他克莫司是一种新型强效免疫抑制性大环内酯类抗生素,主要通过细胞色素 P450(如 CYP3A4和 CYP3A5等)代谢,由 P-糖蛋白进行转运。越来越多的研究发现 CYP3A4,CYP3A5酶及 P-糖蛋白的某些基因多态性可以影响他克莫司的药代和药效。现就 CYP3A4, CYP3A5及 P-糖蛋白的基因变异与他克莫司个体间差异相关性研究进行综述。% Tacrolimus was a new potent immunosuppressive macrolide antibiotics. It was metabolized by cytochrome P450 enzymes (such as CYP3A4, CYP3A5) and transported by P-glycoprotein. Patients with certain genetic variants in CYP3A4, CYP3A5 and P-glycoprotein have been found to influence pharmacokinetics and pharmacodynamics of tacrolimus. This article reviewed studies concerning the correlation between genetic variants in CYP3A4, CYP3A5 and P-glycoprotein with individual differences of tacrolimus.
展开▼