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[Advances in basic and clinical research of flumatinib].氟马替尼的基础与临床研究进展
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Distinct interaction of nilotinib and imatinib with P-Glycoprotein in intracellular accumulation and cytotoxicity in CML Cell Line K562 cells.尼洛替尼和伊马替尼在慢性粒细胞白血病K562细胞系中的细胞内蓄积及细胞毒性方面与P-糖蛋白的独特相互作用。
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BCR-ABL1-independent PI3Kinase activation causing imatinib-resistance.BCR-ABL1 非依赖性 PI3K 激活导致伊马替尼耐药。
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本文引用的文献

1
Case report: Olverembatinib monotherapy: the chemotherapy-free regimen for an elderly patient with relapsed Ph-positive acute lymphoblastic leukemia.病例报告:奥雷巴替尼单药治疗:一位复发的Ph阳性急性淋巴细胞白血病老年患者的无化疗方案
Front Pharmacol. 2023 Nov 16;14:1320641. doi: 10.3389/fphar.2023.1320641. eCollection 2023.
2
[Efficacy and Safety of Flumatinib in Treatment of Patients with Chronic Myeloid Leukemia].氟马替尼治疗慢性髓性白血病患者的疗效与安全性
Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2023 Aug;31(4):1014-1018. doi: 10.19746/j.cnki.issn.1009-2137.2023.04.013.
3
Screening and Analysis of Possible Drugs Binding to PDGFRα: A Molecular Modeling Study.PDGFRα 可能结合药物的筛选与分析:分子建模研究。
Int J Mol Sci. 2023 Jun 1;24(11):9623. doi: 10.3390/ijms24119623.
4
Studies on the inhibitory effect of isavuconazole on flumatinib metabolism and .关于艾沙康唑对氟马替尼代谢的抑制作用的研究 以及 。 (注:原文结尾不完整,翻译只能到这里。)
Front Pharmacol. 2023 May 4;14:1168852. doi: 10.3389/fphar.2023.1168852. eCollection 2023.
5
Basic and clinical study of efficacy and adverse effects of flumatinib in Ph ALL.氟马替尼治疗Ph阳性急性淋巴细胞白血病疗效及不良反应的基础与临床研究
Front Pharmacol. 2023 May 5;14:1178393. doi: 10.3389/fphar.2023.1178393. eCollection 2023.
6
Clinical Efficacy and Safety of Flumatinib in Newly Diagnosed Chronic Myelogenous Leukemia.氟马替尼治疗新诊断慢性髓性白血病的临床疗效和安全性。
Pharmazie. 2023 Apr 15;78(1):13-16. doi: 10.1691/ph.2023.2536.
7
Efficacy of Flumatinib in CML Patients with F359V/C Mutation.氟马替尼在F359V/C突变慢性髓性白血病患者中的疗效
Indian J Hematol Blood Transfus. 2023 Apr;39(2):344-346. doi: 10.1007/s12288-022-01585-3. Epub 2022 Oct 17.
8
[Clinical observation of flumatinib combined with induction chemotherapy and sequential allogeneic hematopoietic stem cell transplantation in the treatment of 6 patients with newly diagnosed Ph(+) acute lymphocytic leukemia].氟马替尼联合诱导化疗及序贯异基因造血干细胞移植治疗6例初诊Ph(+)急性淋巴细胞白血病的临床观察
Zhonghua Xue Ye Xue Za Zhi. 2023 Feb 14;44(2):169-172. doi: 10.3760/cma.j.issn.0253-2727.2023.02.017.
9
Pharmacokinetics of single- and multiple-dose flumatinib in patients with chronic phase chronic myeloid leukemia.慢性期慢性髓性白血病患者单剂量和多剂量氟马替尼的药代动力学
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Tyrosine kinase inhibitors combined with venetoclax and azacytidine as an effective therapy for de novo lymphoid blast phase-chronic myeloid leukemia.酪氨酸激酶抑制剂联合维奈克拉和阿扎胞苷作为初发淋巴母细胞期慢性髓性白血病的有效治疗方法。
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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.

DOI:10.3760/cma.j.cn121090-20231211-00304
PMID:39134501
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11310800/
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。