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- Title
Inhibition of the CYP3A4-mediated metabolism and P-glycoprotein-mediated transport of the HIV-1 protease inhibitor saquinavir by grapefruit juice components.
- Authors
Eagling, V A; Profit, L; Back, D J
- Abstract
Cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (P-gp) are both expressed in the intestinal mucosa and present a barrier to oral drug delivery. CYP3A4 and P-gp share both overlapping tissue distribution and substrate specificity. Grapefruit juice interactions with CYP3A4 substrates are well documented and occur as a consequence of down regulation of intestinal CYP3A4. The aim of the present study was to screen grapefruit juice components against the CYP3A4-mediated metabolism and P-gp mediated transport of the HIV-1 protease inhibitor saquinavir.
- Publication
British journal of clinical pharmacology, 1999, Vol 48, Issue 4, p543
- ISSN
0306-5251
- Publication type
Journal Article
- DOI
10.1046/j.1365-2125.1999.00052.x