2'-O-Methylcytidine is an orally active 2'-substituted nucleoside that acts as an inhibitor of HCV replication with antiviral activity. It inhibits RNA-dependent RNA polymerase (NS5B)-catalyzed RNA synthesis in vitro by competing with substrate nucleoside triphosphate. The compound has shown antiviral activity against Hepatitis C virus infected human Huh7 AVA5 cells with an EC50 of 1.8 μM, and cytotoxicity against the same cells with a CC50 of >300 μM. In HBI10A cells, 2'-O-Methylcytidine inhibits HCV RNA replication with an IC50 value of 21 μM. Furthermore, in vivo studies demonstrated that 2'-O-Methylcytidine (16.6 mg/kg, p.o., daily for 7 days) reduced serum HCV RNA by 1.05 log10 copies/mL in chronically infected chimpanzees.
- Orally active 2'-substituted nucleoside.
- Inhibits HCV replication.
- Exhibits antiviral activity.
- Competitively inhibits RNA-dependent RNA polymerase (NS5B)-catalyzed RNA synthesis in vitro.