Dvory-Sobol Hadas, Shaik Naveed, Callebaut Christian, Rhee Martin S
Gilead Sciences, Foster City, California, USA.
Curr Opin HIV AIDS. 2022 Jan 1;17(1):15-21. doi: 10.1097/COH.0000000000000713.
This review summarizes available data for lenacapavir, an investigational first-in-class agent that disrupts functioning of HIV capsid protein across multiple steps in the viral life cycle.
Lenacapavir demonstrated picomolar potency in vitro with no cross resistance to existing antiretroviral classes and potent antiviral activity in persons with HIV-1. In persons with HIV-1, there was no preexisting resistance to lenacapavir regardless of treatment history. Lenacapavir can be administered orally either daily or weekly and subcutaneously up to every 6 months. In heavily treatment-experienced persons with multidrug-resistant HIV-1 and in treatment-naive persons with HIV-1, lenacapavir in combination with other antiretroviral agents led to high rates of virologic suppression and was well tolerated.
Ongoing studies are evaluating long-acting dosing of lenacapavir for treating HIV-1 in combination with other antiretrovirals and preventing HIV-1 as a single agent.
本综述总结了关于来那卡帕韦的现有数据,来那卡帕韦是一种处于研究阶段的一流药物,可在病毒生命周期的多个步骤中破坏HIV衣壳蛋白的功能。
来那卡帕韦在体外表现出皮摩尔级别的效力,对现有抗逆转录病毒药物类别无交叉耐药性,并且在HIV-1感染者中具有强大的抗病毒活性。在HIV-1感染者中,无论治疗史如何,对来那卡帕韦均无预先存在的耐药性。来那卡帕韦可以每日或每周口服给药,皮下注射给药则最长间隔6个月。在有大量治疗经验的多重耐药HIV-1感染者以及初治HIV-1感染者中,来那卡帕韦与其他抗逆转录病毒药物联合使用可导致高病毒学抑制率,且耐受性良好。
正在进行的研究正在评估来那卡帕韦与其他抗逆转录病毒药物联合治疗HIV-1以及作为单一药物预防HIV-1的长效给药方案。