三苯氧胺
药理学
CYP2D6型
利福平
细胞色素P450
药物相互作用
药物代谢
生物转化
药品
代谢物
新陈代谢
医学
化学
作者
Lisette Binkhorst,T. van Gelder,Walter J. Loos,F. E. de Jongh,P. Hamberg,I.M. Ghobadi Moghaddam-Helmantel,E. de Jonge,Agnes Jager,Caroline Seynaeve,R.H.N. van Schaik,Jaap Verweij,Ron H.J. Mathijssen
标识
DOI:10.1038/clpt.2011.372
摘要
Tamoxifen undergoes biotransformation into several metabolites, including endoxifen. Differences in metabolism contribute to the interindividual variability in endoxifen concentrations, potentially affecting treatment efficacy. We evaluated the effects of cytochrome P450 (CYP) induction by rifampicin on the exposure levels of tamoxifen and its metabolites and found that coadministration of rifampicin resulted in markedly reduced (up to 86%, P ≤ 0.040) concentrations of tamoxifen and its metabolites. Given the extensive metabolism undergone by tamoxifen, several factors may have contributed to this effect. Similar drug-drug interactions may exist between tamoxifen and other strong CYP inducers.
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