In vitro inhibitory effects of herbal supplements on tamoxifen and irinotecan metabolism
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Fran Grappe
Abstract
Background: As the use of herbal supplements continues to rise throughout the world, the potential for drug-herbal interactions also increases. For chemotherapeutic prodrugs, this interaction could prevent the metabolic conversion of the prodrug to its active metabolite(s), thereby potentially resulting in subtherapeutic systemic exposure of the drug and reduced efficacy of the therapy.
Methods: In this study, in vitro metabolism with human liver microsomes is used to measure the impact of ten commonly used herbal supplements on the biotransformation of the chemotherapeutic prodrugs tamoxifen (TAM) and irinotecan (IR).
Results: Four of the herbals tested, echinacea, ginseng, lemon balm, and skullcap, were found to be strong inhibitors of the CYP450 enzymatic bioactivation pathways of TAM with IC50 values as percent of a single dose ranging from 0.019% to 0.34%. Two of the herbals, skullcap and lemon balm, were found to inhibit the carboxyesterase pathway of IR with values of 0.21 and 0.25, respectively.
Conclusions: Our data suggests that based on the measured IC50 values that skullcap and lemon balm could have potential negative clinical impact on the bioactivation of TAM but not likely with IR.
Conflict of interest statement
Authors’ conflict of interest disclosure: The authors stated that there are no conflicts of interest regarding the publication of this article.
Research funding: None declared.
Employment or leadership: None declared.
Honorarium: None declared.
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©2014 by De Gruyter
Artikel in diesem Heft
- Frontmatter
- Editorial
- CYP 2C19 and UDP-glucuronosyltransferases not only for drugs but also for endobiotics
- Review
- Molecular functionality of CYP2C9 polymorphisms and their influence on drug therapy
- Reviews in Population Pharmacogenomics
- Pharmacogenetics in Jewish populations
- Frequency of CYP450 enzyme gene polymorphisms in the Greek population: review of the literature, original findings and clinical significance
- Original Articles
- Inhibition of OATP-1B1 and OATP-1B3 by tyrosine kinase inhibitors
- Effect of silymarin pretreatment on the bioavailability of domperidone in healthy human volunteers
- In vitro inhibitory effects of herbal supplements on tamoxifen and irinotecan metabolism
- Acknowledgment
- Acknowledgment
Artikel in diesem Heft
- Frontmatter
- Editorial
- CYP 2C19 and UDP-glucuronosyltransferases not only for drugs but also for endobiotics
- Review
- Molecular functionality of CYP2C9 polymorphisms and their influence on drug therapy
- Reviews in Population Pharmacogenomics
- Pharmacogenetics in Jewish populations
- Frequency of CYP450 enzyme gene polymorphisms in the Greek population: review of the literature, original findings and clinical significance
- Original Articles
- Inhibition of OATP-1B1 and OATP-1B3 by tyrosine kinase inhibitors
- Effect of silymarin pretreatment on the bioavailability of domperidone in healthy human volunteers
- In vitro inhibitory effects of herbal supplements on tamoxifen and irinotecan metabolism
- Acknowledgment
- Acknowledgment
