基础医学与临床 ›› 2013, Vol. 33 ›› Issue (3): 382-386.

• 短篇综述 • 上一篇    

Crizotinib在ALK基因阳性非小细胞肺癌中的临床研究进展

唐敏,武晓楠,程刚   

  1. 卫生部北京医院
  • 收稿日期:2012-06-14 修回日期:2012-08-27 出版日期:2013-03-05 发布日期:2013-03-05
  • 通讯作者: 程刚 E-mail:gangcheng58@126.com

Clinical research progress of crizotinib in non-small cell lung cancer patients with ALK-rearrangement positive

  • Received:2012-06-14 Revised:2012-08-27 Online:2013-03-05 Published:2013-03-05

摘要: Crizotinib是小分子ATP竞争性抑制剂,对间变性淋巴瘤激酶(ALK)和肝细胞生长因子受体(c-Met/HGFR)以及它们的致癌变异体有选择性抑制作用。在临床研究PROFILE 1001和PROFILE 1005中,ALK重排阳性NSCLC患者对crizotinib有效率达50%~60%,大多数不良反应为1~2度。Vysis ALK breakapart FISH probe kit为检测ALK重排的标准方法。ALK重排更易出现在不吸烟或少吸烟的肺腺癌患者中。crizotinib的耐药机制比较复杂。

关键词: 克唑替尼,间变性淋巴瘤激酶基因重排,非小细胞肺癌

Abstract: Crizotinib is a selective ATP-competitive inhibitor of anaplastic lymphoma kinase(ALK), hepatocyte growth factor receptor(c-Met/HGFR) tyrosine kinases and their oncogenic variants. In PROFILE 1001 and PROFILE 1005 clinical trials, the response rate of crizotinib is 50%~60% for non-small cell lung cancer(NSCLC) patients with ALK rearrangement. Most of the adverse events are grade 1~2. Vysis ALK breakapart FISH probe kit is the standard diagnostic test to detect ALK-rearrangement. ALK-rearrangement is more often seen in never/light smokers with lung adenocarcinomas. The mechanism of crizotinib resistance is complicated.

Key words: crizotinib, anaplastic lymphoma kinase gene rearrangement, non-small cell lung cancer

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