Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2020 Nov;94(11):3671-3722.
doi: 10.1007/s00204-020-02936-7. Epub 2020 Oct 27.

Inhibition and induction of CYP enzymes in humans: an update

Jukka Hakkola  1   2   3 , Janne Hukkanen  2   4 , Miia Turpeinen  1   5 , Olavi Pelkonen  6
Affiliations
Review

Inhibition and induction of CYP enzymes in humans: an update

Jukka Hakkola et al. Arch Toxicol. 2020 Nov.

Abstract

The cytochrome P450 (CYP) enzyme family is the most important enzyme system catalyzing the phase 1 metabolism of pharmaceuticals and other xenobiotics such as herbal remedies and toxic compounds in the environment. The inhibition and induction of CYPs are major mechanisms causing pharmacokinetic drug-drug interactions. This review presents a comprehensive update on the inhibitors and inducers of the specific CYP enzymes in humans. The focus is on the more recent human in vitro and in vivo findings since the publication of our previous review on this topic in 2008. In addition to the general presentation of inhibitory drugs and inducers of human CYP enzymes by drugs, herbal remedies, and toxic compounds, an in-depth view on tyrosine-kinase inhibitors and antiretroviral HIV medications as victims and perpetrators of drug-drug interactions is provided as examples of the current trends in the field. Also, a concise overview of the mechanisms of CYP induction is presented to aid the understanding of the induction phenomena.

Keywords: Cytochrome P450; Drug–drug interaction; Environmental toxicants; Herbal remedies; Induction; Inhibition.

PubMed Disclaimer

Conflict of interest statement

The authors declare that they have no conflict of interest.

References

    1. Abbas R, Hsyu P. Clinical pharmacokinetics and pharmacodynamics of bosutinib. Clin Pharmacokinet. 2016;55:1191–1204. - PubMed
    1. Abbas R, Leister C, El Gaaloul M, Chalon S, Sonnichsen D. Ascending single-dose study of the safety profile, tolerability, and pharmacokinetics of bosutinib coadministered with ketoconazole to healthy adult subjects. Clin Ther. 2012;34:2011–2019.e1. - PubMed
    1. Abbas R, Boni J, Sonnichsen D. Effect of rifampin on the pharmacokinetics of bosutinib, a dual Src/Abl tyrosine kinase inhibitor, when administered concomitantly to healthy subjects. Drug Metab Pers Ther. 2015;30:57–63. - PubMed
    1. Abel S, Back DJ, Vourvahis M. Maraviroc: pharmacokinetics and drug interactions. Antivir Ther (Lond) 2009;14:607–618. - PubMed
    1. Abraham K, Geusau A, Tosun Y, Helge H, Bauer S, Brockmoller J. Severe 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) intoxication: insights into the measurement of hepatic cytochrome P450 1A2 induction. Clin Pharmacol Ther. 2002;72:163–174. - PubMed

Publication types

MeSH terms

LinkOut - more resources