Division of Molecular Pathology, The Institute of Cancer Research, London, SW3 6JB, UK.
Division of Molecular Pathology, The Institute of Cancer Research, London, SW3 6JB, UK.
Semin Cancer Biol. 2020 Apr;61:167-179. doi: 10.1016/j.semcancer.2019.09.015. Epub 2019 Sep 25.
Epidermal growth factor receptor (EGFR) mutations are the second most common oncogenic driver event in non-small cell lung cancer (NSCLC). Classical activating mutations (exon 19 deletions and the L858R point mutation) comprise the vast majority of EGFR mutations and are well defined as strong predictors for good clinical response to EGFR tyrosine kinase inhibitors (EGFRi). However, low frequency mutations including point mutations, deletions, insertions and duplications occur within exons 18-25 of the EGFR gene in NSCLC and are associated with poorer responses to EGFRi. Despite an increased uptake of more sensitive detection methods to identify rare EGFR mutations in patients, our understanding of the biology of these rare EGFR mutations is poor compared to classical mutations. In particular, clinical data focused on these mutations is lacking due to their rarity and challenges in trial recruitment, resulting in an absence of effective treatment strategies for many low frequency EGFR mutations. In this review, we describe the structural and mechanistic features of rare EGFR mutations in NSCLC and discuss the preclinical and clinical evidence for EGFRi response for individual rare EGFR mutations. We also discuss EGFRi sensitivity for complex EGFR mutations, and conclude by offering a perspective on the outstanding questions and future steps required to make advances in the treatment of NSCLC patients that harbour rare EGFR mutations.
表皮生长因子受体 (EGFR) 突变是非小细胞肺癌 (NSCLC) 中第二常见的致癌驱动事件。经典激活突变(外显子 19 缺失和 L858R 点突变)构成了 EGFR 突变的绝大多数,并且被明确为对 EGFR 酪氨酸激酶抑制剂 (EGFRi) 良好临床反应的强烈预测因子。然而,低频率突变包括点突变、缺失、插入和重复,发生在 NSCLC 中的 EGFR 基因的外显子 18-25 内,与对 EGFRi 的反应较差相关。尽管越来越多地采用更敏感的检测方法来识别患者中罕见的 EGFR 突变,但与经典突变相比,我们对这些罕见 EGFR 突变的生物学了解甚少。特别是,由于这些突变的罕见性和试验招募的挑战,缺乏针对这些突变的临床数据,导致许多低频 EGFR 突变缺乏有效的治疗策略。在这篇综述中,我们描述了 NSCLC 中罕见 EGFR 突变的结构和机制特征,并讨论了针对个别罕见 EGFR 突变的 EGFRi 反应的临床前和临床证据。我们还讨论了复杂 EGFR 突变的 EGFRi 敏感性,并就治疗携带罕见 EGFR 突变的 NSCLC 患者方面的未决问题和未来步骤提供了展望。