Interaction potential of etravirine with drug transporters assessed in vitro.

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.

• Authors: Nadine Cécile Luise Zembruski, Walter Emil Haefeli, Johanna Weiss
• Journal: Antimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 55 Issue 3 Pg. 1282-4 (Mar 2011) ISSN: 1098-6596 [Electronic] United States
• PMID: 21189339 (Publication Type: Journal Article)

Chemical References

• ABCB1 protein, human
• ABCG2 protein, human
• ATP Binding Cassette Transporter, Subfamily B
• ATP Binding Cassette Transporter, Subfamily B, Member 1
• ATP Binding Cassette Transporter, Subfamily G, Member 2
• ATP-Binding Cassette Transporters
• Neoplasm Proteins
• Nitriles
• Pyridazines
• Pyrimidines
• Reverse Transcriptase Inhibitors
• etravirine

Topics

• ATP Binding Cassette Transporter, Subfamily B
• ATP Binding Cassette Transporter, Subfamily B, Member 1 (antagonists & inhibitors)
• ATP Binding Cassette Transporter, Subfamily G, Member 2
• ATP-Binding Cassette Transporters (antagonists & inhibitors)
• Animals
• Biological Transport (drug effects)
• Blotting, Western
• Cell Line
• Cell Line, Tumor
• Cell Proliferation
• Dogs
• Humans
• Neoplasm Proteins (antagonists & inhibitors)
• Nitriles
• Pyridazines (adverse effects)
• Pyrimidines
• Reverse Transcriptase Inhibitors (adverse effects)