The present invention relates to pharmaceutical use of 4-quinazolone amide derivatives. Specifically, the present invention relates to a use of 4-quinazolone amide derivatives of general formula (I) and pharmaceutical compositions containing same, in the preparation of a medicament for the treatment of cancer, wherein the said cancer is cancer with drug resistance, preferably drug resistant to reversible inhibitor of EGFR, more preferably drug resistant to Gefitinib, Erlotinib or Lapatinib or wherein the said cancer carries EGFR mutation. And all substitutes of general formula (I) are defined as those in the specification.本發明涉及4-喹唑啉胺衍生物在醫藥上的應用。特別是,本發明涉及通式(I)所示的4-喹唑啉胺衍生物及含有該衍生物的醫藥組成物在製備治療癌症的藥物中的用途,該癌症為具有抗藥性的癌症,較佳為對EGFR的可逆抑制劑具有抗藥性的癌症,特別較佳為對吉非替尼、厄洛替尼或拉帕替尼具有抗藥性的癌症,或者所述癌症攜帶EGFR突變,其中通式(I)的各取代基同說明書中的定義相同。
