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氟马替尼的基础与临床研究进展

[Advances in basic and clinical research of flumatinib].

作者信息

Jiang L, Yang M Z

机构信息

Department of Hematology, the First Affiliated Hospital of Anhui Medical University, Anhui Public Health Clinical Center, Hefei 230032, China.

出版信息

Zhonghua Xue Ye Xue Za Zhi. 2024 Jun 14;45(6):621-624. doi: 10.3760/cma.j.cn121090-20231211-00304.

Abstract

Chronic myelogenous leukemia (CML) is a hematological malignancy originating from the pluripotent hematopoietic stem cells. Imatinib is the first generation of small molecule tyrosine kinase inhibitors (TKI) that revolutionized the treatment of CML. Flumatinib, as a novel oral TKI that independently developed in China, which can be used as a preferred treatment for CML. Basic researches suggested that the inhibitory effect of flumatinib on CML cell lines is stronger than imatinib. Flumatinib demonstrated that it has better efficacy than imatinib on CML in clinical trials and in real world studies. Flumatinib also showed a higher potency against CML with specific mutations, Ph(+) acute lymphoblastic leukemia and some solid tumors. The adverse events are manageable and tolerable.

摘要

慢性粒细胞白血病(CML)是一种起源于多能造血干细胞的血液系统恶性肿瘤。伊马替尼是第一代小分子酪氨酸激酶抑制剂(TKI),它彻底改变了CML的治疗方式。氟马替尼是我国自主研发的新型口服TKI,可作为CML的一线治疗药物。基础研究表明,氟马替尼对CML细胞系的抑制作用强于伊马替尼。临床试验和真实世界研究均显示,氟马替尼治疗CML的疗效优于伊马替尼。氟马替尼对特定突变的CML、Ph(+)急性淋巴细胞白血病和一些实体瘤也显示出更高的活性。其不良事件易于管理且可耐受。

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