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学科主题: 物理化学
题名: The inhibition of noscapine to CYP3A4 and CYP2C9: explanation for clinical DDI between noscapine and warfarin
作者: Fang ZZ(房中则) ;  Yang L(杨凌)
会议名称: International Society for the Study of Xenobiotics
会议日期: 2009-10-18
出版日期: 2009-10-18
会议地点: 美国
其他题名: 那可丁对CYP3A4和CYP2C9的抑制:解释了临床上那可丁和华法林之间产生的药物-药物相互作用
通讯作者: 杨凌
部门归属: 十八室
主办者: AllChemie Inc.
摘要: Abstract: Noscapine, a naturally occurring phthalideisoquinoline alkaloid isolated from opium, has been used as an antitussive drug for more than 30 years. Recently, noscapine is drawing more and more attention as a promising chemotherapeutic agent. However, drug-drug interactions between noscapine and warfarin reported to Swedish adverse drug interaction register (SWEDIS) make researchers worry about its future application to treat cancer. Therefore, clarification of mechanism of drug-drug interaction between noscapine and warfarin is important and necessary. In this study, the inhibition of noscapine to seven CYP isoforms was investigated and the results demonstrated that noscapine strongly inhibited the activity of CYP3A4 and CYP2C9 with both reversible inhibition and time-dependent inhibition type. The kinetic parameters of reversible inhibition (Ki) are 5.2 μM and 8.82 μM for CYP3A4 and CYP2C9, respectively. The results also displayed that the inactivation kinetic parameters (KI and kinact) are 9.3 μM and 0.06 min-1 for CYP3A4, 8.9 μM and 0.014 min-1for CYP2C9. According to the reversible inhibition prediction equation, the value of AUCi/AUC is 1.05 and1.33 for oral administration and intravenous influsion, repectively; While Employing the TDI prediction equation, the value of AUCi/AUC is 2.95 and 7.51 for oral administration and intravenous influsion, respectively. In conclusion, significant increase in AUC of warfarin when coadministrated with noscapine clearly explained the clinical DDI between noscapine and warfarin. Our results also reminded cancer researchers of potential weakness of noscapine which benefits its future application as a chemotherapy agent.
语种: 中文
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内容类型: 会议论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/113512
Appears in Collections:中国科学院大连化学物理研究所_会议论文

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Recommended Citation:
Fang ZZ,Yang L. The inhibition of noscapine to CYP3A4 and CYP2C9: explanation for clinical DDI between noscapine and warfarin[C]. 见:International Society for the Study of Xenobiotics. 美国. 2009-10-18.
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