Gao Hua, Li Libo, Mu Jiao, Tan Jing, Chen Rong
Department of Hematology, The Third People's Hospital of Chengdu, The Affiliated Hospital of Southwest Jiaotong University, 82 Qinglong Road, Chengdu, Sichuan Province P.R. China.
Indian J Hematol Blood Transfus. 2023 Apr;39(2):344-346. doi: 10.1007/s12288-022-01585-3. Epub 2022 Oct 17.
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.
The online version contains supplementary material available at 10.1007/s12288-022-01585-3.
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可克服大多数突变。然而，达沙替尼和尼洛替尼都有一组独特的敏感性降低的突变体。所有TKI都与不良事件相关，这会导致治疗中断并影响患者的生活质量。氟马替尼在体外对BCR-ABL突变体显示出更高的活性。氟马替尼的药物相关不良事件主要为1级或2级事件。尚无研究报道氟马替尼对F359V/C突变的疗效。我们报告了2例对伊马替尼治疗耐药的F359V/C突变慢性粒细胞白血病（CML）患者。1例F359V突变患者改用达沙替尼。达沙替尼治疗后反复出现大量胸腔积液和贫血，迫使减少药物剂量或停药，影响了药物疗效和患者生活质量。2例患者改用氟马替尼。使用氟马替尼治疗后达到了MR4且未检测到F359V/C突变。无明显副作用。患者生活质量高。氟马替尼对F359V/C突变有效，药物相关不良反应较少。对于F359V/C突变患者，氟马替尼可能是更好的选择。
在线版本包含可在10.1007/s12288-022-01585-3获取的补充材料。
