Bictegravir (GS-9883) is a potent inhibitor of HIV-1 integrase (IC50: 7.5 nM).

HIV-1 integrase:7.5 nM

Bictegravir在对抗HIV-1复制方面显示出强烈的抑制作用，不论是在MT-2细胞还是MT-4细胞中，其半最大有效浓度(EC50)分别为1.5 nM和2.4 nM。此外，Bictegravir对HIV-1整合酶的链转移活性显示出显著的抑制效果，其半抑制浓度(IC50)为7.5 nM。相比于其对链转移活性的抑制，Bictegravir对HIV-1整合酶3'处理活性的抑制作用较弱，IC50为241 nM。Bictegravir能够相对于模拟处理对照组，将2-LTR圈的积聚量增加约5倍，并且在受感染的细胞中将真正的整合产物数量降低100倍。在初级CD4+ T淋巴细胞和单核细胞来源的巨噬细胞中，Bictegravir展现出强大的抗病毒效果，其EC50分别为1.5 nM和6.6 nM，与在T细胞系中获得的值相当。

MT-2 cells are infected in bulk culture with HIV-1 IIIb at a cell density of 2×10^6 cells/mL for 3 h at 37°C. Infected MT-2 cells receive either DMSO (mock-treated control) or Bictegravir at a final concentration greater than or equal to 20 times their respective antiviral EC50. These plates are incubated at 37°C for either 12 h (for late reverse transcription product quantification) or 24 h (for 2-LTR circle and Alu-LTR product quantification), after which time the cells are harvested for total DNA isolation. DNA is extracted from each well using the DNA minikit and collected as a 100-μL eluate. TaqMan real-time PCR-quantified 2-LTR junctions, late reverse transcription products, and integration junctions (Alu-LTR) are normalized to the level of host globin gene in each sample[1].