【摘要】 间变性淋巴瘤激酶(ALK)抑制剂是目前治疗NSCLC伴ALK阳性的有效药物,然而,耐药性的产生严重限制了其临床应用。本文对ALK抑制剂耐药产生的主要机制如二次基因突变、基因扩增、旁路通路激活等进行了简要介绍,并对联合用药、开发新型PROTAC降解剂等逆转耐药策略进行了综述,以期为ALK抑制剂药物的未来发展提供参考。更多还原

【Abstract】 Anaplastic lymphoma kinase(ALK) inhibitors are regarded as effective drugs for the treatment of ALK-positive NSCLC.However,the emergence of drug resistance has limited its further clinical application.This article briefly introduces the resistance mechanism of ALK inhibitors including acquired secondary mutations,gene amplification,by pass signaling pathway activation and reviews the recent advances on the reversal strategies such as drug combination,developing novel PROTACs to overcome drug resistance,so as to provide some reference for the development of ALK inhibitors.更多还原