Impact of CYP3A4 and P-glycoprotein on drug disposition in intestine

Abstract

Abstract: Intestinal CYP3A4-mediated biotransformation and active efflux of absorbed drug by P-glycoprotein are major determinants of bioavailability of orally administered drugs. The expression of CYP3A4 and P-glycoprotein in the intestine is not co-ordinately regulated. However, synergistic actions of CYP3A4 and P-glycoprotein in intestinal drug disposition have been confirmed by in vitro and animal studies. Further understanding of this interaction would be potentially useful to improve oral bioavailability of CYP3A4 /-glycoprotein substrates.

Key words: CYP3A4, P-glycoprotein, drug metabolism, intestine, liver, first-pass metabolism, bioavailability, drug interaction

CLC Number:

R969.1

XIN Hua-wen. Impact of CYP3A4 and P-glycoprotein on drug disposition in intestine[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2005, 10(7): 721-725.

References

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