| Literature DB >> 22617226 |
L Binkhorst1, T van Gelder, W J Loos, F E de Jongh, P Hamberg, I M Ghobadi Moghaddam-Helmantel, E de Jonge, A Jager, C Seynaeve, R H N van Schaik, J Verweij, R H J Mathijssen.
Abstract
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.Entities:
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Year: 2012 PMID: 22617226 DOI: 10.1038/clpt.2011.372
Source DB: PubMed Journal: Clin Pharmacol Ther ISSN: 0009-9236 Impact factor: 6.875