Interaction potential of etravirine with drug transporters assessed in vitro
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 tr...
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| Main Authors: | , , |
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| Format: | Article (Journal) |
| Language: | English |
| Published: |
February 24, 2011
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| In: |
Antimicrobial agents and chemotherapy
Year: 2011, Volume: 55, Issue: 3, Pages: 1282-1284 |
| ISSN: | 1098-6596 |
| DOI: | 10.1128/AAC.01527-10 |
| Online Access: | Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1128/AAC.01527-10 Verlag, lizenzpflichtig, Volltext: https://journals.asm.org/doi/10.1128/AAC.01527-10 
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| Author Notes: | Nadine Cécile Luise Zembruski, Walter Emil Haefeli, and Johanna Weiss |
| Summary: | 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. |
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| Item Description: | Gesehen am 22.12.2022 |
| Physical Description: | Online Resource |
| ISSN: | 1098-6596 |
| DOI: | 10.1128/AAC.01527-10 |