Jayaweera Dushyantha T, Espinoza Luis, Castro Jose
University of Miami Miller School of Medicine, 1200 NW 195TH Street, Suite 857, Miami, FL 33136, USA.
Expert Opin Pharmacother. 2008 Dec;9(17):3083-94. doi: 10.1517/14656560802489569.
Etravirine is the first non-nucleoside reverse transcriptase inhibitor (NNRTI) to be active against human immunodeficiency virus with NNRTI mutations.
To understand the unique features of etravirine and to evaluate its safety, efficacy, and optimal use.
The structure and the mechanism of action of etravirine in blocking the reverse transcriptase enzyme and the preclinical, pharmacokinetic and pharmacodynamic studies were reviewed. The DUET Phase III clinical trials and the resistance profile of etravirine were evaluated.
Etravirine has unique activity against most HIV isolates that are resistant to other NNRTIs. Unlike other NNRTIs, it has a higher genetic barrier to developing high-grade resistance. In the DUET studies, etravirine demonstrated virological efficacy superior to the control arms with comparable rates of adverse events with the exception of rash. Because of its effect on the cytochrome P450 system, there are important drug interactions that will need to be taken into consideration with its use.
依曲韦林是首个对具有非核苷类逆转录酶抑制剂（NNRTI）突变的人类免疫缺陷病毒有效的非核苷类逆转录酶抑制剂。
了解依曲韦林的独特特性，并评估其安全性、疗效及最佳用法。
综述了依曲韦林在阻断逆转录酶方面的结构和作用机制，以及临床前、药代动力学和药效学研究。评估了DUET三期临床试验及依曲韦林的耐药情况。
依曲韦林对大多数对其他NNRTIs耐药的HIV分离株具有独特活性。与其他NNRTIs不同，它在产生高度耐药方面具有更高的遗传屏障。在DUET研究中，依曲韦林显示出优于对照组的病毒学疗效，除皮疹外，不良事件发生率相当。由于其对细胞色素P450系统的影响，使用时需要考虑重要的药物相互作用。
