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

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Vishnuvardhan D, Moltke LL, Richert C, Greenblatt DJ

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

AIDS. 2003 May 2;17(7):1092-4.

PubMed ID

12700464 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Drug Transporters

Drug	Transporter	Kind	Organism	Pharmacological Action	Actions
Lopinavir	P-glycoprotein 1	Protein	Humans	Unknown	Inhibitor Inducer	Details

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Lopinavir	P-glycoprotein 1	IC 50 (nM)	1700	N/A	N/A	Details