Article
Antiviral Activity of Bictegravir (GS-9883), a Novel Potent HIV-1 Integrase Strand Transfer Inhibitor with an Improved Resistance Profile.
Antimicrobial agents and chemotherapy - 1 Dec 2016
Tsiang Manuel, Jones Gregg S, Goldsmith Joshua, Mulato Andrew, Hansen Derek, Kan Elaine, Tsai Luong, Bam Rujuta A, Stepan George, Stray Kirsten M, Niedziela-Majka Anita, Yant Stephen R, Yu Helen, Kukolj George, Cihlar Tomas, Lazerwith Scott E, White Kirsten L, Jin Haolun
Abstract excerpt
Bictegravir (BIC; GS-9883), a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase (IN), specifically targets IN strand transfer activity (50% inhibitory concentration [IC50] of 7.5 ± 0.3 nM) and HIV-1 integration in cells. BIC exhibits potent and selective in vitro antiretroviral activity in both T-cell lines and primary human T lymphocytes, with 50% effective concentrations ranging from 1.5 to 2.4...
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