RO-9187 is an effective HCV virus replication inhibitor(IC50: 171 nM).

HCV:171 nM

RO-9187 suppresses RNA synthesis by HCV polymerases from either HCV genotypes 1a and 1b or containing S96T or S282T point mutations with similar potencies, suggesting no cross-resistance with either R1479 or 2′-C-methyl nucleosides. RO-9187 is excellent substrates for deoxycytidine kinase and is phosphorylated with efficiencies up to 3-fold higher than deoxycytidine. The formation of RO-9187-TP increased in a time- and dose-dependent manner [1].

Plasma exposures of RO-9187 in rats increase dose-dependently from 10 to 2000 mg/kg after oral administration. Plasma concentrations of RO-9187 (1.4 and 26 μM) are achieved in rats and dogs at the 10 mg/kg dose, respectively, with concentrations reaching up to 57 μM in rats at 2000 mg/kg/day[1].