Preclinical and clinical experience with dasatinib in Philadelphia chromosome-negative leukemias and myeloid disorders.

Preclinical and clinical experience with dasatinib in Philadelphia chromosome-negative leukemias and myeloid disorders.
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达沙替尼在费城染色体阴性白血病和髓样疾病的临床前和临床经验。

DOI:
10.1016/j.leukres.2008.10.001
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发表时间:
2009-05
期刊:
影响因子:
2.7
通讯作者:
Verstovsek S
Verstovsek S
中科院分区:
医学3区
文献类型:
--
作者:
Verstovsek S

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费城染色体阴性(Ph−)白血病和相关髓系疾病分子特征的最新进展为研究新的靶向治疗提供了明确的依据。达沙替尼是一种酪氨酸激酶抑制剂,具有抗BCR-ABL、血小板衍生生长因子受体(PDGFRs)、c- KIT、成纤维细胞生长因子受体(FGFRs)、SRC家族激酶(SFKs)和EPHA受体的活性,所有这些受体都与Ph -白血病和髓系疾病的发病机制有关。这篇综述介绍了关于达沙替尼在这些疾病中的临床前和临床活性的新数据,这表明有必要进行更大规模的临床研究。
Recent advances in the molecular characterization of Philadelphia chromosome-negative (Ph−) leukemias and related myeloid disorders have provided a clear rationale for investigating novel targeted therapies. Dasatinib is a tyrosine kinase inhibitor with activity against BCR-ABL, platelet-derived growth factor receptors (PDGFRs), c- KIT, fibroblast growth factor receptors (FGFRs), SRC family kinases (SFKs), and EPHA receptors, all of which have been implicated in the pathogenesis of Ph− leukemias and myeloid disorders. This review presents emerging data on the preclinical and clinical activity of dasatinib in these diseases, which suggest that larger clinical studies are warranted.
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