摘要
宝那替尼是第三代激酶抑制剂,旨在克服守门人T315I突变。在不同的试验中,该药物对天然bcr-abl 1激酶有抑制作用。ABL 1突变由于这个原因,目前已表明,在抵抗和/或不耐大司替尼和尼洛替尼的疾病的各个阶段治疗慢性粒细胞白血病(Cml)。而伊马替尼不再被用于治疗T315I突变的患者。该药物也适用于Ph急性淋巴细胞白血病(ALL)。宝那替尼于2013年暂停使用心血管血栓事件的发生。从那时起,不同的研究者分析了普拉替尼患者的基线特征,特别是心血管方面的特征,n说明在这种情况下的一般管理建议。 在这篇综述中,我们将讨论帕纳替尼在CML和Ph所有患者中的临床试验数据。它也将重点关注药物的安全性和耐受性概况以及未来。就业前景。
关键词: 慢性髓系白血病,Ph急性淋巴细胞白血病,扎那替尼,T315I突变,心血管事件,佩斯试验,EPIC试验。
图形摘要
Current Cancer Drug Targets
Title:Ponatinib: A Review of Efficacy and Safety
Volume: 18 Issue: 9
关键词: 慢性髓系白血病,Ph急性淋巴细胞白血病,扎那替尼,T315I突变,心血管事件,佩斯试验,EPIC试验。
摘要: Ponatinib is a third generation kinase inhibitor designed to overcome the gatekeeper T315I mutation. In different trials this drug showed inhibitory activity against native BCR-ABL1 kinase and several ABL1 mutations. For this reason, ponatinib is currently indicated for the treatment of chronic myeloid leukaemia (CML) in every phase of disease resistant and/or intolerant to dasatinib and nilotinib and for whom imatinib is not indicated anymore or for patients with T315I mutation. The drug is also indicated for Ph+ acute lymphoblastic leukaemia (ALL). Ponatinib was temporarily suspended in 2013 for the occurrence of cardiovascular thrombotic events. Since then, different investigators analyzed baseline characteristics of patient candidates for ponatinib, especially cardiovascular profile, in order to describe general management recommendations in this setting.
In this review, clinical trials data about the use of ponatinib in CML and Ph+ ALL patients will be discussed. It will be focused also about the safety and tolerability profile of the drug and future perspectives of employment.
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Cite this article as:
Ponatinib: A Review of Efficacy and Safety, Current Cancer Drug Targets 2018; 18 (9) . https://dx.doi.org/10.2174/1568009617666171002142659
DOI https://dx.doi.org/10.2174/1568009617666171002142659 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
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