HCV Protease Inhibitors
Information about HCV Protease Inhibitors[edit source]
HCV Protease Inhibitors | |
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Drug class | |
Class identifiers | |
Use | Treatment of Hepatitis C |
HCV Protease Inhibitors are antiviral agents specifically designed to combat the Hepatitis C Virus (HCV). These inhibitors function by obstructing the activity of the viral protease, a crucial enzyme for the post-translational modification of the HCV polypeptide. This polypeptide undergoes cleavage into multiple structural and nonstructural regions. The protease inhibitors mimic specific amino acid sequences that the viral serine protease cleaves, thereby acting as competitive inhibitors.
Mechanism of Action[edit | edit source]
HCV Protease Inhibitors primarily target and block the activity of the HCV-encoded protease. This enzyme plays an indispensable role in the post-translational modification process, cleaving the viral polypeptide into various structural and nonstructural regions. The inhibitors resemble the specific amino acid sequence that the protease would typically cleave, thereby effectively inhibiting its activity.
US FDA Approval[edit | edit source]
Several HCV Protease Inhibitors, distinguished by their '-previr' suffix, have secured approval from the US FDA:
- Boceprevir – 2012
- Telaprevir – 2012
- Simeprevir – 2013
- Paritaprevir – 2014
- Grazoprevir – 2015
Furthermore, numerous other inhibitors are progressing through different phases of preclinical and clinical evaluation.
Adverse Effects[edit | edit source]
While HCV Protease Inhibitors are predominantly well-received by patients, some common side effects have been documented:
Liver Safety Concerns[edit | edit source]
Although many HCV Protease Inhibitors are generally deemed safe, there have been instances of liver injury associated with certain drugs. Asunaprevir, in particular, has been implicated in cases of acute hepatitis characterized by immunoallergic features. These events sometimes manifest as part of a broader hypersensitivity reaction. The onset of injury typically appears between 4 to 12 weeks post-administration, often accompanied by symptoms like fever, rash, and eosinophilia. Although the jaundice is usually mild to moderate, at least one fatal incident involving liver injury has been reported in association with asunaprevir. While this drug is often co-administered with daclatasvir and occasionally ribavirin, most evidence points to asunaprevir as the primary agent responsible for the observed liver injuries.
List of HCV Protease Inhibitors[edit | edit source]
- Asunaprevir
- Boceprevir
- Glecaprevir
- Grazoprevir – Branded as Zepatier
- Paritaprevir – Marketed under Technive and Viekira Pak
- Simeprevir
- Telaprevir
References[edit | edit source]
External Links[edit | edit source]
HCV Protease Inhibitors Resources | |
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Antiviral agents[edit source]
Drugs for HIV Infection, in the Subclass Antiretroviral Agents
- Fusion Inhibitors (HIV)
- Integrase Inhibitors (HIV)
- Nonnucleoside Reverse Transcriptase Inhibitors (HIV)
- Interferon Based Therapies
HCV NS5A Inhibitors
HCV NS5B (Polymerase) Inhibitors
- Asunaprevir, Boceprevir, Glecaprevir, Grazoprevir, Paritaprevir, Simeprevir, Telaprevir, Voxilaprevir
Combination Therapies
Drugs for Herpes Virus Infections (HSV, CMV, others)
Drugs for Influenza
The following are drugs for Hepatitis C:
HCV NS5A Inhibitors
HCV NS5B (Polymerase) Inhibitors
HCV Protease Inhibitors
- Asunaprevir, Boceprevir, Glecaprevir, Grazoprevir, Paritaprevir, Simeprevir, Telaprevir, Voxilaprevir
Combination Therapies
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