Wang Shuhang, Cang Shundong, Liu Delong
The Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education), Peking University Cancer Hospital, Beijing, China.
Department of Oncology, People's Hospital of Henan Province, Zhengzhou University, Zhengzhou, China.
J Hematol Oncol. 2016 Apr 12;9:34. doi: 10.1186/s13045-016-0268-z.
The tyrosine kinase inhibitors (TKI) against epidermal growth factor receptor (EGFR) are widely used in patients with non-small cell lung cancer (NSCLC). However, EGFR T790M mutation leads to resistance to most clinically available EGFR TKIs. Third-generation EGFR TKIs against the T790M mutation have been in active clinical development. These agents include osimertinib, rociletinib, HM61713, ASP8273, EGF816, and PF-06747775. Osimertinib and rociletinib have shown clinical efficacy in phase I/II trials in patients who had acquired resistance to first- or second-generation TKIs. Osimertinib (AZD9291, TAGRISSO) was recently approved by FDA for metastatic EGFR T790M mutation-positive NSCLC. HM61713, ASP8237, EGF816, and PF-06747775 are still in early clinical development. This article reviews the emerging data regarding third-generation agents against EGFR T790M mutation in the treatment of patients with advanced NSCLC.
针对表皮生长因子受体（EGFR）的酪氨酸激酶抑制剂（TKI）被广泛应用于非小细胞肺癌（NSCLC）患者。然而，EGFR T790M突变会导致对大多数临床可用的EGFR TKI产生耐药性。针对T790M突变的第三代EGFR TKI已处于积极的临床开发阶段。这些药物包括奥希替尼、罗西替尼、HM61713、ASP8273、EGF816和PF-06747775。奥希替尼和罗西替尼在对第一代或第二代TKI产生耐药性的患者的I/II期试验中已显示出临床疗效。奥希替尼（AZD9291，泰瑞沙）最近被美国食品药品监督管理局（FDA）批准用于转移性EGFR T790M突变阳性的NSCLC。HM61713、ASP8237、EGF816和PF-06747775仍处于早期临床开发阶段。本文综述了关于第三代针对EGFR T790M突变的药物在晚期NSCLC患者治疗中的最新数据。
