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

Daesety Vishnuvardhan, Lisa L Moltke, Clemens Richert, David J Greenblatt

Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA.

AIDS (London, England) 2003 May 2

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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 (IC50 1.7 microM). 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.

Citation

Daesety Vishnuvardhan, Lisa L Moltke, Clemens Richert, David J Greenblatt. Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein. AIDS (London, England). 2003 May 2;17(7):1092-4