2. Academic Validation
  3. Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein

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

  • AIDS. 2003 May 2;17(7):1092-4. doi: 10.1097/01.aids.0000060380.78202.b5.
Daesety Vishnuvardhan 1,  Lisa L Moltke,  Clemens Richert,  David J Greenblatt
Affiliations

Affiliation

  • 1 Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA.
PMID: 12700464 DOI: 10.1097/01.aids.0000060380.78202.b5
Abstract

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.

Figures