ALK抑制剂研究进展

The development and progress of ALK inhibitors

间变性淋巴瘤激酶(anaplastic lymphoma kinase,ALK)基因是一种跨膜受体酪氨酸激酶,可在多种恶性肿瘤中发生变异或与其他癌基因融合,是肿瘤的致癌驱动基因。ALK抑制剂包括克唑替尼、色瑞替尼及艾乐替尼,其在ALK阳性的非小细胞肺癌(non-small cell lung cancer,NSCLC)患者中已表现出显著的疗效。然而ALK抑制剂的耐药问题也较为普遍,新的抑制剂和其他靶向策略正在研发中。现对ALK抑制剂在NSCLC治疗中的研究进展及克服耐药的新策略进行综述。

As a transmembrane tyrosine kinase receptor, the anaplastic lymphoma kinase（ALK） can be oncogenically altered and fuse with other oncogenes in several malignancies. As a result, it is involved in the carcinogenesis process of cancers. ALK inhibitors, including Crizotinib, Ceritinib and Alectinib, have been demonstrated significant effectiveness in ALK-positive patients, in particular in non-small cell lung cancer（NSCLC）. However, the emergence of resistance is still a concern and challenge for doctors. Newly developed ALK inhibitors and other targeting strategies are being studied. This review outlines recent developments in the treatment of ALK positive NSCLC and new strategies overcoming the ALK inhibitors resistance.