Afatinib (maleate)

EGFR和ErbB2抑制剂（IC50分别为0.5和14nM）；在过表达P-糖蛋白的多药耐药A549T肺癌细胞中以浓度依赖性方式增加阿霉素的细胞毒性；在20mg/kg剂量下降低ErbB2扩增的NCI-N87和NUGC4胃癌小鼠异种移植模型中的肿瘤生长。An inhibitor of EGFR and ErbB2 (IC50s = 0.5 and 14 nM, respectively); increases the cytotoxicity of adriamycin in a concentration-dependent manner in multidrug-resistant A549T lung cancer cells overexpressing P-glycoprotein; reduces tumor growth in ErbB2-amplified NCI-N87 and NUGC4 gastric cancer mouse xenograft models at 20 mg/kg.