Okeke N Lance, Hicks Charles
Duke University Medical Center, Department of Hospital Medicine, Durham Regional Hospital, Durham, North Carolina, USA.
HIV AIDS (Auckl). 2011;3:81-92. doi: 10.2147/HIV.S13985. Epub 2011 Jul 15.
The development of multiple agents with potent antiretroviral activity against HIV has ushered in a new age of optimism in the management of patients infected with the virus. However, the viruses' dynamic ability to develop resistance against these agents necessitates the investigation of novel targets for viral suppression. Raltegravir represents a first-in-class agent targeting the HIV integrase enzyme, which is responsible for integration of virally encoded DNA into the host genome. Over the last 5 years, clinical trials data has demonstrated an increasing role for raltegravir in the management of both treatment-experienced and treatment-naïve HIV-1-infected patients. This review focuses on the evidence supporting raltegravir's efficacy in an array of clinical settings. Other HIV-1 integrase inhibitors in development are also briefly discussed.
多种具有强效抗HIV病毒活性的药物的研发,为感染该病毒患者的治疗带来了新的乐观时代。然而,病毒对这些药物产生耐药性的动态能力,使得有必要研究新的病毒抑制靶点。拉替拉韦是靶向HIV整合酶的一流药物,该酶负责将病毒编码的DNA整合到宿主基因组中。在过去5年中,临床试验数据表明,拉替拉韦在治疗经验丰富和初治的HIV-1感染患者的管理中发挥着越来越重要的作用。本综述重点关注支持拉替拉韦在一系列临床环境中疗效的证据。还简要讨论了其他正在研发的HIV-1整合酶抑制剂。