ALK抑制剂上市药物的研发历程

Development History of Marketed ALK Inhibitors

ALK为间变性淋巴瘤激酶,是胰岛素受体酪氨酸激酶家族中的一员。ALK基因在多种肿瘤细胞中异常活跃,是抗肿瘤药物研究中较为成熟的重要靶标之一。主要对ALK的结构与功能、 EML4-ALK融合基因信号通路在治疗NSCLC中的调控作用以及目前已经上市的ALK抑制剂的研发历程进行综述,旨在为药物,特别是以ALK为靶点的药物研发提供指导。

ALK, an anaplastic lymphoma kinase, is a member of the insulin receptor tyrosine kinase family. It was observed that the ALK gene was extremely active in a variety of tumor cells and was an important target for the study of antitumor drugs. This review mainly discussed the structure and function of ALK, and the role of the EMIA-ALK mutations signaling pathway in treating NSCLC. Meanwhile, the development process of currently marketed ALK inhibitors was also described focusing on providing effective research ideas for developing new drugs based on ALK or other targets.