Information about Zepatier
Zepatier is an oral, fixed combination of antiviral agents that is used to treat chronic hepatitis C, genotypes 1 and 4. This combination has been associated with low rate of transient serum enzyme elevations during therapy, but has not been implicated in cases of clinically apparent liver injury with jaundice.
Mechanism of action of Zepatier
Zepatier is the commercial name for a combination of antiviral agents used to treat chronic hepatitis C associated with HCV genotypes 1 and 4. The hepatitis C virus (HCV) encodes several nonstructural (NS) polypeptides that are essential for its replication, NS3/4 that has protease and helicase activities, NS5A that is a membrane bound polypeptide of uncertain purpose and NS5B an HCV specific, RNA-dependent, RNA polymerase. These polypeptides are effective targets for antiviral therapy of hepatitis C.
Combination of grazoprevir and elbasvir
Zepatier is a fixed dose combination of grazoprevir (graz oh’ pre vir) which is a potent HCV NS3/4 protease inhibitor and elbasvir (elb’ as vir) an NS5A inhibitor. In cell culture and in humans infected with HCV, each of these agents has potent activity against HCV, but antiviral resistance arises rapidly with continued exposure. The combination of several direct acting agents with different molecular targets allows for a sustained viral suppression while avoiding antiviral resistance.
Clinical use of Zepatier
The combination of these two agents with and without the ribavirin (an antiviral nucleoside analogue with activity against HCV) was shown to be very effective in suppressing HCV replication in patients infected with HCV genotypes 1 and 4, and to result in sustained virological responses and eradication of HCV in more than 95% of patients when given for 12 weeks or more.
FDA approval information for Zepatier
Zepatier was approved for use in the United States in 2016, the third all-oral antiviral combination to receive approval for chronic hepatitis C. It is available as tablets with the fixed dose combination of 100 mg of grazoprevir and 50 mg of elbasvir.
Dosage and administration for Zepatier
The recommended dose in adults is 1 tablet daily for 12 weeks. The addition of ribavirin for 12 weeks and prolongation of therapy to 16 weeks is recommended for some groups of HCV infected patients, such as those with previous non-response to antiviral therapy and those with preexisting resistance associated viral variants. Current indications are limited to patients with HCV genotypes 1 and 4.
Side effects of Zepatier
Side effects are uncommon, but are generally mild and can include fatigue, headache and nausea.
Drugs for HIV Infection, in the Subclass Antiretroviral Agents
- Nonnucleoside Reverse Transcriptase Inhibitors (HIV)
- Nucleoside Analogues (HIV)
- Protease Inhibitors (HIV)
HCV NS5A Inhibitors
HCV NS5B (Polymerase) Inhibitors
- Asunaprevir, Boceprevir, Glecaprevir, Grazoprevir, Paritaprevir, Simeprevir, Telaprevir, Voxilaprevir
Drugs for Herpes Virus Infections (HSV, CMV, others)
Drugs for Influenza