HCV Protease Inhibitors

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Information about HCV Protease Inhibitors

The HCV protease inhibitors block the activity of the viral encoded protease that is essential in the post-translational modification of the viral polypeptide that is cleaved into a series of structural and nonstructural (enzyme) regions. The HCV proteases that have been developed are polypeptide-like molecules, modified amino acids that act as competitive inhibitors of the viral serine protease, resembling the specific amino acid sequence that the protease cleaves.

FDA approval information for HCV Protease Inhibitors

At least four HCV protease inhibitors (-previrs) have been approved for use in the United States (boceprevir [2012], telaprevir [2012], simeprevir [2013], paritaprevir [2014]) and grazoprevir [2015], and several more are in various stages of preclinical and clinical development.

Side effects of HCV Protease Inhibitors

The HCV protease inhibitors are generally well tolerated, but common adverse events include headache, dizziness, nausea, diarrhea, abdominal discomfort and rash.

Liver safety of HCV Protease Inhibitors

Liver injury has been reported with several of the HCV protease inhibitors, particularly asunaprevir which has been linked to acute hepatitis with immunoallergic features, sometimes as a part of a generalized hypersensitivity reaction. The onset of injury was within 4 to 12 weeks and was usually accompanied by fever, rash and eosinophilia. Serum enzyme elevations are typically hepatocellular and jaundice is mild-to-moderate in severity. At least one fatal instance of liver injury has been reported with asunaprevir. While asunaprevir has generally been given in combination with daclatasvir and sometimes with ribavirin, the liver injury has convincingly been attributed to asunaprevir in most cases.

HCV Protease Inhibitors

The following are drugs for Hepatitis C:

Interferon Based Therapies

HCV NS5A Inhibitors

HCV NS5B (Polymerase) Inhibitors

HCV Protease Inhibitors

Combination Therapies

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