Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein

Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein

The effect of lopinavir on P-glycoprotein-mediated rhodamine 123 efflux was studied in Caco-2 monolayer cells. Lopinavir is a potent inhibitor of Rh123 efflux in Caco-2 monolayers (IC sub(50) 1.7 mu M). Chronic lopinavir exposure (72 h) in LS 180V cells reduced the content of intracellular Rh123 by...

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Bibliographic Details
Published in:AIDS (London) Vol. 17; no. 7; pp. 1092 - 1094
Main Authors: Vishnuvardhan, D, von Moltke, LL, Richert, C, Greenblatt, D J
Format: Journal Article
Language:English
Published: 02-05-2003
Online Access:Get full text
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Summary:The effect of lopinavir on P-glycoprotein-mediated rhodamine 123 efflux was studied in Caco-2 monolayer cells. Lopinavir is a potent inhibitor of Rh123 efflux in Caco-2 monolayers (IC sub(50) 1.7 mu M). Chronic lopinavir exposure (72 h) in LS 180V cells reduced the content of intracellular Rh123 by approximately 50%, indicating increased efflux activity. In LS 180V cells, lopinavir induced P-glycoprotein immunoreactive protein (up to threefold) and messenger RNA levels in a concentration-dependent fashion.
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ISSN:0269-9370
DOI:10.1097/01.aids.0000060380.78202.b5