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. 2019 Apr 25;63(5):e00014-19.
doi: 10.1128/AAC.00014-19. Print 2019 May.

Comparison of the Antiviral Activity of Bictegravir Against HIV-1 and HIV-2 Isolates and Integrase Inhibitor-Resistant HIV-2 Mutants

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Comparison of the Antiviral Activity of Bictegravir Against HIV-1 and HIV-2 Isolates and Integrase Inhibitor-Resistant HIV-2 Mutants

Robert A Smith et al. Antimicrob Agents Chemother. .
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Abstract

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.

Keywords: HIV treatment; HIV-2; West Africa; antiretroviral therapy; bictegravir; drug resistance; human immunodeficiency virus; integrase.

Figures

FIG 1
FIG 1
Antiviral activity of bictegravir against HIV-1NL4-3 and HIV-2ROD9 in MAGIC-5A cells. Error bars indicate ±1 SD and, when not visible, are smaller than the symbols. (A) Results from a single assay in which HIV-1NL4-3 and HIV-2ROD9 were tested head to head. Data points represent the amount of β-galactosidase activity produced in HIV-infected bictegravir-treated cultures relative to HIV-infected solvent-only (i.e., no-drug) controls. Each point is the mean of two cultures that were maintained in parallel. Curves were generated using a sigmoidal regression equation (GraphPad Prism 6.0 software). (B) EC50 values from seven independent runs of the single-cycle assay in which HIV-1NL4-3 and HIV-2ROD9 were tested head to head. P value is the result of a paired t test.
FIG 2
FIG 2
Summary of the activity of bictegravir against HIV-1 and HIV-2 isolates in MAGIC-5A cells. (A) Comparison of the EC50 values for group A and group B isolates of HIV-2. (B) Comparison of all EC50 values for HIV-1 and HIV-2. Each point represents the mean EC50 for a single virus isolate. Filled squares and circles indicate the EC50 values for HIV-1NL4-3 and HIV-2ROD9, respectively. Horizontal lines indicate the mean EC50 values for each grouping. P values are from Welch’s t tests.

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