Hepatitis C is a liver infection caused by the hepatitis C virus (HCV). Hepatitis C is a blood-borne virus. Today, most people become infected with the hepatitis C virus by sharing needles or other equipment to inject drugs. For some people, hepatitis C is a short-term illness but for 70%–85% of people who become infected with the hepatitis C virus, it becomes a long-term, chronic infection.
Chronic hepatitis C is a serious disease than can result in long-term health problems, even death. Many people might not be aware of their infection because they are not clinically ill. There is no vaccine for hepatitis C. The best way to prevent hepatitis C is by avoiding behaviors that can spread the disease, especially injecting drugs.
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Ravidasvir (PPI-668;BI 238630) is a potent pan-genotypic HCV NS5A inhibitor with IC50 of 0.12/0.01/1.14 nM for HCV gt-1a/1b/3a in replicon luciferase assay; has been well tolerated and shown high sustained viral response rates as a key component in all-oral combination regimens in multiple human clinical trials.
A potent, selective, broad-spectrum MMP inhibitor with Ki of <9 nM for MMP2, 3, 8, 9, 12, 13 and 14, but not MMP1 and 7; displays little or no activity for other proteinases including caspases, the initiator and effector proteinases of apoptosis; attenuates hepatocyte apoptosis, liver injury and hepatic fibrosis, and is an attractive agent as a potential hepato-protective agent in HCV patients.
Velpatasvir (GS-5816) is a second generation, pan-genotypic inhibitor of HCV NS5A, demonstrates a high barrier to resistance in HCV replicon assays.
GSK-2485852 (GSK2485852, GSK5852) is a highly potent, selective HCV NS5B polymerase inhibitor with IC50 of 3.0 and 1.6 nM for HCV genotypes 1a and 1b in replicon assay, respectively; displays an excellent resistance profile and shows a <5-fold potency loss across the clinically important NS5B resistance mutations P495L, M423T, C316Y, and Y448H; targets NNI palm site 2 of NS5B and inhibits all HCV genotypes.
BMS-929075 is a highly potent, selective, orally bioavailable HCV NS5B polymerase inhibitor with IC50 of 9, 4, and 18 nM for GT1a, GT1b, and GT1b-C316N mutant in HCV replicon assay, respectively; possesses excellent pharmacokinetic parameters across preclinical animal species.
GSK-625433 is a highly potent, selective HCV NS5B polymerase inhibitor for treatment of HCV infection.
Ruzasvir is a potent, pan-genotype HCV NS5A inhibitor with replicon EC90 of 0.003, 0.016, 0.067, 0.036, 0.007, and 0.007 nM for GT1a, GT1a L31V, GT1a Y93H, GT2b, GT3a, and Gt4a, respectively.
INX-08189 is a phosphoramidate prodrug of O-6-methyl-2-C-methyl guanosine, potent inhibitor of HCV NS5B polymerase with IC50 of 10 nM in replicon assay; inhibits viral replication with EC50 of 35 nM, inhibits mutant NS5b S282T mutant replicon with EC90 of 344 nM; orally active.
Coblopasvir (KW136, KW-136) is a novel HCV NS5A inhibitor under development for treatment of HCV infection.
Merimepodib (VX-497, VI-21497, MMPD) is a potent, selective, reversible, uncompetitive IMPDH inhibitor with broad-spectrum antiviral activity; inhibits HBV, HCMV, RSV and HSV-1 with IC50 of 0.4, 0.8, 1.1 and 6.3 uM, also inhibits BVDV, VEEV, Coxsackie B3 and Dengue virus with IC50 at low uM level; Merimepodib is 17- to 186-fold more potent than ribavirin against HBV, HCMV, RSV, HSV-1, parainfluenza-3 virus, EMCV, and VEEV infections in cultured cells, also demonstrates additivity when coapplied with IFN-alpha
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