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Efficacy of Flumatinib in CML Patients with F359V/C Mutation
Indian Journal of Hematology and Blood Transfusion ( IF 0.7 ) Pub Date : 2022-10-17 , DOI: 10.1007/s12288-022-01585-3
Hua Gao 1 , Libo Li 1 , Jiao Mu 1 , Jing Tan 1 , Rong Chen 1
Affiliation  

The BCR-ABL mutation is the main cause of tyrosine kinase inhibitors(TKI) resistance. The second-generation TKI can overcome most of the mutations. However, both dasatinib and nilotinib have a unique set of mutants with reduced sensitivity. All TKIs are associated with adverse events, which lead to treatment discontinuation and affect the quality of life of patients. Flumatinib showed higher activity against BCR-ABL mutants in vitro. Drug-related adverse events of flumatinib were mainly grade 1 or grade 2 events. There is no study that reported the efficacy of flumatinib against F359V/C mutation.We report two cases of chronic myelocytic leukemia(CML) patients with F359V/C mutation resistance to Imatinib therapy. One patient with F359V mutation was shifted to Dasatinib. Repeated massive pleural effusion and anemia occurred after Dasatinib treatment, forcing drug dosage reduction or withdrawal, affecting drug efficacy and quality of life of patient. Two patients were shifted to Flumatinib. MR4 was achieved and F359V/C mutation was not detected after treatment with Flumatinib. There was no significant side effect. The patients had a high quality of life. Flumatinib is effective against F359V/C mutation, has less drugrelated adverse reactions. Flumatinib may be a better choice for patients with F359V/C mutation.



中文翻译:


氟马替尼治疗 F359V/C 突变 CML 患者的疗效



BCR-ABL突变是酪氨酸激酶抑制剂(TKI)耐药的主要原因。第二代TKI可以克服大部分突变。然而,达沙替尼和尼洛替尼都有一组独特的突变体,其敏感性降低。所有 TKI 均与不良事件相关,这些不良事件会导致治疗中断并影响患者的生活质量。 Flumatinib 在体外对 BCR-ABL 突变体表现出更高的活性。氟马替尼药物相关不良事件主要为1级或2级事件。目前尚无研究报道氟马替尼对 F359V/C 突变的疗效。我们报告了两例 F359V/C 突变对伊马替尼治疗耐药的慢性粒细胞白血病 (CML) 患者。一名 F359V 突变患者转至达沙替尼治疗。达沙替尼治疗后反复出现大量胸腔积液和贫血,迫使药物剂量减少或停药,影响药物疗效和患者生活质量。两名患者被转移至氟马替尼。氟马替尼治疗后达到MR4,未检测到F359V/C突变。没有明显的副作用。患者的生活质量很高。氟马替尼对F359V/C突变有效,药物相关不良反应少。对于 F359V/C 突变患者来说,氟马替尼可能是更好的选择。

更新日期:2022-10-18
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