2018 年第 2 期 第 13 卷

间变性淋巴瘤激酶-酪氨酸激酶抑制剂耐药机制及耐药后治疗策略研究进展

作者：彭昆伟尤长宣

英文作者：

单位：510515广州，南方医科大学南方医院肿瘤内科

英文单位：

关键词：癌,非小细胞肺；间变性淋巴瘤激酶-酪氨酸激酶抑制剂；耐药机制；治疗策略

英文关键词：

• 摘要：

• 间变性淋巴瘤激酶-酪氨酸激酶抑制剂（ALK-TKIs）能够有效治疗ALK阳性非小细胞肺癌(NSCLC)患者，可明显改善这类患者的生存状况。但是进行ALK-TKIs长期治疗仍不可避免地存在耐药问题。因此针对一代ALK-TKIs的耐药问题，不断有新一代的ALK-TKIs研发出来。国外上市的下一代ALK-TKIs有色瑞替尼、艾乐替尼、Brigatinib、Loriatinib，尽管这些新药已经批准用于克唑替尼耐药后治疗，但是这些药物同样会再次出现耐药现象,主要的耐药机制包括：原发性耐药、ALK相关继发性耐药、旁路激活以及一些少见的耐药机制。在此，我们将对ALK-TKIs的耐药机制及耐药后的治疗策略进行综述,为进一步研究提供依据。

• Research progress of mechanisms and treatments of anaplastic lymphoma kinase-tyrosine kinase inhibitors resistance

  Peng Kunwei, You Changxuan

  Department of Oncology, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China

  Corresponding author: You Changxuan, Email: ycx6026@126.com

  【Abstract】Anaplastic lymphoma kinase-tyrosine kinase inhibitors(ALK-TKIs) is effective in treatment of ALK-positive non-small-cell lung cancer, but drug resistance is an inevitable problem in long-term clinical practice. To conquer the resistance to crizotinib the first ALK-TKIs, new generation of ALK-TKIs such as ceritinib, alectinib, brigatinib and loriatinib have been applied in clinical practice. Great attentions should be paid on clinical use of new ALK-TKIs to deal with new drug resistance phenomenon after initial therapy. This paper reviewed common mechanisms of ALK-TKIs resistance and the treatment strategies.

  【Key words】Carcinoma, non-small-cell lung;Anaplastic lymphoma kinase-tyrosine kinase inhibitors;Resistance mechanism;Treatment strategy

  【Fund program】Science and Technology Project of Guangdong Province（2017B090901067）