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。
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 a standard diagnostic test to detect ALK-rearrangement. ALK-rearrangement is more often seen in ers with lung adenocarcinomas. The mechanism of crizotinib resistance is complicated. FISH probe kit is never/light smok ers with lung adenocarcinomas. The mechanism of crizotinib resistance is complicated.
出处
《基础医学与临床》
CSCD
北大核心
2013年第3期382-386,共5页
Basic and Clinical Medicine
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
crizotinib, anaplastic lymphoma kinase gene rearrangement, non-small cell lung cancer
