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FLT3抑制剂能否克服急性髓系白血病的耐药性?

Can FLT3 inhibitors overcome resistance in AML?

作者信息

Tam Winnie F, Gary Gilliland D

机构信息

Brigham and Women's Hospital, Harvard Medical School, Boston, MA 02115, USA.

出版信息

Best Pract Res Clin Haematol. 2008 Mar;21(1):13-20. doi: 10.1016/j.beha.2007.11.003.

DOI:10.1016/j.beha.2007.11.003
PMID:18342808
Abstract

The identification of FLT3 mutations across a range of the cytogenetic subgroups of AML has opened up the possibility of a targeted therapeutic approach with broad applicability. Four agents are currently in clinical trials, at least 3 of which have both sufficient activity against AML and sufficiently acceptable toxicity profiles to support continued efforts to refine their inclusion into therapeutic regimens for AML. Better understanding of the genetics of inherent and acquired resistance is needed to guide development of second-generation agents. Optimizing the integration of FLT3 inhibitor therapy with chemotherapy has the potential both to decrease toxicity and improve response.

摘要

在一系列急性髓系白血病(AML)细胞遗传学亚组中对FLT3突变的识别开启了一种具有广泛适用性的靶向治疗方法的可能性。目前有四种药物正在进行临床试验,其中至少有三种对AML具有足够的活性且毒性特征足够可接受,以支持继续努力优化将它们纳入AML治疗方案。需要更好地了解内在和获得性耐药的遗传学,以指导第二代药物的开发。优化FLT3抑制剂治疗与化疗的整合有可能降低毒性并改善反应。

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Mol Cell Biochem. 2016 Sep;420(1-2):121-8. doi: 10.1007/s11010-016-2775-1. Epub 2016 Jul 20.
2
Mechanisms of resistance to FLT3 inhibitors.FLT3抑制剂的耐药机制。
Drug Resist Updat. 2009 Feb-Apr;12(1-2):8-16. doi: 10.1016/j.drup.2008.12.001. Epub 2009 Jan 21.