Royal Liverpool & Broadgreen University Hospital Trust, NIHR Biomedical Research Centre, Liverpool, UK.
Expert Opin Drug Metab Toxicol. 2010 Dec;6(12):1575-85. doi: 10.1517/17425255.2010.535811.
successful long-term treatment of HIV is hindered by development of resistance and providing active regimens for treatment-experienced patients remains challenging. Development of antiretrovirals active against resistant virus, such as the diarylpyrimidine non-nucleoside reverse transcriptase inhibitor (NNRTI) etravirine, is important to broaden treatment options to patients who have few available.
we summarise pharmacology, pharmacokinetics, drug-drug interactions and clinical data of etravirine based on a PubMed search between 01 January 2003 and 01 September 2010 as well as relevant information from conference proceedings and the latest Summary of Product Characteristics and US Prescribing Information.
the reader will gain a comprehensive overview of etravirine clinical pharmacology, drug-drug interactions and mechanism of action. Information regarding efficacy, safety and tolerability in specific patients groups is provided to allow the reader to form an opinion regarding the role of etravirine in clinical practice.
etravirine, along with other new antiretrovirals, has widened treatment options for patients with multi-drug resistance. Etravirine is well tolerated with the majority of drug-drug interactions manageable and is effective in triple-class experienced patients. Clinical studies investigating etravirine in treatment-naive patients are ongoing to further clarify its safety and resistance profile.
成功的长期治疗艾滋病的发展受到阻碍的抗药性和提供积极的方案治疗经验丰富的患者仍然具有挑战性。开发抗艾滋病病毒的药物，如 diarylpyrimidine 非核苷类逆转录酶抑制剂（NNRTI）依曲韦林，是重要的，以扩大治疗选择的患者有几个可用。
我们总结了依曲韦林的药理学、药代动力学、药物相互作用和临床数据，检索时间为 2003 年 1 月 1 日至 2010 年 9 月 1 日，基于 PubMed 的研究，以及会议记录和最新的产品特性概要和美国处方信息中的相关信息。
读者将获得一个全面的概述依曲韦林的临床药理学，药物相互作用和作用机制。关于疗效，安全性和耐受性在特定的患者群体的信息，以允许读者形成一个关于依曲韦林在临床实践中的作用的意见。
依曲韦林与其他新的抗逆转录病毒药物一起，为多药耐药患者扩大了治疗选择。依曲韦林具有良好的耐受性，大多数药物相互作用是可以管理的，并且在三药经验丰富的患者中是有效的。正在进行临床试验，研究依曲韦林在治疗初治患者中的安全性和耐药性，以进一步阐明其安全性和耐药性特征。
