小分子表皮生长因子受体酪氨酸激酶抑制剂的研究进展

Research Progress of Small-molecule Epidermal Growth Factor Receptor-Tyrosine Kinase Inhibitors

表皮生长因子受体是一种具有酪氨酸激酶活性的膜受体,在细胞的增殖、迁移、代谢、分化和存活中发挥重要作用。目前,表皮生长因子受体酪氨酸激酶抑制剂(epidermal growth factor receptor-tyrosine kinase inhibitors,EGFR-TKIs)的开发已成为肿瘤治疗领域的热点。EGFR-TKIs分为可逆性EGFR-TKIs和不可逆性EGFR-TKIs,可逆性EGFR-TKIs主要包括吉非替尼和厄洛替尼等已上市的药物,不可逆性EGFR-TKIs主要包括阿法替尼和一些正处于临床研究中的药物,如AZD9291、CO-1686和HM61713等。本文对EGFRTKIs的研究进展进行了综述,为非小细胞肺癌临床治疗的药物选择提供参考。

Epidermal growth factor receptor（EGFR）, a receptor on membrane surface, is over expressed in non-small cell lung cancer with tyrosine kinase activity. It plays an important role in proliferation, metastasis, metabolism, differentiation and survival of cells. Currently, the development of epidermal growth factor receptor-tyrosine kinase inhibitors（EGFR-TKIs） has become a hot topic in the field of tumor therapy. According to the reversibility of binding with EGFR, the EGFR-TKIs can be classified into reversible and irreversible EGFR-TKIs. Reversible EGFR-TKIs include gefitinib, erlotinib and some others which are available in the market. Irreversible EGFR-TKIs involve afatinib and some novel antineoplastics which are still in clinical trials, including AZD9291, CO-1686 and HM61713. In this work, some latest researches about the development of EGFR-TKIs were reviewed for provide some information to non-small cell lung cancer therapies in clinic.