Heterotropic effects on drug-metabolizing enzyme activities: in vitro curiosity emerges as a clinically meaningful phenomenon (perhaps?)

Clinical Pharmacology and Therapeutics
R Scott Obach

Abstract

Alterations in cytochrome P4503A4 are the most frequent underlying cause of drug-drug interactions (DDIs). This enzyme exhibits some unusual behaviors; for example, it has been observed that certain inhibitors can affect some CYP3A4-catalyzed reactions more than others, even for the same substrate. This has been proposed to be due to the simultaneous binding of more than one ligand to the enzyme. This behavior has been frequently observed in vitro, but seldom are analogous effects evident in vivo.

References

Dec 14, 1999·British Journal of Clinical Pharmacology·K E KenworthyJ B Houston
Feb 28, 2003·The Journal of Pharmacology and Experimental Therapeutics·Ann-Charlotte EgnellScott Boyer
Jun 20, 2003·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Thorir D BjornssonUNKNOWN FDA Center for Drug Evaluation and Research (CDER)
Jul 20, 2004·The Journal of Biological Chemistry·Jason K YanoEric F Johnson
Sep 30, 2005·The Journal of Pharmacology and Experimental Therapeutics·R Scott ObachLarry M Tremaine
Jun 10, 2008·Current Drug Metabolism·Toshiro NiwaHiroshi Yamazaki

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