依曲韦林与药物转运体的体外相互作用研究。
Interaction potential of etravirine with drug transporters assessed in vitro.
机构信息
Department of Clinical Pharmacology and Pharmacoepidemiology, University Hospital Heidelberg, Im Neuenheimer Feld 410, 69120 Heidelberg, Germany.
出版信息
Antimicrob Agents Chemother. 2011 Mar;55(3):1282-4. doi: 10.1128/AAC.01527-10. Epub 2010 Dec 28.
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.
摘要
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。
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