Induction of cytochrome P450 enzymes: a view on human in vivo findings

Abstract

The induction of drug-metabolizing enzymes is a special case of pharmacokinetic interactions with consequences for the concurrent drug therapy. The most important enzymes affecting the pharmacokinetics of pharmaceuticals are cytochrome P450 (CYP) enzymes and their induction is often of utmost importance for the effects of the metabolized drugs. This review presents the current knowledge on the inducers of the specific CYP enzymes in humans. The focus is solely on human in vivo findings; in vitro results are referenced only when needed to interpret the induction mechanisms. As the mechanisms of CYP induction are important in understanding the effects of inducers, a concise overview of the various receptors affecting the induction of human CYP enzymes is presented.

Keywords::

• aryl hydrocarbon receptor
• constitutive androstane receptor
• cytochrome P450
• estrogen receptor
• glucocorticoid receptor
• induction
• pharmacokinetics
• pregnane X receptor
• retinoid X receptor

Financial & competing interests disclosure

The author has no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

No writing assistance was utilized in the production of this manuscript.