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治疗上皮样肉瘤新药:zeste基因增强子同源物2抑制剂tazemetostat
引用本文:柴芳,汪龙,宋佳伟,邢孔浪. 治疗上皮样肉瘤新药:zeste基因增强子同源物2抑制剂tazemetostat[J]. 中国新药与临床杂志, 2021, 0(3): 183-186
作者姓名:柴芳  汪龙  宋佳伟  邢孔浪
作者单位:三亚市人民医院药学部;蚌埠市第三人民医院药学部;亳州市人民医院药学部
摘    要:tazemetostat(Taz)是一种zeste基因增强子同源物2(EZH2)抑制剂,能够有效抑制多梳蛋白复合体2(PRC2)发挥组蛋白赖氨酸甲基转移酶(HKMT)活性,通过全新的表观遗传调控机制而发挥抗肿瘤活性.2020年1月23日,美国食品和药物管理局(FDA)批准Taz用于不适合完全切除的转移性或局部晚期上皮样...

关 键 词:tazemetostat  上皮样肉瘤  临床研究  作用机制  药动学

A new drug in treating epithelioid sarcoma:enhancer of zeste homolog 2 inhibitor tazemetostat
CHAI Fang,WANG Long,SONG Jia-wei,XING Kong-lang. A new drug in treating epithelioid sarcoma:enhancer of zeste homolog 2 inhibitor tazemetostat[J]. Chinese Journal of New Drugs and Clinical Remedies, 2021, 0(3): 183-186
Authors:CHAI Fang  WANG Long  SONG Jia-wei  XING Kong-lang
Affiliation:(Department of Pharmacy,People’s Hospital of Sanya,Sanya HAINAN 572000,China;Department of Pharmacy,the Third People’s Hospital of Bengbu,Bengbu ANHUI 233099,China;Department of Pharmacy,People’s Hospital of Bozhou,Bozhou ANHUI 236800,China)
Abstract:Tazemetostat(Taz)is an enhancer of zeste homolog 2(EZH2)inhibitor.It can effectively inhibit the histone lysine methyltransferase(HKMT)activity of polycomb repressive complexes 2(PRC2)and plays an anti-tumor role through a novel epigenetic regulatory mechanisms.It was approved for the treatment of patients with metastatic or locally advanced epithelioid sarcoma(ES)who were not eligible for complete resection by the U.S.Food and Drug Administration(FDA)on January 23,2020.Taz is now the first and only FDA-approved EZH2 inhibitor,and the first and only FDAapproved treatment specifically indicated for ES patients.The latest studies have shown that the overall response rate was 15%in patients who received Taz treatment.The common adverse reactions include pain,fatigue,nausea,and so on.
Keywords:tazemetostat  epithelioid sarcoma  clinical study  action mechanism  pharmacokinetics
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