Center for Emerging and Reemerging Infectious Diseases and Department of Medicine, Division of Allergy and Infectious Diseases, University of Washington, Seattle, Washington, USA
Center for Emerging and Reemerging Infectious Diseases and Department of Medicine, Division of Allergy and Infectious Diseases, University of Washington, Seattle, Washington, USA.
Antimicrob Agents Chemother. 2019 Apr 25;63(5). doi: 10.1128/AAC.00014-19. Print 2019 May.
We compared the activity of the integrase inhibitor bictegravir against HIV-1 and HIV-2 using a culture-based, single-cycle assay. Values of 50% effective concentrations ranged from 1.2 to 2.5 nM for 9 HIV-1 isolates and 1.4 to 5.6 nM for 15 HIV-2 isolates. HIV-2 integrase mutants G140S/Q148R and G140S/Q148H were 34- and 110-fold resistant to bictegravir, respectively; other resistance-associated mutations conferred ≤5-fold changes in bictegravir susceptibility. Our findings indicate that bictegravir-based antiretroviral therapy should be evaluated in HIV-2-infected individuals.
我们使用基于培养的单周期测定法比较了整合酶抑制剂比替拉韦对 HIV-1 和 HIV-2 的活性。9 株 HIV-1 分离株的半数有效浓度（EC50）值范围为 1.2 至 2.5 nM，15 株 HIV-2 分离株的 EC50 值范围为 1.4 至 5.6 nM。HIV-2 整合酶突变体 G140S/Q148R 和 G140S/Q148H 对比替拉韦的耐药性分别为 34 倍和 110 倍；其他与耐药性相关的突变使比替拉韦的敏感性变化≤5 倍。我们的研究结果表明，应在感染 HIV-2 的个体中评估基于比替拉韦的抗逆转录病毒疗法。
