Interaction potential of etravirine with drug transporters assessed in vitro

• Verfasst von: Zembruski, Nadine Cécile Luise [VerfasserIn]
• Verfasst von: Haefeli, Walter E. [VerfasserIn]
• Verfasst von: Weiß, Johanna [VerfasserIn]
• Titel: Interaction potential of etravirine with drug transporters assessed in vitro
• Verf.angabe: Nadine Cécile Luise Zembruski, Walter Emil Haefeli, and Johanna Weiss
• E-Jahr: 2011
• Jahr: February 24, 2011
• Umfang: 3 S.
• Fussnoten: Gesehen am 22.12.2022
• Titel Quelle: Enthalten in: Antimicrobial agents and chemotherapy
• Ort Quelle: Washington, DC : Soc., 1972
• Jahr Quelle: 2011
• Band/Heft Quelle: 55(2011), 3, Seite 1282-1284
• ISSN Quelle: 1098-6596
• DOI: doi:10.1128/AAC.01527-10
• Datenträger: Online-Ressource
• Sprache: eng
• K10plus-PPN: 1828335673

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.