Lee Chung-Shien, Sharma Sandhya, Miao Emily, Mensah Cheryl, Sullivan Kevin, Seetharamu Nagashree
Department of Clinical Health Professions, St. John's University, College of Pharmacy and Health Sciences, Queens, NY 11439, USA.
Division of Medical Oncology and Hematology, Northwell Health Cancer Institute, Donald and Barbara Zucker School of Medicine at Hofstra/Northwell, Lake Success, NY 11042, USA.
Lung Cancer (Auckl). 2020 Oct 7;11:73-103. doi: 10.2147/LCTT.S258444. eCollection 2020.
Mutations in the epidermal growth factor receptor (EGFR) are common amongst those with non-small cell lung cancer and represent a major factor in treatment decisions, most notably in the advanced stages. Small molecule tyrosine kinase inhibitors (TKIs) that target the EGFR, such as erlotinib, gefitinib, icotinib, afatinib, dacomitinib and osimertinib, have all shown to be effective in this setting. Osimertinib, a third-generation EGFR TKI, is a favorable option, but almost all patients develop resistance at some time point. There are no effective treatment options for patients who progress on osimertinib, but ongoing trials will hopefully address this unmet need. The aim of this review is to provide a comprehensive review of the data with EGFR TKIs, management of the toxicities and the ongoing trials with this class of agents.
表皮生长因子受体（EGFR）突变在非小细胞肺癌患者中很常见，是治疗决策的主要因素，在晚期尤为明显。靶向EGFR的小分子酪氨酸激酶抑制剂（TKIs），如厄洛替尼、吉非替尼、埃克替尼、阿法替尼、达可替尼和奥希替尼，在这种情况下均显示出疗效。奥希替尼作为第三代EGFR TKI是一个不错的选择，但几乎所有患者在某个时间点都会产生耐药性。对于奥希替尼治疗进展的患者，目前尚无有效的治疗方案，但正在进行的试验有望满足这一未得到满足的需求。本综述的目的是全面回顾EGFR TKIs的数据、毒性管理以及这类药物正在进行的试验。
