The role of dasatinib in the management of chronic myeloid leukemia.
The role of dasatinib in the management of chronic myeloid leukemia.
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达沙替尼在慢性粒细胞白血病治疗中的作用
DOI：
10.2147/dddt.s80207
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发表时间：
2015
期刊：
影响因子：
--
通讯作者：
Chen B
中科院分区：
文献类型：
--
作者：
Chen R;Chen B
达沙替尼是一种第二代酪氨酸激酶抑制剂（TKI），用于对既往治疗有耐药性或不耐受的慢性、母细胞性或加速期慢性髓性白血病（CML）患者。它能有效抑制BCR/ABL和SRC家族激酶（SRC、LCK、HCK、YES、FYN、FGR、BLK、LYN、FRK），以及c-KIT、PDGFR-a和-b和ephrin受体激酶。各种临床试验证明，它具有更持久的完全血液学和细胞遗传学反应，以及在伊马替尼耐药或不耐受的CML中更强的效力，并且与伊马替尼相比，它在新诊断的CML中也显示出其优势。本文就达沙替尼的结构、作用机制、药代动力学和药物遗传学等方面作一综述。我们还总结了达沙替尼治疗CML的临床试验，并提出了我们对达沙替尼治疗CML的建议。
Dasatinib is a second-generation tyrosine kinase inhibitor (TKI) for chronic, blastic, or accelerated phase chronic myeloid leukemia (CML) patients who are resistant or intolerant to previous treatment. It potently inhibits BCR/ABL and SRC-family kinases (SRC, LCK, HCK, YES, FYN, FGR, BLK, LYN, FRK), as well as c-KIT, PDGFR-a and -b, and ephrin receptor kinase. Various clinical trials have provided evidence that it has more durable complete hematologic and cytogenetic responses, as well as more potency in imatinib-resistant or -intolerant CML, and it has also shown its advantages in newly diagnosed CML compared to imatinib. In this review, we mainly focus on the structure, mechanisms, pharmacokinetics, and pharmacogenetics of dasatinib. We also summarize clinical trials with dasatinib on CML and provide our recommendations for dasatinib in the treatment of CML.