环磷酰胺与异环磷酰胺在体内的代谢研究  

Study on the metabolism of cyclophosphamide and ifosfamide in vivo

作　　者：杨凤艳 YANG Feng-yan(Tianjin UniversitySchoool of Pharmaceutical Science and Technology,Tianjin 300072,China)

机构地区：[1]天津大学药物科学与技术学院

出　　处：《化学工程师》2019年第12期51-53,共3页Chemical Engineer

基　　金：天津市自然科学基金(合同编号：17JCZDJC32000)

摘　　要：环磷酰胺与异环磷酰胺是临床上常用氮芥类抗肿瘤药物,两药代谢前均无烷化剂活性,须依赖肝细胞微粒体系中的细胞色素P450酶系代谢转变为有活化作用的磷酰胺氮芥而起用。肝脏不同的P450酶系在环磷酰胺和异环磷酰胺的生物转化中所起的作用不同,CYP2B6和3A4分别催化环磷酰胺和异环磷酰胺的羟化。本文对两药在体内的代谢过程进行了比较分析,阐明两药在代谢上的异同,为临床合理用药及有效预防毒副作用提供用药依据。Cyclophosphamide and ifosfamide are commonly used as anti-tumor drugs for nitrogen mustard in clinical practice.Both drugs have no alkylating agent activity before metabolism,and they depend on the metabolism of cytochrome P450 enzyme in hepatocyte microparticle system to activate.The action of the phosphoramide mustard is used.Different P450 enzymes in the liver play different roles in the biotransformation of cyclophosphamide and ifosfamide,and CYP2B6 and 3A4 catalyze the hydroxylation of cyclophosphamide and ifosfamide,respectively.In this paper,the metabolic process of the two drugs in the body was compared and analyzed,and the similarities and differences between the two drugs were elucidated,which provided the basis for clinical rational drug use and effective prevention of side effects.

关 键 词：环磷酰胺 异环磷酰胺 抗肿瘤药物 CYP2B1 基因治疗 

分 类 号：R99[医药卫生—毒理学]