达沙替尼
伊马替尼
医学
酪氨酸激酶
髓系白血病
酪氨酸激酶抑制剂
阿布勒
癌症研究
内科学
甲磺酸伊马替尼
费城染色体
肿瘤科
药理学
染色体易位
化学
癌症
受体
基因
生物化学
作者
Markus Lindauer,Andreas Hochhaus
出处
期刊:Recent results in cancer research
日期:2018-01-01
卷期号:: 29-68
被引量:45
标识
DOI:10.1007/978-3-319-91439-8_2
摘要
Dasatinib is an oral available short-acting inhibitor of multiple tyrosine kinases. It was designed to inhibit ABL and SRC, but also has activity in multiple other kinases, including c-KIT, PDGFR-α, PDGFR-β, and ephrin receptor kinases. Dasatinib is a very potent inhibitor of BCR-ABL and an effective treatment for the BCR-ABL-driven diseases chronic myeloid leukemia (CML) and Philadelphia-chromosome-positive acute lymphoblastic leukemia (Ph+ ALL), characterized by the constitutively active tyrosine kinase, BCR-ABL. Dasatinib is approved for the treatment of CML (all phases) including children and for the treatment of Ph+ ALL, resistant or intolerant to prior imatinib treatment. Randomized trials in CML comparing dasatinib with imatinib show that first-line dasatinib causes significantly deeper and faster molecular remissions. In accelerated and blastic phase CML, as well as in Ph+ ALL, dasatinib frequently induces complete hematologic and cytogenetic remissions even in imatinib pretreated patients. Remissions however are often short. Dasatinib is administered independent of food intake as a once-daily dose of 100 mg in chronic phase CML and 140 mg in Ph+ ALL or blastic phase. Side effects of dasatinib are frequent but mostly moderate and manageable and include cytopenias and pleural effusions. The review presents the preclinical and clinical activity of dasatinib with a focus on clinical studies in CML.
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