用于非小细胞肺癌治疗的第三代 EGFR-TKIs 研究进展

肺癌是全球致死率最高的恶性肿瘤,其中非小细胞肺癌(NSCLC)占全部肺癌病例的 80% 左右。相较于传统化疗,表皮生长因 子受体酪氨酸激酶抑制剂(EGFR-TKIs)用于 EGFR 突变型 NSCLC 患者,可获得更为卓越的疗效。但是,EGFR-TKIs 长期使用会产生 获得性耐药,主要机制为 EGFR T790M 突变。临床研究表明,以奥希替尼、rociletinib 和 HM61713 为代表的第三代 EGFR-TKIs 对 EGFR T790M 突变阳性 NSCLC 具有较好的疗效,为 EGFR T790M 突变阳性患者的有效治疗带来了新的希望。综述第三代 EGFR-TKIs 的最新临床研究及耐药机制研究进展。

Research Progress in the Third Generation EGFR-TKIs for Non-small Cell Lung Cancer

Lung cancer is a malignant tumor with the highest mortality over the world, in which non-small cell lung cancer (NSCLC) accounts for about 80%. Compared with conventional chemotherapies, epidermal growth factor receptor-tyrosine kinase inhibitors(EGFR-TKIs) have shown remarkable ef cacy in NSCLC patients with EGFR mutation. However, acquired resistance due to EGFR T790M mutation develops after long-term use of EGFR-TKIs. It has been suggested that the third generation EGFR-TKIs such as osimertinib, rociletinib and HM61713 are highly ef cacious for EGFR T790M-positive NSCLC, bringing new hope to the effective treatment of EGFR T790M-positive NSCLC patients. In this article, the latest progress in clinical researches and resistance mechanisms of the third generation EGFR-TKIs were reviewed.