Dasatinib
Dasatinib
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DOI：
10.1007/978-3-642-01222-8_7
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发表时间：
2010-01-01
期刊：
影响因子：
--
通讯作者：
Hochhaus, Andreas
中科院分区：
文献类型：
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作者：
Lindauer, Markus;Hochhaus, Andreas
dasatinib（前BMS 354825）是一种口服的小分子多次激酶抑制剂。它有效抑制BCR-ABL和SRC家庭激酶（SRC，LCK，是的，FYN），但也可以抑制C-KIT，PDGFR-ALPHA和BETA和EPHRIN受体激酶。Dasatinib.dasatinib在表达细胞中的效力大约300倍体外未经未来的BCR-ABL。该药物表现出对临床相关突变的活性，包括持续伊马替尼治疗期间与预后不良相关的突变。Dasatinib被批准用于治疗BCR-ABL阳性慢性髓样白血病（CML）患者，耐药或对伊马替尼在慢性，慢性，慢性，抗imatinib的耐受性治疗。加速和爆炸阶段。它还被批准用于治疗费城染色体阳性（pH+）急性淋巴细胞白血病（全）对伊马替尼的抗药性或不耐受性。在慢性期CML中，每日100 mg的单一剂量会导致高血液学和分子缓解率和生存期的延长。在加速阶段以及总共中，建议每天两次两次。即使在预后不良的患者群体中，也经常发生完全的血液学和细胞遗传学减免（CR）。然而，汇总的速度很短。达沙尼的侧面效果频繁，但大多是中等且易于管理的，包括细胞质和胸腔积液。必须鉴定达沙替尼在包括实体瘤在内的其他疾病中的作用。
Dasatinib, (former BMS 354825), is an orally available small-molecule multikinase inhibitor. It potently inhibits BCR-ABL and SRC-family kinases (SRC, LCK, YES, FYN), but also c-KIT, PDGFR-alpha and beta, and ephrin receptor kinase.Dasatinib is about 300 times more potent than imatinib in cells expressing unmutated BCR-ABL in vitro. The drug has demonstrated activity against clinically relevant mutations, including those associated with poor prognosis during ongoing imatinib therapy.Dasatinib is approved for the treatment of patients with BCR-ABL-positive chronic myeloid leukemia (CML), resistant or intolerant to imatinib in chronic, accelerated, and blast phase. It also is approved for the treatment of Philadelphia Chromosome positive (Ph+) acute lymphoblastic leukemia (ALL) resistant or intolerant to imatinib.A single daily dose of 100 mg in chronic phase CML results in high hematologic and molecular remission rates and prolongation of survival. In accelerated and blastic phase as well as in ALL, 70 mg twice daily is recommended. Complete hematologic and cytogenetic remissions (CR) frequently occur even in this patient group with poor prognosis. Remissions however are very short.Side effects of dasatinib are frequent but mostly moderate and manageable and include cytopenias and pleural effusions. The role of dasatinib in other diseases, including solid tumors, has to be identified.