islatravir在HIV治疗和预防中的作用:最新进展。

IF 4.5 3区 医学 Q2 IMMUNOLOGY
Abdallah Derbalah, Hayley Christine Karpick, Holly Maize, Preston Skersick, Mackenzie Cottrell, Gauri G Rao
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引用次数: 0

摘要

综述的目的:总结islatravir在HIV治疗和预防中的潜在作用的最新进展。最近发现:Islatravir是一种正在研究的抗逆转录病毒药物,具有独特的药理学特性,有利于灵活的给药方案。当与多拉韦林和拉米夫定联合使用时,Islatravir已显示出强大的抗病毒活性和对耐药性的高屏障。一种简化的双药HIV治疗方案islatravir联合doravirine也显示出与标准的三药治疗方案相当的疗效。islatravir活性代谢物的长半衰期和高效力可能支持其作为HIV暴露前预防(PrEP)的长效选择。每月口服一次依拉他韦可在整个给药间隔内维持其活性代谢物的有效浓度。此外,一种试验性的可植入制剂预计将提供至少一年的有效浓度,并在阴道和直肠组织中表现出相当的分布,使其成为男性和女性个体的有前途的PrEP选择。Islatravir具有最小的药物相互作用风险,因为它不是主要药物代谢物和转运体的底物、诱导剂或抑制剂。最后,临床试验表明,islatravir具有良好的安全性,仅显示轻微和短暂的不良事件。摘要:利用islatravir独特的药理学特性为简化HIV治疗方案和长效PrEP提供了机会,使其成为抗逆转录病毒武器库的宝贵补充。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Role of islatravir in HIV treatment and prevention: an update.

Purpose of review: To summarize recent updates on the potential role of islatravir for HIV treatment and prevention.

Recent findings: Islatravir is an investigational antiretroviral agent with unique pharmacologic properties that facilitate flexible dosing regimens. Islatravir has demonstrated potent antiviral activity and a high barrier to resistance when combined with doravirine and lamivudine. A simplified two-drug HIV treatment regimen of islatravir combined with doravirine has also demonstrated comparable efficacy to standard of care three-drug regimens. The long half-life and high potency of islatravir's active metabolite may support its use as a long-acting option for HIV preexposure prophylaxis (PrEP). A once monthly oral dose of islatravir maintains effective concentrations of its active metabolite over the entire dosing interval. Furthermore, an investigational implantable formulation has been projected to provide efficacious concentrations for at least a year and exhibits comparable distribution into vaginal and rectal tissues making it a promising PrEP option for male and female individuals. Islatravir has minimal risks of drug interactions as it is not a substrate, inducer, or inhibitor of major drug metabolizers and transporters. Finally, clinical trials demonstrate islatravir's favorable safety profile revealing only mild and transient adverse events.

Summary: Leveraging the unique pharmacological properties of islatravir offers opportunities for simplified HIV treatment regimens and long-acting PrEP making it a valuable addition to the antiretroviral arsenal.

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来源期刊
Current Opinion in HIV and AIDS
Current Opinion in HIV and AIDS IMMUNOLOGY-INFECTIOUS DISEASES
CiteScore
7.40
自引率
7.30%
发文量
115
审稿时长
6-12 weeks
期刊介绍: Published bimonthly and offering a unique and wide ranging perspective on the key developments in the field, each issue of Current Opinion in HIV and AIDS features hand-picked review articles from our team of expert editors. With six disciplines published across the year – including HIV and ageing, a HIV vaccine, and epidemiology – every issue also contains annotated reference detailing the merits of the most important papers.
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