VX-680/MK-0457 - Aurora kinase inhibitor oncolytic

被引：8
|
作者：
Wang, Y. [1 ]
Serradell, N. [1 ]
机构：
[1] Prous Sci, E-08080 Barcelona, Spain
来源：
DRUGS OF THE FUTURE | 2007年 / 32卷 / 02期
关键词：
D O I：
10.1358/dof.2007.032.02.1076496
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
VX-680/MK-0457 is a small-molecule Aurora kinase inhibitor with inhibition constants (K(i)) of 0.6, 18 and 4.6 nM for Aurora kinase A, B and C, respectively; it also inhibits Flt-3 and AN kinases, particularly mutant forms. The compound displays potent antitumor activity in a broad range of cancer cell lines and is well tolerated in preclinical studies. A phase I clinical trial of VX-680/MK-0457 was carried out in patients with chronic myeloid leukemia (CML) or acute lymphocytic leukemia (ALL) with the T315l Bcr-Abl resistance mutation and patients with refractory JAK2-positive myeloproliferative disease. VX-680/MK-0457 demonstrated encouraging antitumor activity and a good overall safety profile.
引用
收藏
页码：144 / 147
页数：4
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