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他克莫司的药物基因组学与个体化用药

朱琳 华之卉 宋洪涛

中国临床药理学与治疗学2011,Vol.16Issue(6):710-715,6.
中国临床药理学与治疗学2011,Vol.16Issue(6):710-715,6.

他克莫司的药物基因组学与个体化用药

Pharmacogenomics and personalized medicine of tacrolimus

朱琳 1华之卉 2宋洪涛1

作者信息

  • 1. 南京军区福州总医院药学科,福州350025,福建
  • 2. 沈阳药科大学药学院,沈阳110016,辽宁
  • 折叠

摘要

Abstract

Tacrolimus (FK506) , a widely used immunosuppressant, exerts a key effect in patients with organ transplantation. The drug requires therapeutic monitoring due to its narrow therapeutic index and great inter-individual variability. FK506 is known to be a substrate of CYP3A and P-glycoprotein (P-gp) . FK506 is metabolized by CYP3A and transported by P-gp.The difference in expression level and the bioactivity of these proteins may explain individual variations of FK506 pharmacokinetics. The differences in bioactivities of CYP3A and P-gp are believed to be due to CYP3A and MDR1 geneticmutation. Therefore, genetic variations of CYP3A and MDR1 may play an important role in the inter-individual variability of FK506. In this article, we reviewed the effect of CYP3A and MDR1 gene polymorphisms on pharmacokinetics of FK506 in patients with organ trans plantation. This article presents an overview of the current research progress of pharmacog enomics of tacrolimus.

关键词

他克莫司/基因多态性/CYP3A4/CYP3A5/多药耐药基因

Key words

Tacrolimus/ Gene polymor phism/CYP3A4/CYP3A5/MDR1

分类

医药卫生

引用本文复制引用

朱琳,华之卉,宋洪涛..他克莫司的药物基因组学与个体化用药[J].中国临床药理学与治疗学,2011,16(6):710-715,6.

中国临床药理学与治疗学

OACSCDCSTPCD

1009-2501

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