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学科主题物理化学
The inhibition of noscapine to CYP3A4 and CYP2C9: explanation for clinical DDI between noscapine and warfarin
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
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
页码150/1
部门归属十八室
主办者AllChemie Inc.
英文摘要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
WOS记录号WOS:000280165300137
引用统计
文献类型会议论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/113512
专题中国科学院大连化学物理研究所
通讯作者Yang L(杨凌)
推荐引用方式
GB/T 7714
Fang ZZ,Yang L. The inhibition of noscapine to CYP3A4 and CYP2C9: explanation for clinical DDI between noscapine and warfarin[C],2009:150/1.
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