tcsc2028 Dasabuvir

Dasabuvir (ABT-333) is a nonnucleoside inhibitor of the RNA-dependent RNA polymerase encoded by the HCV NS5B gene, inhibits recombinant NS5B polymerases derived from HCV genotype 1a and 1b clinical isolates, with IC₅₀ between 2.2 and 10.7 nM.

IC50 & Target: IC50: 2.2-10.7 nM (NS5B polymerase)^[1]

In Vitro: Dasabuvir (ABT-333) is at least 7,000-fold selective for the inhibition of HCV genotype 1 polymerases over human/mammalian polymerases. Dasabuvir (ABT-333) 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. Dasabuvir (ABT-333) 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].