With a greater understanding of tumor biology, novel molecular-targeted strategies that block cancer progression pathways have been evaluated as a new therapeutic approach for treating non-small cell lung cancer (NSCLC). Epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKIs), such as gefitinib and erlotinib, show favorable response to EGFR mutant lung cancer in some populations of NSCLC patients. However, the efficacy of EGFR-TKIs is limited by either primary (de novo) or acquired resistance after therapy. This review will focus on recently identified mechanisms of primary and acquired resistance to EGFR TKIs and strategies currently being employed to overcome resistance.
随着分子靶向治疗药物的发展，以吉非替尼（gefitinib, iressa）和厄洛替尼（erlotinib, tarceva）为代表的表皮生长因子受体酪氨酸激酶抑制剂（epidermal growth factor receptor-tyrosine kinases inhibitors, EGFR-TKIs）在治疗非小细胞肺癌中发挥了重要作用。然而在临床前和临床研究中发现许多患者对此药物存在原发性耐药或获得性耐药，使该类药物的使用受到一定限制。本文就近年来对EGFR-TKIs耐药机制的研究进展进行综述。