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AFATINIB.pdf
阿法替尼是一种EGFR/HER2激酶抑制剂,用于治疗转移性非小细胞肺癌。推荐剂量为每次口服40 mg,每日1次;本文包含销量,化合物、组合物和适应症专利等信息;还收录了1条原研路线,4条创新型化学合成路线;其共价键和EGFR激酶结合,不可逆地抑制酪氨酸激酶自体磷酸化HER1 (IC50 = 0.5 nM),HER2 (IC50 = 14 nM)和HER4 (IC50 = 1 nM);在小型猪中的生物利用度(F%)为11.2%;小鼠和大鼠的MTD均为30 mg/kg。

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