymorphisms of CYP3A and MDR1 probably influence the expressions and bioactivity of CYP3A and P-gp,and may affect the pharmacokinetics of CsA.This issue summarizes the correlation between genetic polymorphisms of CYP3A and MDR1 and the pharmacokinetics of CsA to guide the rational and individualized medication.%环孢素A（CsA）属环状多肽化合物，作为基础免疫抑制剂广泛用于实体器官移植后的抗排斥反应，其主要经P-糖蛋白（P-gp）转运，细胞色素P450（CYP）3A酶代谢，CYP3A及多药耐药基因1（MDR1）的多态性可能影响CYP3A酶和P-gp的表达水平和生物活性，进而可能对CsA的药代动力学过程产生影响。本文就CYP3A和MDR1基因多态性对CsA药代动力学的影响进行综述，以期指导临床制定合理的个体化用药方案。
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