选择性EGFR酪氨酸激酶抑制剂-吉非替尼

吉非替尼(Gefitinib,ZD1839,Iressa)是一种口服选择性表皮生长因子受体(EGFR)酪氨酸激酶抑制剂。表皮生长因子受体在一些类型的人类肿瘤细胞中存在过度表达,吉非替尼通过抑制表皮生长因子受体酪氨酸激酶的ATP结合位点发挥抗肿瘤作用。2003年5月经FDA批准上市,用于一线化疗失败的局部晚期或转移性非小细胞肺癌的治疗。

Gefitinib is an orally active, selective tyrosine kinase inhibitor of epidermal growth factor receptor（EGFR）. EGFR is overexpressed in the cells of certain types of human carcinomas. Gefitinib inhibits EGFR tyrosine by binding to the adenosine triphosphate （ATP）-bindingsite of the enzyme and then malignant cells are inhibited.And it was approved by FDA in May 2003. Gefitinib is currently only indicated for the treatment of locally advanced or metastatic non-small-cell-lung cancer （NSCLC） in patients who have previously received chemotherapy.