他莫昔芬代谢产物endoxifen的研究进展  

Research Progress in Tamoxifen Metabolite Endoxifen

作　　者：豆妮娜 袁欣 王帅兵 马海艳 陈魁霞 潘丹 庄爱爱 Dou Nina;Yuan Xin;Wang Shuaibing;Ma Haiyan;Chen Kuixia;Pan Dan;Zhuang Aiai(Department of Pharmacy,Hebei PetroChi-na Central Hospital,Hebei Langfang 065000,China)

机构地区：[1]河北中石油中心医院药学部,河北廊坊065000

出　　处：《中国药师》2022年第5期867-872,共6页China Pharmacist

摘　　要：他莫昔芬是一种内分泌治疗药物,被批准用于预防和治疗雌激素受体阳性的乳腺癌患者。他莫昔芬的重要次级代谢产物endoxifen,因其比他莫昔芬更强的雌激素受体亲和力,以及更强的抑制雌激素依赖性细胞增殖作用,引起研究人员的重视。Endoxifen的特性,如口服利用度高、不良反应发生率低以及对雌激素受体阳性且内分泌治疗耐药的乳腺癌患者具有抗肿瘤活性,使其成为治疗乳腺癌患者的潜在药物。本文就他莫昔芬转化为endoxifen的代谢过程、药理作用与临床研究进行概述,讨论endoxifen的应用前景。Tamoxifen is an endocrine therapy drug approved for the prevention and treatment of estrogen receptor-positive breast cancer patients.Endoxifen,an important secondary metabolite of tamoxifen,has attracted much attention of researchers because of its stronger affinity for estrogen receptors than tamoxifen and its stronger inhibition of estrogen-dependent cell proliferation.The characteristics of endoxifen,such as high oral availability,low incidence of adverse reactions and antitumor activity in breast cancer patients with estrogen receptor-positive and endocrine therapy resistance make it a potential drug for the treatment of breast cancer patients.This article summarized the metabolic process of tamoxifen into endoxifen,the pharmacological effects and clinical research of endoxifen,and discussed the application prospects of endoxifen.

关 键 词：他莫昔芬 ENDOXIFEN 抗肿瘤活性 药理作用 

分 类 号：R979.1[医药卫生—药品]