Lomibuvir (VX-222; VCH-222) is a non-cytotoxic, orally active non-nucleoside inhibitor (NNI) against hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (genotype 1a/1b IC50 = 0.94/1.2 μM). Lomibuvir exhibits HCV genotype-selective antiviral activity in vitro (genotype 1a//1b EC50 = 23.3 nM/12 nM; ineffective against 2a & 2b) and in vivo by targeting HCV NS5B thumb II allosteric pocket, exhibiting no inhibitory potency against human DNA polymerase (α, β, γ IC50 ≥56 μM), respiratory syncytial virus, Influenza A and B, and West Nile virus.
Non-cytotoxic, orally active hepatitis C virus (HCV) NS5B RNA polymerase inhibitor with HCV genotype 1a/1b-selective antiviral activity in vitro and in vivo.
Therapeutic targeting of membrane-associated viral proteins is complicated by the challenge of investigating their enzymatic activities in the native membrane-bound state. To permit functional characterization of these proteins, we hypothesized that the supported lipid bilayer (SLB) can support in situ
Hepatitis C virus (HCV) is a genetically diverse virus with multiple genotypes exhibiting remarkable differences, particularly in drug susceptibility. Drug and vaccine development will benefit from high-titer HCV cultures mimicking the complete viral life cycle, but such systems only exist
The six major epidemiologically important hepatitis C virus (HCV) genotypes differ in global distribution and antiviral responses. Full-length infectious cell-culture adapted clones, the gold standard for HCV studies in vitro, are missing for genotypes 4 and 5. To address this
European journal of gastroenterology & hepatology, 26(7), 761-773 (2014-06-06)
To investigate in this phase 2a study (ZENITH) the safety, tolerability, and antiviral activity of VX-222, a selective, non-nucleoside inhibitor of hepatitis C virus (HCV) NS5B polymerase, combined with various telaprevir-based regimens for treatment of genotype 1 HCV. In total
Development of allosteric inhibitors into efficient drugs is hampered by their indirect mode-of-action and complex structure-kinetic relationships. To enable the design of efficient allosteric drugs targeting the polymerase of hepatitis C virus (NS5B), the interaction characteristics of three non-nucleoside compounds
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