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长效抗逆转录病毒药物:我们现在处于什么阶段?

Long-Acting Antiretrovirals: Where Are We now?

作者信息

Nyaku Amesika N, Kelly Sean G, Taiwo Babafemi O

机构信息

Division of Infectious Diseases, Department of Medicine, Rutgers-New Jersey Medical School, Newark, NJ, USA.

Division of Infectious Diseases, Department of Medicine, Vanderbilt University, Nashville, TN, USA.

出版信息

Curr HIV/AIDS Rep. 2017 Apr;14(2):63-71. doi: 10.1007/s11904-017-0353-0.

DOI:10.1007/s11904-017-0353-0
PMID:28303548
Abstract

PURPOSE OF REVIEW

Current HIV treatment options require daily use of combination antiretroviral drugs. Many persons living with HIV experience treatment fatigue and suboptimal adherence as a result. Long-acting antiretroviral drugs are being developed to expand options for HIV treatment. Here, we review the agents in development, and evaluate data from recent clinical trials. In addition, we anticipate challenges to successful widespread use of long-acting antiretrovirals.

RECENT FINDINGS

Parenteral nanosuspensions of cabotegravir and rilpivirine, and dapivirine vaginal ring are the farthest in clinical development. Long-acting modalities in earlier development stages employ drug-loaded implants, microparticles, or targeted mutagenesis, among other innovations. Long-acting antiretroviral drugs promise new options for HIV prevention and treatment, and ways to address poor adherence and treatment fatigue. Further studies will identify the long-acting agents or combinations that are suitable for routine use. Creative solutions will be needed for anticipated implementation challenges.

摘要

综述目的

目前的艾滋病病毒治疗方案需要每日服用抗逆转录病毒药物组合。因此,许多艾滋病病毒感染者会出现治疗疲劳和依从性欠佳的情况。长效抗逆转录病毒药物正在研发中,以扩大艾滋病病毒的治疗选择。在此,我们综述正在研发的药物,并评估近期临床试验的数据。此外,我们预测长效抗逆转录病毒药物成功广泛应用所面临的挑战。

最新发现

卡博特韦和利匹韦林的肠胃外纳米混悬液以及达匹韦林阴道环在临床研发方面进展最远。处于早期研发阶段的长效剂型采用了载药植入物、微粒或靶向诱变等创新方法。长效抗逆转录病毒药物有望为艾滋病病毒的预防和治疗提供新的选择,以及解决依从性差和治疗疲劳问题的方法。进一步的研究将确定适合常规使用的长效药物或药物组合。对于预期的实施挑战,将需要创造性的解决方案。

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A long-acting formulation of the integrase inhibitor raltegravir protects humanized BLT mice from repeated high-dose vaginal HIV challenges.整合酶抑制剂拉替拉韦的长效制剂可保护人源化BLT小鼠免受反复高剂量阴道HIV攻击。
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Safety and Efficacy of Long-Acting Injectable Agents for HIV-1: Systematic Review and Meta-Analysis.长效注射抗 HIV-1 药物的安全性和疗效:系统评价和荟萃分析。
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