Carpinelli Patrizia, Moll Jürgen
Nerviano Medical Sciences Srl, Nerviano, Milano, Italy.
Curr Opin Drug Discov Devel. 2009 Jul;12(4):533-42.
The development of Aurora kinase inhibitors is a competitive research field, with many inhibitors currently being evaluated in preclinical and clinical studies. Progress during the past few years, both preclinically and clinically, has increased the evidence supporting Aurora kinases as promising molecular targets for the treatment of cancer. Aurora kinase inhibitors differ based on their selectivity within the Aurora kinase family and their cross-reactivities with other kinases. Additional factors that will contribute to the success or failure of the Aurora kinase inhibitors include: routes of administration, drug-like properties, workable combinations with approved drugs, adequate clinical development paths, and the identification of the appropriate patient population. The clinical trial results that are emerging for the most advanced inhibitors are promising, and it is probable that clinical proof of concept will be achieved, and that Aurora kinase inhibitors will be part of treatment for cancer in the future.
极光激酶抑制剂的研发是一个竞争激烈的研究领域,目前有许多抑制剂正处于临床前和临床研究阶段。过去几年在临床前和临床方面取得的进展增加了支持极光激酶作为治疗癌症的有前景分子靶点的证据。极光激酶抑制剂因其在极光激酶家族中的选择性以及与其他激酶的交叉反应性而有所不同。其他将影响极光激酶抑制剂成败的因素包括:给药途径、类药性质、与已获批药物的可行联合用药、适当的临床开发路径以及确定合适的患者群体。针对最先进抑制剂的临床试验结果很有前景,很可能会实现临床概念验证,并且极光激酶抑制剂未来将成为癌症治疗的一部分。