Department of Pharmaceutical and Pharmacological Sciences, Laboratory for Molecular Virology and Gene Therapy, Herestraat 49, 3000 KU Leuven, Belgium.
Expert Opin Pharmacother. 2013 Jun;14(8):1087-96. doi: 10.1517/14656566.2013.787411. Epub 2013 Apr 8.
Etravirine (TMC125) is an orally administered second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) that is approved in treatment-experienced patients as addition to an optimized background therapy (OBT).
A Medline search was conducted of Phase II - IV clinical trials, as well as a review of abstracts from major HIV and infectious disease conferences from 2010 - 2013, involving etravirine.
Etravirine is a well-tolerated NNRTI with a good safety profile and a higher genetic barrier for resistance compared to first-generation NNRTIs. Rash is a potential side effect but remains mostly mild to moderate. The necessity of taking it twice daily with food (200 mg bid.), potential pharmacokinetic interactions and low concentrations in the central nervous system (CNS) represent limitations. The efficacy of once daily etravirine (400 mg qid.) and the use in treatment modification/simplification strategies requires further research. Despite its favorable profile, etravirine is currently not sufficiently investigated nor approved for use in treatment-naïve patients which should be balanced against its potential as a backup NNRTI and the broad cross-resistance conferred by etravirine failure to other NNRTIs. Etravirine should be avoided following treatment failure with regimens containing rilpivirine, another second-generation NNRTI.
依曲韦林（TMC125）是一种口服的第二代非核苷类逆转录酶抑制剂（NNRTI），在优化背景治疗（OBT）的基础上，适用于经治患者。
对 II 期至 IV 期临床试验进行了 Medline 检索，同时还对 2010 年至 2013 年主要的 HIV 和传染病会议的摘要进行了综述，涉及依曲韦林。
依曲韦林是一种耐受性良好的 NNRTI，与第一代 NNRTIs 相比，具有更好的安全性和更高的耐药遗传屏障。皮疹是一种潜在的副作用，但大多为轻度至中度。需要每日两次随餐服用（200mg bid.），存在潜在的药代动力学相互作用和中枢神经系统（CNS）中的低浓度，这些都是其局限性。每日一次服用依曲韦林（400mg qid.）的疗效以及在治疗修改/简化策略中的应用需要进一步研究。尽管其作用良好，但依曲韦林目前尚未充分研究，也未获准用于初治患者，这需要平衡其作为后备 NNRTI 的潜力，以及依曲韦林失效对其他 NNRTIs 的广泛交叉耐药性。在含有利匹韦林（另一种第二代 NNRTI）的方案治疗失败后，应避免使用依曲韦林。
