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中华乳腺病杂志(电子版) ›› 2011, Vol. 05 ›› Issue (05) : 601 -607. doi: 10.3877/cma.j.issn.1674-0807.2011.05.012

综述

药物代谢酶细胞色素P450 2D6 在他莫昔芬个体化治疗中的研究进展
谢新华1, 韦尉东1, 孔亚楠1, 郭姣丽1, 吕宁1, 唐军1, 肖祥胜1, 谢小明1,()   
  1. 1.510060 广州,中山大学肿瘤防治中心乳腺科,华南肿瘤学国家重点实验室
  • 收稿日期:2011-09-06 出版日期:2011-10-01
  • 通信作者: 谢小明
  • 基金资助:
    国家自然科学基金重点项目(31030061);教育部高等学校博士学科点专项科研基金资助项目(20090171110078);广东省自然科学基金资助项目(9151008901000124)

Advances in study of genotyping of CYP2D6 and individualized treatment with tamoxifen

Xin-hua XIE, Wei-dong WEI, Ya-nan KONG, Jiaoli Guo, Ning Lv, Jun Tamg, Xiangsheng Xiao, Xiaoming Xie()   

  • Received:2011-09-06 Published:2011-10-01
  • Corresponding author: Xiaoming Xie
引用本文:

谢新华, 韦尉东, 孔亚楠, 郭姣丽, 吕宁, 唐军, 肖祥胜, 谢小明. 药物代谢酶细胞色素P450 2D6 在他莫昔芬个体化治疗中的研究进展[J/OL]. 中华乳腺病杂志(电子版), 2011, 05(05): 601-607.

Xin-hua XIE, Wei-dong WEI, Ya-nan KONG, Jiaoli Guo, Ning Lv, Jun Tamg, Xiangsheng Xiao, Xiaoming Xie. Advances in study of genotyping of CYP2D6 and individualized treatment with tamoxifen[J/OL]. Chinese Journal of Breast Disease(Electronic Edition), 2011, 05(05): 601-607.

图1 他莫昔芬的代谢简图 他莫昔芬(TAM)主要经CYP3A4 或CYP3A5 生成N-去甲基-TAM(NDM-TAM),后者再经CYP2D6 代谢成endoxifen;TAM也可通过CYP2D6 等生成少量4-羟基-TAM(4-OH-TAM),后者再进一步经CYP3A4 或CYP3A5 转化为endoxifen。CYP2D6 无效等位基因或者中强效酶抑制剂可阻断endoxifen 的代谢合成[5]
表1 CYP2D6 基因型与TAM 疗效相关性的临床研究结果
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