Mechanisms of Resistance of EGFR Tyrosine Kinase Inhibitors

• 作 者: LiwuFu;
• 机 构: State Key Laboratory of Oncology in Southern China,Cancer Center,Sun Yat-Sen University,Guangzhou 51
• 出 处: 2014医学科学前沿暨第三届个体化治疗与抗肿瘤药物研究新趋向研讨会
• 发表日期: 2014年期

　　Since that non-small cell lung cancer (NSCLC) is activated by epidermal growth factor receptor (EGFR) mutations was found, the EGFR tyrosine kinase inhibitors (EGFR-TKIs) such as gefitinib and elrotinib have put into use in the clinical treatment and received a good effect.However, patients eventually develop drug resistance.Resistance to EGFR-TKIs is inevitable due to various mechanisms, such as the secondary mutation (T790M), activation of alternative pathways (c-Met, HGF, AXL),aberrance of the downstream pathways (K-ras mutations, loss of PTEN), impairment of apoptosis pathway mediated by EGFR-TKIs (BIM deletion polymorphism),histologic transformation and ATP binding cassette (ABC) transporter effusion.Here we aim to review and summarize the resistant mechanisms to EGFR-TKIs and to provide guidance for the therapeutic strategies.