817204-33-4

PSI-6130 is a nucleoside inhibitor of the NS5B RNA polymerase of hepatitis C virus (HCV; K_i = 4.3 μM). It inhibits HCV genotype 1b (GT-1b) Con1 and GT-1a H77 viral replication in Huh7 replicon cells using a luciferase-based assay (EC₅₀s = 0.51 and 0.30 μM, respectively). PSI-6130 also inhibits replication of HCV GT-1b and GT-1a replicons from clinical isolates, with EC₅₀ values ranging from 0.60 to 1.41 μM, and 0.20 to 0.43 μM, respectively, in the same assay. It has little or no activity against West Nile Virus (WNV), Dengue type 2 virus (DV), human immunodeficiency virus (HIV), or hepatitis B virus (HBV; EC₉₀s = 46.3, >100, >100, and >10 μM, respectively).

PSI-6130 is an experimental treatment for hepatitis C. PSI-6130 is a member of a class of antiviral drugs known as nucleoside polymerase inhibitors. PSI-6130 inhibits the hepatitis C virus RNA dependant RNA polymerase called NS5B.

Hepatitis C Virus Nucleoside

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[1] EISUKE MURAKAMI. Mechanism of activation of beta-D-2’-deoxy-2’-fluoro-2’-c-methylcytidine and inhibition of hepatitis C virus NS5B RNA polymerase.[J]. Antimicrobial Agents and Chemotherapy, 2007, 51 2: 503-509. DOI: 10.1128/aac.00400-06
[2] LIEVEN J STUYVER. Inhibition of hepatitis C replicon RNA synthesis by beta-D-2’-deoxy-2’-fluoro-2’-C-methylcytidine: a specific inhibitor of hepatitis C virus replication.[J]. Antiviral Chemistry and Chemotherapy, 2006, 17 2: 79-87. DOI: 10.1177/095632020601700203