谷胱甘肽转移酶基因多态性对白消安体内代谢的影响  

Influence of glutathione S-transferase polymorphisms on busulfan pharmacokinetics

作　　者：黄菁菁[1] 陈冰[1] 杨婉花[1] 

机构地区：[1]上海交通大学医学院附属瑞金医院药剂科,上海200025

出　　处：《中国临床药理学杂志》2012年第11期869-871,共3页The Chinese Journal of Clinical Pharmacology

摘　　要：白消安是造血干细胞移植(HSCT)前大剂量预处理方案中的常用药物,患者间存在较大的药代动力学差异和较高的不良反应发生率。白消安主要通过谷胱甘肽转移酶(GST)催化,在肝脏与谷胱甘肽(GSH)结合代谢,GST基因多态性显著影响白消安的体内代谢过程。因此可根据患者的基因型,调整白消安用量,制定个体化用药方案。Busulfan is commonly used at high dosages as a component of conditioning regimens before hematopoietic stem cell transplantation（HSCT）.In patients receiving either intravenous or oral busulfan,there is a wide pharmacokinetic interindividual variability and high incidence of adverse event.Busulfan metabolism occurs in the liver via conjugation with glutathione（GSH） catalyzed by glutathione-S transferase（GST）.GSTs is a family of phase Ⅱ detoxification enzymes,comprised by different isozymes.GST polymorphisms affect busulfan metabolism remarkably.The genotype-based dose adjustment could make plasma concentration reach and maintain the therapeutic window.It will provide effective basis for setting individual dosage regimen and reduction of adverse drug reaction.

关 键 词：白消安 GST基因多态性 药代动力学 

分 类 号：R969.1[医药卫生—药理学] R979.19[医药卫生—药学]