Title : Inhibition of the CYP3A4-mediated metabolism and P-glycoprotein-mediated transport of the HIV-1 protease inhibitor saquinavir by grapefruit juice components.

Pub. Date : 1999 Oct

PMID : 10583025






3 Functional Relationships(s)
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1 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. Saquinavir phosphoglycolate phosphatase Homo sapiens
2 These compounds were also screened as modulators of P-gp activity by assessing the directional transport of saquinavir across Caco-2 cell monolayers which express P-gp. Saquinavir phosphoglycolate phosphatase Homo sapiens
3 CONCLUSIONS: Grapefruit juice components inhibit CYP3A4-mediated saquinavir metabolism and also modulate, to a limited extent, P-gp mediated saquinavir transport in Caco-2 cell monolayers. Saquinavir phosphoglycolate phosphatase Homo sapiens