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Safety, pharmacokinetics, and antiretroviral activity of islatravir (ISL, MK-8591), a novel nucleoside reverse transcriptase translocation inhibitor, following single-dose administration to treatment-naive adults infected with HIV-1: An open-label, phase 1b, consecutive-panel trial

The Lancet HIV Mar 13, 2020

Schürmann D, Rudd DJ, Zhang S, et al. - Researchers investigated the safety, pharmacokinetics, and antiretroviral activity of islatravir in treatment-naive adults with HIV-1 infection via conducting an open-label, consecutive-panel, phase 1b trial at Charité Research Organisation (Berlin, Germany). Participants were men and women (aged 18–60 years, inclusive) with HIV-1 infection who were ART-naive and were needed to have plasma HIV-1 RNA counts of at least 10,000 copies per mL within 30 days before the trial treatment phase, without evidence of resistance to nucleoside reverse transcriptase inhibitors. Enrollment of 30 participants (six per panel) was done in one of five consecutive dosing panels, receiving a single oral dose of islatravir (0·5–30 mg). Outcomes revealed significant suppression of HIV-1 RNA by more than 1·0 log at day 7 in treatment-naive adults with HIV-1 infection with using single doses of islatravir as low as 0·5 mg. The doses were generally well-tolerated, backing the further development of islatravir as a flexible-dose regimen for people with HIV-1 infection.
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