Department of Pharmacy Practice, Auburn University Harrison College of Pharmacy, Auburn, AL, USA.
Auburn University Harrison College of Pharmacy, Auburn, AL, USA.
Ann Pharmacother. 2023 Mar;57(3):306-316. doi: 10.1177/10600280221102532. Epub 2022 Jul 1.
Review the pharmacology, pharmacokinetics, efficacy, safety, and role of long-acting injectable cabotegravir (CAB-LA) in HIV preexposure prophylaxis (PrEP).
A literature search was performed using PubMed and Google Scholar (2012 to April 2022) with the search terms cabotegravir, preexposure prophylaxis, and PrEP. Other resources included abstracts presented at recent conferences, the manufacturer's Web site, prescribing information, and review articles.
All English-language articles of studies assessing the efficacy and safety of CAB-LA for PrEP were included.
CAB-LA is the first long-acting injectable therapy approved for HIV-1 PrEP in both men and women. It is a suspension given intramuscularly every other month. CAB-LA has been shown to be more effective than daily oral tenofovir disoproxil fumarate/emtricitabine (TDF/FTC) in preventing HIV-1 infection among high-risk individuals. Two phase 3 trials were stopped early on the basis of superior efficacy of CAB-LA. The most common adverse effects were injection site reactions (ISRs), although they tended to decrease over time, and few participants in clinical trials discontinued use due to ISRs.
CAB-LA may be particularly useful for individuals with known adherence problems to oral therapy, those with renal impairment, and those with decreased bone mineral density. However, CAB-LA is more expensive than generic TDF/FTC and may be associated with weight gain.
CAB-LA is the first long-acting injectable agent for HIV PrEP. It is more effective than oral TDF/FTC, is well-tolerated aside from ISRs, and has few clinically significant drug-drug interactions.
综述长效注射用卡替拉韦(CAB-LA)在 HIV 暴露前预防(PrEP)中的药理学、药代动力学、疗效、安全性和作用。
使用 PubMed 和 Google Scholar(2012 年至 2022 年 4 月)进行文献检索,检索词包括卡替拉韦、暴露前预防和 PrEP。其他资源包括最近会议上的摘要、制造商的网站、说明书和综述文章。
所有评估 CAB-LA 用于 PrEP 的疗效和安全性的英文文章均被纳入。
CAB-LA 是第一种批准用于男性和女性 HIV-1 PrEP 的长效注射治疗药物。它是一种每两个月肌肉注射一次的混悬剂。CAB-LA 已被证明在预防高危人群中的 HIV-1 感染方面比每日口服替诺福韦二吡呋酯/恩曲他滨(TDF/FTC)更有效。两项 3 期试验因 CAB-LA 的疗效优于 TDF/FTC 而提前终止。最常见的不良反应是注射部位反应(ISRs),尽管随着时间的推移,这些反应往往会减少,且临床试验中很少有参与者因 ISRs 而停止使用。
CAB-LA 可能对已知口服治疗依从性问题、肾功能损害和骨密度降低的患者特别有用。然而,CAB-LA 比 TDF/FTC 更昂贵,并且可能与体重增加有关。
CAB-LA 是第一个用于 HIV PrEP 的长效注射剂。它比口服 TDF/FTC 更有效,除了注射部位反应外,耐受性良好,且与药物相互作用相关的临床重要问题很少。