hcv 1b

Paritaprevir free base (ABT-450) is an orally bioavailable, synthetic acylsulfonamide inhibitor of the hepatitis C virus (HCV) protease complex comprised of non-structural protein 3 and 4A (NS3/NS4A), with potential activity against HCV genotype 1. Upon administration, paritaprevir reversibly binds to the active center and binding site of the HCV NS3/NS4A protease and prevents NS3/NS4A protease-mediated polyprotein maturation. This disrupts both the processing of viral proteins and the formation of the viral replication complex, which inhibits viral replication in HCV genotype 1-infected host cells.

Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is an orally available antiviral agent that inhibits the NS5A region of the hepatitis C virus (HCV) and is used in combination with other oral antivirals to treat chronic hepatitis C. Elevations in serum enzyme levels during daclatasvir therapy are uncommon, and it has not been convincingly implicated in cases of clinically apparent liver injury with jaundice.

JTK-853 is a novel, non-nucleoside inhibitor of Hepatitis C Virus (HCV) polymerase, exhibiting effective antiviral activity in HCV replicon cells with EC50s of 0.38 μM for genotype 1a H77 strain and 0.035 μM for genotype 1b Con1 strain.

NITD008 (7-Deaza-2'-C-acetylene-adenosine) is a potent and selective adenosine nucleoside inhibitor.NITD008 is an adenosine nucleoside analog with broad-spectrum antiviral activity that inhibits dengue, animal cupripoxvirus, and Zika virus.

Filibuvir (PF-00868554) is a selective and noncovalent inhibitor of HCV NS5B RNA-dependent RNA polymerase. Filibuvir inhibits genotype 1a and 1b replicons with EC50s of 59 nM.

Furaprofen is an orally available, selective and potent HCV inhibitor with anti-inflammatory activity, inhibits carrageenan-induced paw edema in rats and inhibits cotton pellet-induced granulomas in rats at higher doses.

Setrobuvir (ANA-598) is an orally active, highly selective non-nucleoside HCV NS5B polymerase inhibitor that inhibits new RNA synthesis and primer extension, with IC₅₀ values ranging from 4 to 5 nM. Setrobuvir exhibits high binding affinity for SARS-CoV-2 RdRp and induces inhibition of RdRp. Setrobuvir is suitable for Antiviral drugs studies.

HCV-IN-30 is an HCV NS5A replication complex inhibitor (IC50s: 901 and 102 nM for genotypes 1a and 1b replicons).

Faldaprevir is an orally effective, selective, non-covalent HCV NS3/4A protease inhibitor with high inhibitory activity against HCV 1a and 1b genotypes (Ki=2.6 nM &2.0 nM).Faldaprevir inhibits viral replication by blocking the breakdown of viral precursor proteins, and is well tolerated with good antiviral activity against hepatitis C virus.

Inarigivir soproxil (SB9200) is an agonist of innate immunity that demonstrates effective antiviral activity against resistant hepatitis C virus (HCV) variants, with EC50s of 2.2 and 1.0 μM for HCV 1a/1b in cells of genotype 1 HCV replicon systems.

Voxilaprevir is an inhibitor of hepatitis C virus (HCV) nonstructural (NS) protein 3/4A protease.

IDX375 is a non-nucleoside inhibitor that selectively targets the HCV NS5B enzyme. It shows promising selectivity for genotypes 1a and 1b. The structure and binding sites of IDX375 have been confirmed through X-ray co-crystallization studies.

PTC725 is a selective HCV 1b replicons inhibitor. It has been shown to target the nonstructural protein 4B.

GSK-625433, a homochiral inhibitor of the hepatitis C virus (HCV) RNA-dependent RNA polymerase, has the ability to inhibit the polymerase of both HCV genotypes 1a and 1b.

Asunaprevir (BMS-650032) is an effective hepatitis C virus (HCV) NS3 protease inhibitor.

Danoprevir (RG7227) is a peptidomimetic inhibitor of the NS3/4A protease(IC50=0.2-3.5 nM) of hepatitis C virus (HCV).

SMCypIC31 is a non-peptide cyclophilin inhibitor that effectively inhibits peptidyl-prolyl cis/trans isomerase (PPIase) (IC50: 0.1 μM). SMCypI C31 has a pan-genotypic effect against HCV, with an EC50 range of 1.20-7.76 μM against genotypes 1a, 1b, 2a, 3a and 5a HCV-SGRs and chimeric genotypes 2a/4a HCV-SGRs.

Dasabuvir (ABT-333) sodium is a non-nucleoside hepatitis C virus (HCV) polymerase inhibitor that exhibits inhibition of the RNA-dependent RNA polymerase (RNA polymerase) encoded by the HCV NS5B gene. Dasabuvir sodium inhibited genotype 1a (strain H77) replicon (EC50: 7.7 nM) and 1b (strain Con1) replicon (EC50: 1.8 nM).

Lomibuvir (VCH-222) is a selective, non-nucleoside allosteric inhibitor of HCV NS5B polymerase (RdRp) with a Kd of 17 nM. Lomibuvir inhibits the 1b/Con1 HCV subgenomic replicon with an EC 50 of 5.2 nM. Lomibuvir preferentially inhibits elongative RNA synthesis rather than de novo -initiated RNA synthesis [1].

Beclabuvir, also known as BMS-791325, is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase. BMS-791325 inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 at 50% inhibitory concentrations (IC50) below 28 nM. In cell culture, BMS-791325 inhibited replication of HCV subgenomic replicons representing genotypes 1a and 1b at 50% effective concentrations (EC50s) of 3 nM and 6 nM, respectively, with similar (3 to 18 nM) values for genotypes 3a, 4a, and 5a. B

Deleobuvir sodium is the salt form of Deleobuvir, also known as BI207127, a non-nucleoside hepatitis C virus NS5B polymerase inhibitor for the treatment of hepatitis C. Deleobuvir was tested in combination regimens with pegylated interferon and ribavirin, and in interferon-free regimens with other direct-acting antiviral agents including faldaprevir. Deleobuvir showed that a triple combination of deleobuvir, faldaprevir, and ribavirin performed well in HCV genotype 1b patients. Efficacy fell below 50%, however, for dual regimens without ribavirin and for genotype 1a patients. In December 2013, deleobuvir was discontinued since recent findings from phase III trials did not suggest sufficient efficacy.

NS5A-IN-3 (Compound 15) is a potent NS5A inhibitor with high efficacy against HCV genotype 1b, enhanced activity towards genotype 3a (GT 3a), and substantial metabolic stability. It exhibits superior resistance barrier compared to daclatasvir in genotype 1b [1].

Cis-Lomibuvir (cis-VX-222), a cis-isomer of Lomibuvir, is a selective non-nucleoside inhibitor of the hepatitis C virus (HCV) NS5B polymerase (RdRp), targeting thumb pocket 2 with a dissociation constant (Kd) of 17 nM. It exhibits an EC50 of 5.2 nM against the 1b/Con1 HCV subgenomic replicon, demonstrating a preference for inhibiting elongative RNA synthesis over de novo-initiated RNA synthesis.

NS5A-IN-2 (Compound 33) is a potent NS5A inhibitor with remarkable efficacy against HCV genotype 1b, increased activity against genotype 3a (GT 3a), and significant metabolic stability [1].