University of North Carolina Eshelman School of Pharmacy, Chapel Hill, North Carolina, USA.
Clin Pharmacol Ther. 2021 Apr;109(4):841-855. doi: 10.1002/cpt.2187. Epub 2021 Mar 5.
Despite significant advances in HIV treatment over the past 30 years, critical barriers to an HIV cure persist. The HIV reservoir, defined at both the cellular and anatomical level, constitutes the main barrier to cure. While the mechanisms underlying the reservoir are not yet well understood, one theory to explain persistence at the anatomical level is that subtherapeutic exposure to antiretroviral therapy (ART) within certain tissue compartments permits ongoing replication. Characterizing ART pharmacology throughout the body is important in the context of these potential pharmacologic sanctuaries and for maximizing the probability of success with forthcoming cure strategies that rely on latency reversal and require ART to prevent reseeding the reservoir. In this review, we provide a comprehensive overview of ART and latency reversal agent distribution at the site of action for HIV cure (i.e., anatomical sites commonly associated with HIV persistence, such as lymphoid organs and the central nervous system). We also discuss methodologic approaches that provide insight into HIV cure pharmacology, including experimental design and advances within the computational, pharmaceutical, and analytical chemistry fields. The information discussed in this review will assist in streamlining the development of investigational cure strategies by providing a roadmap to ensure therapeutic exposure within the site of action for HIV cure.
尽管在过去的 30 年中,HIV 治疗取得了重大进展,但治愈 HIV 的关键障碍仍然存在。HIV 储存库在细胞和解剖学水平上都有定义,是治愈的主要障碍。虽然储存库的机制尚未得到很好的理解,但一种解释解剖学水平上持续存在的理论是,抗逆转录病毒疗法 (ART) 在某些组织隔室中的亚治疗暴露允许持续复制。在这些潜在的药物避难所的背景下,以及在依赖潜伏期逆转和需要 ART 来防止储存库重新播种的即将到来的治愈策略中,最大限度地提高成功概率的情况下,全面描述整个身体的 ART 药理学非常重要。在这篇综述中,我们全面概述了 HIV 治愈作用部位的 ART 和潜伏逆转剂分布(即与 HIV 持续存在相关的常见解剖部位,如淋巴器官和中枢神经系统)。我们还讨论了提供 HIV 治愈药理学见解的方法学方法,包括实验设计以及计算化学、制药化学和分析化学领域的进展。本综述中讨论的信息将通过提供确保 HIV 治愈作用部位治疗暴露的路线图,协助简化研究性治愈策略的开发。