Liu Yuanyuan, Li Yihui, Wang Jiangong
First Department of Comprehensive Treatment of Tumors, Tangshan People's Hospital, North China University of Science and Technology, Tangshan 063000, China.
Zhongguo Fei Ai Za Zhi. 2020 Nov 20;23(11):970-975. doi: 10.3779/j.issn.1009-3419.2020.102.28. Epub 2020 Aug 10.
Lung cancer has the highest mortality rate in the world. The first- and second-generation epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs) greatly improve the survival time and quality of life of patients with non-small cell lung cancer (NSCLC) to some extent. However, after a period of progression-free survival, most patients develop drug resistance, in which T790M mutation is the mainly resistance mechanism. The third-generation EGFR-TKIs, represented by osimertinib, are found to have significant effect on this resistance. The effect is remarkable, but drug resistance is still inevitable. For example, C797S mutation, mesenchymal-epithelial transition (MET), RAS mutation, BRAF mutation, transformation of small cell lung cancer (SCLC), transformation of epithelial mesenchymal transition (EMT), etc. But, there is no standard and effective treatment after the third-generation EGFR-TKIs resistance. In this view, we summarize the research progress in the new generation EGFR-TKIs after third-generation, in order to provide some reference for the follow-up research and treatment. .
肺癌是全球死亡率最高的癌症。第一代和第二代表皮生长因子受体酪氨酸激酶抑制剂(EGFR-TKIs)在一定程度上极大地提高了非小细胞肺癌(NSCLC)患者的生存时间和生活质量。然而,在经历一段无进展生存期后,大多数患者会产生耐药性,其中T790M突变是主要的耐药机制。以奥希替尼为代表的第三代EGFR-TKIs被发现对这种耐药性有显著效果。其效果显著,但耐药性仍不可避免。例如,C797S突变、间质-上皮转化(MET)、RAS突变、BRAF突变、小细胞肺癌(SCLC)转化、上皮间质转化(EMT)转化等。但是,第三代EGFR-TKIs耐药后尚无标准有效的治疗方法。鉴于此,我们总结了第三代之后新一代EGFR-TKIs的研究进展,以便为后续的研究和治疗提供一些参考。