Zepatier (elbasvir, grazoprevir)

Reviewed by: HU Medical Review Board | Last reviewed: March 27, 2022 | Last updated: April 2022

Zepatier (elbasvir and grazoprevir) is a fixed-dose combination medicine used to treat adults with chronic HCV genotype 1 or 4. In some cases, Zepatier is used along with ribavirin. Zepatier is a direct-acting antiviral (DAA) drug.1,2

What are the ingredients in Zepatier?

The active ingredients in Zepatier are elbasvir and grazoprevir.1

How does Zepatier work?

The active ingredients in Zepatier work in 2 different ways:1

  • Elbasvir is a direct-acting antiviral that inhibits HCV NS5A. NS5A is a protein made by the HCV virus that is important to the virus’ growth and replication. It works to eliminate NS5A proteins made by the virus that are used for RNA replication and virion assembly.
  • Grazoprevir is also a direct-acting antiviral that acts as an HCV NS3/4A protease inhibitor. This protease is an essential enzyme the virus needs to replicate. By blocking this enzyme, the virus is not able to grow and reproduce.

Many direct-acting antivirals work this way, targeting proteins, enzymes, and specific steps in the HCV life cycle.

What are the possible side effects of Zepatier?

The most common side effects of Zepatier include:1

  • Headache
  • Tiredness
  • Nausea

The most common side effects of Zepatier and ribavirin together include:1,2

  • Low red blood cell count (anemia)
  • Headache

Zepatier has a boxed warning, the strictest warning from the U.S. Food and Drug Administration (FDA). This is because it may worsen or reactivate the hepatitis B virus (HBV) during or after treatment. This may cause serious liver problems, including liver failure or death. People with current or past HBV infection should be monitored during treatment with Zepatier. Some may also need to be treated for HBV. Your doctor should take a blood test to check for HBV before your treatment with Zepatier.1

Your doctor will monitor your liver function before and during treatment. Contact your doctor right away if you have signs of liver problems, including:1

  • Weakness
  • Loss of appetite
  • Nausea and vomiting
  • Yellowing of skin or eyes
  • Color changes in stools
  • Tiredness

These are not all the possible side effects of Zepatier. Talk to your doctor about what to expect or if you experience any changes that concern you during treatment with Zepatier.

Things to note about Zepatier

Before starting Zepatier, tell your doctor if you have:1

  • A current or previous hepatitis B infection
  • Current or prior liver problems other than those related to HCV

Zepatier should not be used by people who:1

  • Have moderate or severe hepatic impairment (Child-Pugh B or C)
  • Take OATP1B1/3 inhibitors that significantly increase grazoprevir plasma concentrations, strong CYP3A inducers, and efavirenz

Zepatier taken with ribavirin can harm an unborn baby. If you or your partner can become pregnant, you should use birth control during treatment and for some time after the last dose of Zepatier and ribavirin. You should also not breastfeed during treatment with Zepatier and ribavirin and for some time after the last dose. Talk to your doctor about your options for birth control and breastfeeding while taking Zepatier and ribavirin.1

Before beginning treatment for HCV, tell your doctor about all your health conditions and any other drugs, vitamins, or supplements you are taking. This includes over-the-counter drugs.

For more information, read the full prescribing information of Zepatier.

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