| BMS-790052 is the most potent hepatitis C virus (HCV) replication inhibitor. BMS-790052 targets nonstructural protein 5A (NS5A). BMS-790052 is highly efficacious against genotype 1 replicons. BMS-790052 also displays robust genotype 1 anti-HCV activity. [1] The mean EC50 of BMS-790052 against genotype 1a and 1b replicons is 50 and 9 pM, respectively. Combination of BMS-790052 with with interferon-α/ribavirin, an inhibitor of NS3 protease (ITMN-191), produces additive-to-synergistic effects. BMS-790052 potently inhibits the JFH-1 genotype 2a infectious virus that replicates in cell culture with an EC50 of 28 pM. Additionally, BMS-790052 has similar potency among Huh-7, HeLa and HEK293T cells.[2] BMS-790052 inhibits genotype 2a JFH1 replicon cells and cell culture infectious virus with EC50 of 46.8 and 16.1 pM, respectively. BMS-790052 inhibits JFH1-L31M (Renilla luciferase) and JFH1-WT (β-lactamase) replicons with EC50 of 6.4 and 0.07 nM, respectively.[1] For genotype 1b, BMS-790052 retains subnanomolar potency against all variants with single amino acid substitutions, indicating that multiple mutations will likely be required for significant in vivo resistance in this genetic background. Importantly, BMS-790052-resistant variants remain completely sensitive to alpha interferon and small-molecule inhibitors of HCV protease and polymerase.[3] |
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