Interaction Potential of Etravirine with Drug Transporters Assessed In Vitro

被引：29
|
作者：
Zembruski, Nadine Cecile Luise [1 ]
Haefeli, Walter Emil [1 ]
Weiss, Johanna [1 ]
机构：
[1] Univ Heidelberg Hosp, Dept Clin Pharmacol & Pharmacoepidemiol, D-69120 Heidelberg, Germany
来源：
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY | 2011年 / 55卷 / 03期
关键词：
MULTIDRUG-RESISTANCE PROTEIN-2; P-GLYCOPROTEIN; PROTEASE INHIBITORS; PHARMACOKINETICS; ATAZANAVIR; RITONAVIR; BLOCKERS; RECEPTOR; TMC125; CELLS;
D O I：
10.1128/AAC.01527-10
中图分类号：
Q93 [微生物学];
学科分类号：
071005 ; 100705 ;
摘要：
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.
引用
收藏
页码：1282 / 1284
页数：3
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