肺癌是严重威胁人类健康的重大疾病，而非小细胞肺癌（non-small cell lung cancer，NSCLC）则占所有类型肺癌的85%以上。目前，“个体化给药”是改善晚期NSCLC患者治疗效果的一条前景良好的途径。2011年8月，美国食品和药物管理局（FDA）批准了克里唑替尼（crizotinib），一种ALK/MET/ROS1抑制剂，用于治疗间变性淋巴瘤激酶（ALK）基因重排的非小细胞肺癌，同时还批准了一种ALK荧光原位杂交法检测试剂盒，作为伴侣诊断试剂，用于ALK重排的非小细胞肺癌的检测。随后，克里唑替尼被作为一种ALK和MET抑制剂开发，用于治疗由ALK和MET 突变驱动的其他类型的肿瘤。最近已经证实在ROS1重排的非小细胞肺癌中克里唑替尼是一种有效的ROS1抑制剂，并且未来可能用于ROS1基因重排肿瘤的临床治疗。对克里唑替尼的设计开发、治疗ALK重排的NSCLC的的临床应用、药物不良反应以及相应的疾病诊断检测方法进行了回顾，以期为NSCLC的靶向治疗药物的研究和开发提供参考。

Lung cancer is the major disease seriously threaten human health, in which non-small cell lung cancer (NSCLC) account to more than 85%. At present, “personalized administration” is a promising approach that could improve the treatment outcomes in patients with NSCLC. In August 2011, crizotinib was approved by the US Food and Drug Administration (FDA) for the treatment of anaplastic lymphoma kinase (ALK)-rearranged NSCLC as an ALK/MET/ROS1 inhibitor. At the same time, an ALK companion diagnostic fluorescence in situ hybridization assay was approved by FDA as an accompanied reagent for the detection of ALK-rearranged NSCLC. Crizotinib was developed as an ALK and MET inhibitor to treat other tumor types driven by alteration in ALK and MET. Recently, it has been shown that crizotinib is a kind of effective ROS1 inhibitor on ROS1-rearranged NSCLC, and it may be used in the clinical treatment of ROS1-rearranged tumors. This article reviewed the design and development of crizotinib, its clinical application in ALK-rearranged NSCLC, its adverse drug effects, and the dignaose methods for the disease, in order to support the references to the research and development of the targeting drug for the treatment of NSCLC.