一项关于研究性极光激酶A抑制剂阿利西替尼（MLN8237）在急性髓性白血病和骨髓增生异常综合征中的探索性2期研究。
An exploratory phase 2 study of investigational Aurora A kinase inhibitor alisertib (MLN8237) in acute myelogenous leukemia and myelodysplastic syndromes.
作者信息
Goldberg Stuart L, Fenaux Pierre, Craig Michael D, Gyan Emmanuel, Lister John, Kassis Jeannine, Pigneux Arnaud, Schiller Gary J, Jung JungAh, Jane Leonard E, Fingert Howard, Westervelt Peter
机构信息
John Theurer Cancer Center at Hackensack University Medical Center, Hackensack, NJ, USA.
Service d׳hématologie Clinique, Hôpital Avicenne (AP-HP)/Université, Paris 13, Bobigny, France.
出版信息
Leuk Res Rep. 2014 Jul 5;3(2):58-61. doi: 10.1016/j.lrr.2014.06.003. eCollection 2014.
Alisertib (MLN8237) is an investigational, oral, selective, Aurora A kinase (AAK) inhibitor. In this phase 2 trial, 57 patients with acute myeloid leukemia (AML) or high-grade myelodysplastic syndrome received alisertib 50 mg BID for 7 days in 21-day cycles. Responses in 6/35 AML patients (17% response rate with an additional 49% stable disease, 34% transfusion independence) included 1 complete response lasting >1 year. No responses were observed in MDS patients. Adverse events >30% included diarrhea, fatigue, nausea, febrile neutropenia, and stomatitis. Results suggest modest activity in AML, supporting further research to better understand how AAK inhibition may induce leukemic cell senescence.
阿利西替尼（MLN8237）是一种处于研究阶段的口服选择性极光激酶A（AAK）抑制剂。在这项2期试验中，57例急性髓系白血病（AML）或高级别骨髓增生异常综合征患者接受阿利西替尼50毫克每日两次，持续7天，每21天为一个周期。35例AML患者中有6例出现反应（缓解率为17%，另有49%病情稳定，34%实现输血独立），其中1例完全缓解持续超过1年。骨髓增生异常综合征（MDS）患者未观察到反应。发生率超过30%的不良事件包括腹泻、疲劳、恶心、发热性中性粒细胞减少和口腔炎。结果表明阿利西替尼在AML中有一定活性，支持进一步研究以更好地了解抑制AAK如何诱导白血病细胞衰老。
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