Department of Infectious Diseases, IRCCS San Raffaele Scientific Institute, Milan, Italy.
Vita-Salute San Raffaele University, Milan, Italy.
Expert Rev Anti Infect Ther. 2023 Jul-Dec;21(11):1167-1176. doi: 10.1080/14787210.2023.2268281. Epub 2023 Nov 8.
Darunavir (DRV)/cobicistat (COBI)/emtricitabine (FTC)/tenofovir alafenamide (TAF) is the only protease inhibitor-based single-tablet regimen (STR) approved for the treatment of HIV infection of adults and pediatric patients weighing at least 40 kg. DRV/COBI/FTC/TAF has demonstrated to be an effective regimen, to have a high genetic barrier to resistance, and to be well tolerated.
The authors summarize the chemistry and pharmacology of DRV, COBI, FTC, and TAF and discuss trials conducted on antiretroviral therapy (ART)-naïve and -experienced people living with HIV designed to evaluate safety, tolerability, and efficacy of the STR. This work also reports studies comparing DRV/COBI/FTC/TAF with competitive agents in real-world settings.
Despite the availability of newer antiretroviral drugs and strategies in the management of HIV infection, including long-acting therapies, DRV/COBI/FTC/TAF is still considered an alternative regimen for the treatment of ART-naïve adults. DRV/COBI/FTC/TAF is an effective, well-tolerated, and safe antiretroviral regimen and represents a valid option for people who need to switch therapy due to tolerability issues, such as the onset of neuropsychiatric effects related to integrase strand transfer inhibitors, or virological failure.
达芦那韦(DRV)/考比司他(COBI)/恩曲他滨(FTC)/替诺福韦艾拉酚胺(TAF)是唯一获批用于治疗成人和体重至少 40kg 的儿科 HIV 感染者的基于蛋白酶抑制剂的单片复方制剂(STR)。DRV/COBI/FTC/TAF 已被证明是一种有效的方案,具有较高的耐药基因屏障,且耐受性良好。
作者总结了 DRV、COBI、FTC 和 TAF 的化学和药理学,并讨论了针对初治和经治 HIV 感染者进行的抗逆转录病毒治疗(ART)试验,旨在评估 STR 的安全性、耐受性和疗效。本研究还报告了在真实环境中比较 DRV/COBI/FTC/TAF 与竞争药物的研究。
尽管在 HIV 感染管理中可应用更新的抗逆转录病毒药物和策略,包括长效治疗,但 DRV/COBI/FTC/TAF 仍被视为初治成人的替代治疗方案。DRV/COBI/FTC/TAF 是一种有效、耐受性良好且安全的抗逆转录病毒方案,对于因整合酶抑制剂相关神经精神副作用或病毒学失败等耐受性问题需要转换治疗的患者来说是一种有效选择。