Pharmacokinetic-Pharmacodynamic Consequences and Clinical Relevance of Cytochrome P450 3A4 Inhibition

By G. Dresser, J. Spence, D. Bailey. Clinical Pharmacokinetics, 2000

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Clinical pharmacokinetics and metabolism of irinotecan (CPT-11). (2001, background): “The recognition that CPT-11 is a CYP3A substrate is an important finding, because it makes this agent subject to a host of enzyme-mediated drug interactions, even with commonly prescribed comedication (81, 87).”
Review of the flavonoids quercetin, hesperetin, and naringenin. Dietary sources, bioactivities, bioavailability, and epidemiology (2004, background): “The considerable increase in plasma concentrations of many drugs metabolized by intestinal cytochrome P-450 IIIA (CYP3A4) when administered concominantly with grapefruit juice is well documented and is of clinical relevance [67,68].”
Species differences between mouse, rat, dog, monkey and human CYP-mediated drug metabolism, inhibition and induction (2006, background): “CYP3A4 and its related -3A5 are the most abundant CYP isoforms in human liver, and are involved in the biotransformation of the majority of drugs [183].”