【摘 要】
：
Compared to traditional cytotoxic agents, gefitinib, an orally available EGFR tyrosine kinase inhibitors, can prolong survival of NSCLC patients and cause f
【机 构】
：
Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics,Chinese Academ
【出 处】
：
2015年第一届药代动力学朝阳论坛
论文部分内容阅读
Compared to traditional cytotoxic agents, gefitinib, an orally available EGFR tyrosine kinase inhibitors, can prolong survival of NSCLC patients and cause few drug adverse events.However, further investigation showed P450 1A1 could metabolize gefitinib to reactive intermediate in lung microsome of smokers, and gefitinib-induced ILD easier occurred in smokers, the CYP1A1 of those patients were greatly induced by tobacco smoke, which implicated that the bioactivation of gefitinib by CYP1A1 may related to gefitinib-induced ILD.To our knowledge, no further study has been conducted to identify the role of bioactivation by CYP1A1 in the cytotoxic effects of gefitinib and the mechanisms of toxicity.In our study, we first established an in vitro cell culture model with CYP1A1 inducer.
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