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

页码：1282 / 1284

页数：3

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