|Description||Against JFH1/3a-NS5A, DCV was more potent (EC(50) = 0.52 nM) than GS-5885 (EC(50) = 141 nM). DCV sensitivity was increased against JFH1/3a-NS5A-M28V (EC50 = 0.006 nM), A30V (EC(50) = 0.012 nM), and E92A (EC(50) = 0.004 nM) while the NS5A-A30K and -Y93H variants exhibited reduced sensitivity to DCV (EC50 values of 23 nM and 1120 nM, respectively) and to GS-5885 (EC50 values of 1770 nM and 4300 nM, respectively). GS-5885 was well tolerated and resulted in median maximal reductions in HCV RNA ranging from 2.3 log(10) IU/ml (1 mg QD) to 3.3 log(10) IU/ml (10 mg QD in genotype 1b and 30 mg QD). E(max) modeling indicated GS-5885 30 mg was associated with>95% of maximal antiviral response to HCV genotype 1a. HCV RNA reductions were generally more sustained among patients with genotype 1b vs. 1a. Three of 60 patients had a reduced response and harbored NS5A-resistant virus at baseline. NS5A sequencing identified residues 30 and 31 in genotype 1a, and 93 in genotype 1b as the predominant sites of mutation following GS-5885 dosing. Plasma pharmacokinetics was consistent with QD dosing.|
|Synonyms||GS-5885 acetone; GS 5885 acetone; GS5885 acetone|
Ombitasvir, a NS5A inhibitor, could be effective in the treatment of HCV as an antiviral agent. IC50: 14 pM and 5 pM (EC50) for genotype 1a-H77 and 1b-Con1 resp...
An NS3 serine protease inhibitor of hepatitis C virus, for the treatment of HCV infection.
PSI-7977 is a prodrug that is metabolized to the active antiviral agent 2'-deoxy-2'-α-fluoro-β-C-methyluridine-5'-monophosphate and is currently being investiga...
Artemisinin is a drug used to treat multi-drug resistant strains of falciparum malaria.
PSI-6130 is a potent and selective inhibitor of HCV NS5B polymerase. It is metabolized to two pharmacologically active species in primary human hepatocytes.
Asunaprevir is a potent hepatitis C virus (HCV) non-structural protein protease inhibitor currently in Phase III clinical trials for the treatment of HCV infect...
Elbasvir has been found to restrain viral phosphoprotein so that could be used against hepatitis C virus and is currently under Phase II trail.
Dasabuvir is an antiviral drug for the treatment of hepatitis C. It inhibits hepatitis C virus (HCV) non-nucleoside NS5B palm polymerase to suppress RNA replica...
Against JFH1/3a-NS5A, DCV was more potent (EC(50) = 0.52 nM) than GS-5885 (EC(50) = 141 nM). DCV sensitivity was increased against JFH1/3a-NS5A-M28V (EC50 = 0.0...
MK-5172 potassium salt
In biochemical assays, MK-5172 was effective against a panel of major genotypes and variants engineered with common resistant mutations observed in clinical stu...
Ribavirin is a guanosine (ribonucleic) analog used to stop viral RNA synthesis and viral mRNA capping, thus, it is a nucleoside inhibitor.
Danoprevir(ITMN-191;R7227; RO5190591;RG7227) is a peptidomimetic inhibitor of the NS3/4A protease of hepatitis C virus (HCV) with IC50 of 0.2-3.5 nM, inhibition...
Daclatasvir dihydrochloride is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype...
Ledipasvir (GS5885) is a HCV NS5A polymerase inhibitor, used for the treatment of hepatitis C virus infection.
VX-222 (VCH-222, Lomibuvir)
VX-222 (VCH-222) is a novel, potent and selective inhibitor of HCV polymerase with IC50 of 0.94-1.2 μM, 15.3-fold less effective for mutant M423T, and 108-fold ...
APC-6336 is a Hepatitis C virus NS3 protein inhibitor.
Tegobuvir is a non-nucleoside nonstructural protein (NS)5B polymerase inhibitor.
BMS-890068 is an acyclic P1 bi-cyclopropaneacylsulfonamidetripeptide that can be used as hepatitis C virus (HCV) NS3 protease inhibitor.
Radalbuvir is a Hepatitis C virus NS 5 protein inhibitor for the treatment of hepatitis C virus (HCV) infection developed by Gilead Sciences. In 2014, Gilead co...
PSI-7409, the active 5′-triphosphate metabolite of PSI-7851, is a potent inhibitor of the HCV NS5B RNA dependent RNA polymerase.