治疗上皮样肉瘤新药:zeste基因增强子同源物2抑制剂tazemetostat

A new drug in treating epithelioid sarcoma:enhancer of zeste homolog 2 inhibitor tazemetostat

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肉瘤(ES)患者的治疗。Taz是目前首款且唯一获得FDA批准上市的EZH2抑制剂,也是首款且唯一针对性治疗ES的药物。最新研究表明,接受Taz治疗的患者客观缓解率为15%。常见不良反应包括疼痛、疲劳和恶心等。

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.