Department of Clinical Pharmacology and Pharmacoepidemiology, University Hospital Heidelberg, Im Neuenheimer Feld 410, 69120 Heidelberg, Germany.
Antimicrob Agents Chemother. 2011 Mar;55(3):1282-4. doi: 10.1128/AAC.01527-10. Epub 2010 Dec 28.
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.
依曲韦林是一种新型的非核苷类逆转录酶抑制剂（NNRTI），用于治疗 HIV-1 感染。ABC 转运蛋白可能介导临床上相关的药物相互作用。我们评估了依曲韦林对 ABC 转运蛋白的底物特性、抑制和诱导潜力。依曲韦林不抑制 P-糖蛋白/ABCB1，也不被测试的 ABC 转运蛋白转运，但它是 BCRP/ABCG2 的有效抑制剂。依曲韦林诱导了几种 ABC 转运蛋白，特别是 BCRP/ABCG2。这些数据表明，依曲韦林通过调节几种 ABC 转运蛋白的表达和功能，具有发生药物相互作用的潜力。
