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PMID: 25709401 已发表 · epublish 英语

The role of dasatinib in the management of chronic myeloid leukemia.

Drug design, development and therapy ·第 9 卷 ·2016-05-17

Chen Runzhe, Chen Baoan

摘要

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.

关键词
clinical trials imatinib tyrosine kinase inhibitor
文献信息
期刊
Drug design, development and therapy
期刊简称
Drug Des Devel Ther
发表日期
2016-05-17
收录日期
2015-02-24
更新日期
2015-04-08
语言
英语
国家/地区
New Zealand
NLM ID
101475745
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