Marin-Acevedo Julian A, Pellini Bruna, Kimbrough ErinMarie O, Hicks J Kevin, Chiappori Alberto
Division of Medical Oncology, Indiana University Melvin and Bren Simon Comprehensive Cancer Center, Indianapolis, IN 46202, USA.
Department of Thoracic Oncology, Moffitt Cancer Center and Research Institute, Tampa, FL 33612, USA.
Cancers (Basel). 2023 Jan 19;15(3):629. doi: 10.3390/cancers15030629.
The development of targeted therapies over the past two decades has led to a dramatic change in the management of -mutant non-small cell lung cancer (NSCLC). While there are currently five approved EGFR tyrosine kinase inhibitors (TKIs) for treating -mutant NSCLC in the first-line setting, therapy selection after progression on EGFR TKIs remains complex. Multiple groups are investigating novel therapies and drug combinations to determine the optimal therapy and treatment sequence for these patients. In this review, we summarize the landmark trials and history of the approval of EGFR TKIs, their efficacy and tolerability, and the role of these therapies in patients with central nervous system metastasis. We also briefly discuss the mechanisms of resistance to EGFR TKIs, ongoing attempts to overcome resistance and improve outcomes, and finalize by offering treatment sequencing recommendations.
在过去二十年中，靶向治疗的发展使表皮生长因子受体（EGFR）突变的非小细胞肺癌（NSCLC）的治疗发生了巨大变化。虽然目前有五种获批的EGFR酪氨酸激酶抑制剂（TKIs）用于一线治疗EGFR突变的NSCLC，但EGFR TKIs治疗进展后的治疗选择仍然复杂。多个研究团队正在研究新的治疗方法和药物组合，以确定这些患者的最佳治疗方案和治疗顺序。在本综述中，我们总结了EGFR TKIs的标志性试验、获批历程、疗效和耐受性，以及这些疗法在中枢神经系统转移患者中的作用。我们还简要讨论了对EGFR TKIs的耐药机制、克服耐药性和改善预后的持续尝试，并通过提供治疗顺序建议来完成本综述。
