Dasabuvir (sodium)

Dasabuvir (ABT-333) sodium is a nonnucleoside hepatitis C virus (HCV) polymerase inhibitor. Dasabuvir sodium inhibits RNA-dependent RNA polymerase encoded by the HCV NS5B gene. Dasabuvir sodium inhibits genotype 1a (strain H77) and 1b (strain Con1) replicons, with EC₅₀ values of 7.7 and 1.8 nM, respectively^[1]. IC50 & Target: IC50: 2.2 ± 0.3 nM (HCV genotype 1b N), 2.8 ± 0.2 nM (HCV genotype 1a H77), 3.1 ± 0.21 nM (HCV genotype 1b BK), 0.7 ± 1.4 nM (HCV genotype 1b Con1)^[1] In Vitro: Dasabuvir (ABT-333) sodium is at least 7,000-fold selective for the inhibition of HCV genotype 1 polymerases over human/mammalian polymerases^[1].
Dasabuvir sodium inhibits the polymerase enzymatic activity of genotype 1 laboratory strain enzymes (H77, BK, N, and Con1 strains), as well as enzymes produced from polymerase genes from HCV genotype 1-infected subjects, with IC₅₀s between 2.2 and 10.7 nM^[1].
Dasabuvir sodium inhibits replication of HCV subgenomic replicons in cell culture assays, with EC₅₀ values of 7.7 and 1.8 nM against genotype 1a (H77) and 1b (Con1), respectively. In the presence of 40% human plasma, there is a 12- to 13-fold decrease in inhibitory potency, yielding EC₅₀s of 99 and 21 nM for HCV genotype 1a (H77) and 1b (Con1) replicons, respectively^[1].