Bictegravir

Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase with an IC₅₀ of 7.5 nM. IC50 & Target:IC50: 7.5 nM (HIV-1 integrase)^[1] In Vitro:Bictegravir (BIC) inhibits the strand transfer activity with an IC₅₀ of 7.5± 0.3 nM. Relative to its inhibition of strand transfer activity, Bictegravir is a much weaker inhibitor of 3′-processing activity of HIV-1 IN, with an IC₅₀ of 241±51 nM. Bictegravir enhances the accumulation of 2-LTR circles ~5-fold relative to the mock-treated control and reduces the amount of authentic integration products in infected cells by 100-fold. Bictegravir potently inhibits HIV-1 replication in both MT-2 and MT-4 cells with EC₅₀s of 1.5 and 2.4 nM, respectively. Bictegravir exhibits potent antiviral effects in both primary CD4⁺ T lymphocytes and monocyte-derived macrophages, with EC₅₀s of 1.5±0.3 nM and 6.6±4.1 nM, respectively, which are comparable to values obtained in T-cell lines^[1].