Interaction potential of etravirine with drug transporters assessed in vitro.

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Zembruski NC, Haefeli WE, Weiss J

Interaction potential of etravirine with drug transporters assessed in vitro.

Antimicrob Agents Chemother. 2011 Mar;55(3):1282-4. doi: 10.1128/AAC.01527-10. Epub 2010 Dec 28.

PubMed ID
21189339 [ View in PubMed
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Abstract

Etravirine is a novel nonnucleoside reverse transcriptase inhibitor (NNRTI) for the treatment of HIV-1 infections. ABC transporters potentially mediate clinically relevant drug-drug interactions. We assessed substrate characteristics and the inhibitory and inductive potential of etravirine on ABC transporters. Etravirine did not inhibit P-gp/ABCB1 and was not transported by the tested ABC transporters but was a potent inhibitor of BCRP/ABCG2. Etravirine induced several ABC transporters, especially BCRP/ABCG2. These data demonstrate that etravirine has the potential for drug-drug interactions by modulation of expression and function of several ABC transporters.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
EtravirineP-glycoprotein 1IC 50 (nM)7600N/AN/ADetails