Molecular targeted therapy has been reported to have fewer adverse effects, and offer a more convenient route of administration, compared with conventional chemotherapy. With the development of sequencing technology, and research on the molecular biology of lung cancer, especially whole-genome information on non-small cell lung cancer (NSCLC), various therapeutic targets have been unveiled. Among the NSCLC-driving gene mutations, epidermal growth factor receptor (EGFR) mutations are the most common, and approximately 10% of Caucasian, and more than 50% of Asian, NSCLC patients have been found to have sensitive EGFR mutations. A variety of targeted therapeutic agents for EGFR mutations have been approved for clinical applications, or are undergoing clinical trials around the world. This review focuses on: the indications of approved small molecular kinase inhibitors for EGFR mutation-positive NSCLC; the mechanisms of drug resistance and the corresponding therapeutic strategies; the principles of reasonable and precision molecular structure; and the drug development discoveries of next-generation inhibitors for EGFR.

中文翻译：

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小分子酪氨酸激酶抑制剂针对 NSCLC EGFR 突变的迭代升级：必要性和前景

据报道，与传统化疗相比，分子靶向治疗的不良反应更少，并且提供更方便的给药途径。随着测序技术的发展，以及肺癌分子生物学尤其是非小细胞肺癌（NSCLC）全基因组信息的研究，各种治疗靶点不断被揭示。在NSCLC驱动基因突变中，表皮生长因子受体（EGFR）突变是最常见的，大约10%的白种人、超过50%的亚洲人NSCLC患者被发现有敏感的EGFR突变。全球多种针对EGFR突变的靶向治疗药物已获批临床应用，或正在进行临床试验。本次综述重点关注：已批准的小分子激酶抑制剂治疗 EGFR 突变阳性 NSCLC 的适应症；耐药机制及相应的治疗策略；分子结构合理、精密的原则；以及下一代 EGFR 抑制剂的药物开发发现。