有机阴离子转运多肽1B1的遗传药理学进展

人体存在多种类型的药物转运体,对于药物的吸收、分布和排泄起重要作用。参与药物跨膜转运的转运体功能受影响,将可能导致诸多临床药物的疗效、毒副作用甚至药物相互作用的发生。在各种影响因素中,遗传多态性所起的作用最为重要,可导致基因表达和蛋白功能发生改变。目前,阐明转运体基因的多态性以及基因型与表型之间的相互关系已成为应用遗传信息指导临床个体化用药的必要步骤。本文就肝脏有机阴离子转运多肽1B1(OATP1B1OATP-C],编码基因SLCO1B1)基因多态性对药代动力学和药效动力学的影响及其临床意义等方面的进展作一综述。

Progress and research in pharmacogenetics of OATP1B1

Many types of drug transporters are expressed in different organs.The transporters play important roles in drug absorption, distribution and excretion, and lead to consequences for interindividual differences in disposition kinetics, interaction profiles of clinical drugs, susceptibility to side effects and treatment efficacy.The genetic polymorphisms have been shown to alter both the expression and function of their gene products.The identification of allelic variations and their functional confirmations is a necessary step towards the use of genetic information for personalized medicine.This review focuses on the role of organic anion transporting polypeptide 1B1 (OATP1B1) gene polymorphisms in pharmacokinetic and pharmacodynamic consequences in pharmacotherapy.