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

页码：144 / 147

页数：4