Formulation: A solid
Formal Name: 2,3,4,5,7,9,13,13a-octahydro-8-hydroxy-7,9-dioxo-N-[(2,4,6-trifluorophenyl)methyl]-2,5-methanopyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide, monosodium salt
Purity: ≥95%
Formula Markup: C21H17F3N3O5 • Na
Formula Weight: 471,4
Shelf life (days): 1460
CAS Number: 1807988-02-8
Notes: Bictegravir is an inhibitor of HIV-1 integrase (IC50 = 7.5 nM for strand transfer activity).{47145} It has antiviral activity against clinical isolates of HIV-1 in human peripheral blood mononuclear cells (PBMCs; EC50s = 0.04-1.7 nM). Bictegravir also inhibits HIV-1 viral infection in MT-2 and MT-4 cells, CD4+ T cells, and macrophages (EC50s = 1.5, 2.5, 1.5, and 6.6 nM, respectively) without exhibiting cytotoxicity (CC50s = 10.3, 3.7, 13, and 29.8 μM, respectively). Formulations containing bictegravir in combination with emtricitabine and tenofovir alafenamide have been used in the treatment of HIV-1 infections.
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