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Drugs. 2022 Nov;82(16):1621-1627. doi: 10.1007/s40265-022-01800-5.
Valemetostat tosilate (valemetostat; EZHARMIA), a selective dual inhibitor of histone-lysine N-methyltransferases enhancer of zeste homolog 1 and 2 (EZH1/2), is being developed by Daiichi Sankyo Company, Ltd for the treatment of various haematological malignancies and solid tumours, including types of non-Hodgkin lymphomas (NHL). Valemetostat was approved in Japan in September 2022 for the treatment of patients with relapsed or refractory adult T-cell leukaemia/lymphoma (R/R ATL), a subtype of NHL. This article summarizes the milestones in the development of valemetostat leading to this first approval for R/R ATL.
甲苯磺酸瓦利美特司他(瓦利美特司他;EZHARMIA)是组蛋白赖氨酸 N-甲基转移酶增强子的锌指蛋白 1 和 2(EZH1/2)的选择性双重抑制剂,由第一三共株式会社开发,用于治疗各种血液恶性肿瘤和实体瘤,包括非霍奇金淋巴瘤(NHL)。瓦利美特司他于 2022 年 9 月在日本获批用于治疗复发或难治性成人 T 细胞白血病/淋巴瘤(R/R ATL),这是非霍奇金淋巴瘤的一种亚型。本文总结了瓦利美特司他的开发里程碑,最终该药在 R/R ATL 中获得首次批准。