阿法替尼在非小细胞肺癌中的临床应用进展

Progress on the Clinical Application of Afatinib in Non-small Cell Lung Cancer

阿法替尼（afatinib）是表皮生长因子受体（EGFR）酪氨酸激酶家族的抑制剂,与第一代表皮生长因子受体酪氨酸激酶抑制剂（epidermal growth factor receptor-tyrosine kinase inhibitor,EGFR-TKI）非共价结合于EGFR胞内段不同,阿法替尼共价结合于所有由EGFR、Her-2、ErbB3和ErbB4组成的同源或异源二聚体,从而抑制酪氨酸激酶自磷酸化和下游信号,且这种结合不可逆。目前非小细胞肺癌靶向治疗领域,共有三代EGFR-TKI药物。文章就三代药物同堂的情况下,如何合理使用介于第一和第三代药物之间的第二代药物阿法替尼作一综述。

Afatinib is a protein kinase inhibitor that irreversibly inhibits the ErbB family tyrosine kinases with oral administration. There are three generations of epidermal growth factor receptor-tyrosine kinase inhibitors（EGFR-TKI） in non-small cell lung cancer（NSCLC） targeted therapy at present. This article aims to review how to make rational use of the second generation drug afatinib in this situation.