Effects of CYP Induction by Rifampicin on Tamoxifen Exposure

被引：33

作者：

Binkhorst, L. ^{[1
,2
]}

van Gelder, T. ^{[2
]}

Loos, W. J. ^{[1
]}

de Jongh, F. E. ^{[3
]}

Hamberg, P. ^{[4
]}

Moghaddam-Helmantel, I. M. Ghobadi ^{[1
]}

de Jonge, E. ^{[5
]}

Jager, A. ^{[1
]}

Seynaeve, C. ^{[1
]}

van Schaik, R. H. N. ^{[5
]}

Verweij, J. ^{[1
]}

Mathijssen, R. H. J. ^{[1
]}

机构：

[1] Univ Med Ctr, Daniel den Hoed Canc Ctr, Erasmus MC, Dept Med Oncol, Rotterdam, Netherlands

[2] Univ Med Ctr, Dept Hosp Pharm, Erasmus MC, Rotterdam, Netherlands

[3] Ikazia Hosp, Dept Internal Med, Rotterdam, Netherlands

[4] St Franciscus Gasthuis, Dept Internal Med, Rotterdam, Netherlands

[5] Univ Med Ctr, Dept Clin Chem, Erasmus MC, Rotterdam, Netherlands

来源：

CLINICAL PHARMACOLOGY & THERAPEUTICS | 2012年 / 92卷 / 01期

关键词：

BREAST-CANCER; POSTMENOPAUSAL WOMEN; ESTROGEN-RECEPTOR; PHASE-I; GENOTYPE; METABOLITES; ENDOXIFEN; PLASMA; BIOTRANSFORMATION; INHIBITORS;

D O I：

10.1038/clpt.2011.372

中图分类号：

R9 [药学];

学科分类号：

1007 ;

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.

引用

页码：62 / 67

页数：6

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