Elbasvir/grazoprevir (trade name Zepatier /ˈzɛpətɪər/ ZEP-ə-teer) is a fixed-dose combination for the treatment of hepatitis C, containing elbasvir (an inhibitor of hepatitis C virus’s NS5A protein) and grazoprevir (an NS3/4A inhibitor). It is used to treat chronic hepatitis C virus (HCV) genotypes 1 or 4 infection in both treatment-naïve and treatment-experienced patients.
Zepatie Medical uses
Elbasvir/grazoprevir received FDA approval in January 2016. Its indication is for treatment of chronic hepatitis C of the genotypes 1 and 4 for adults. Hepatitis C is a global disease that infects upwards of 150 million people worldwide, especially in older generations. Hepatitis C causes inflammation of the liver that eventually leads to diminished liver function or even failure. Zepatier is indicated for treatment with or without use of ribavirin, as well. Zepatier has shown enough efficacy to be considered a first line of treatment for first-time patients with GT 1a and 1b, with or without cirrhosis. It is recommended for non-naive patients of the same genotypes, in addition to patients of GT4.
It consists of 50 mg of elbasvir and 100 mg of grazoprevir. Genetic testing for genotype 1 is recommended to determine if the patient is NS5A resistant before the initial treatment. This resistance results in a likely decrease in SRV12.Dosage is taken once daily over the most common span of 12-weeks. Elbasvir/grazoprevir is oftentimes prescribed with ribavirin for patients with renal impairment. “Zepatier is available as a beige-colored, oval-shaped, film-coated tablet debossed with “770” on one side and plain on the other.
Patient population Treatment Duration
Genotype 1a: Treatment-naïve or PegIFN/RBV-experienced without baseline NS5A polymorphisms Zepatier 12 weeks
Genotype 1a: Treatment-naïve or PegIFN/RBV-experienced with baseline NS5A polymorphisms Zepatier + ribavirin 16 weeks
Genotype 1b: Treatment-naïve or PegIFN/RBV-experienced Zepatier 12 weeks
Genotype 1a§ or 1b: PegIFN/RBV/PI-experienced Zepatier + ribavirin 12 weeks
Genotype 4: Treatment-naïve Zepatier 12 weeks
Genotype 4: PegIFN/RBV-experienced Zepatier + ribavirin 16 weeks
Interactions and contraindications
Grazoprevir is transported by the solute carrier proteins SLCO1B1 and SLCO1B3. Drugs that inhibit this proteins, such as rifampicin, ciclosporin, and a number of HIV medications (atazanavir, darunavir, lopinavir, saquinavir, tipranavir, cobicistat), can cause a significant increase in grazoprevir blood plasma levels. Combination of elbasvir/grazoprevir with these drugs is therefore contraindicated.
Both elbasvir and grazoprevir are degraded by the liver enzyme CYP3A4. Combination with drugs that induce this enzyme, such as efavirenz, carbamazepine or St. John’s wort, is contraindicated because it can lead to ineffectively low plasma levels of elbasvir and grazoprevir. Combination with CYP3A4 inhibitors may increase plasma levels and is not recommended by the manufacturer.