Department of Microbiology, School of Medicine, Tehran University of Medical Sciences, Tehran, Iran.
Department of Chemistry, Medicinal Chemistry Research Laboratory, Shiraz University of Technology, Shiraz, Iran.
Expert Rev Anti Infect Ther. 2022 Aug;20(8):1135-1147. doi: 10.1080/14787210.2022.2081153. Epub 2022 Jun 13.
The development of long-acting (LA) drugs has changed the management of common medical conditions for human replication immunodeficiency virus (HIV). Cabenuva (cabotegravir/Rilpivirine) is the first LA antiretroviral injectable drug composed of nano-formulation of cabotegravir (CAB) and rilpivirine (RPV).
In this review article, we aim to have a brief overview of results of major clinical trials that administrated Cabotegravir/Rilpivirine for patients considering the efficacy and safety profiles. Moreover, we discuss about CAB and RPV chemical structure, mechanism of action, activity against drug-sensitive and -resistant HIV, and pharmacodynamics/pharmacokinetics properties.
Based on the results of the ATLAS and FLAIR trials, Cabotegravir/Rilpivirine regimen once-monthly has shown equal effectivity to oral combination antiretroviral therapy (cART) in maintaining HIV-1 suppression in patients. Furthermore, ATLAS-2 M study revealed the non-inferiority of Cabotegravir/Rilpivirine regimen every 8 weeks compared to every 4 weeks. The injectable LA ART reduces the number of treatment intake as well as increases adherence, especially in patients with HIV-related stigma. Administration of extended-release agents probably minimize the risk of treatment-related toxicity and resistance related to sub-optimal adherence to oral ART, so Cabotegravir/Rilpivirine can be suggested as a suitable alternative for HIV infection control in current era.
长效（LA）药物的发展改变了人类复制免疫缺陷病毒（HIV）常见医疗条件的管理方式。卡布韦（卡替拉韦/利匹韦林）是第一种由卡替拉韦（CAB）和利匹韦林（RPV）纳米制剂组成的 LA 抗逆转录病毒注射药物。
在这篇综述文章中，我们旨在简要概述为考虑疗效和安全性概况的患者管理卡替拉韦/利匹韦林的主要临床试验结果。此外，我们讨论了 CAB 和 RPV 的化学结构、作用机制、对药物敏感和耐药 HIV 的活性以及药代动力学/药效学特性。
基于 ATLAS 和 FLAIR 试验的结果，卡替拉韦/利匹韦林方案每月一次与口服联合抗逆转录病毒疗法（cART）在维持 HIV-1 抑制方面具有同等效果。此外，ATLAS-2M 研究表明，卡替拉韦/利匹韦林方案每 8 周给药与每 4 周给药相比具有非劣效性。长效 LAART 减少了治疗摄入次数，并提高了依从性，尤其是在具有 HIV 相关耻辱感的患者中。延长释放制剂的给药可能最大限度地降低了与口服 ART 依从性不佳相关的治疗相关毒性和耐药性的风险，因此卡替拉韦/利匹韦林可以作为当前控制 HIV 感染的一种合适替代方案。
