Elbasvir

Elbasvir Uses, Dosage, Side Effects, Food Interaction and all others data.

Elbasvir is a direct-acting antiviral medication used as part of combination therapy to treat chronic hepatitis C, an infectious liver disease caused by infection with hepatitis C virus (HCV). HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most common in the United States, affecting 72% of all chronic HCV patients. Treatment options for chronic hepatitis C have advanced significantly since 2011, with the development of direct-acting antivirals (DAAs) such as elbasvir. Elbasvir is an inhibitor of NS5A, a protein essential for viral replication and virion assembly. The barrier to the development of resistance to NS5A inhibitors is lower than that of NS5B inhibitors, another class of DAAs. Substitutions at amino acid positions 28, 30, 31, or 93 are known to confer resistance to elbasvir. Despite this disadvantage elbasvir is still effective against HCV, particularly when paired with grazoprevir.

Elbasvir is available as a fixed-dose combination product with grazoprevir (tradename: Zepatier) used for the treatment of chronic hepatitis C. Approved in January 2016 by the FDA, Zepatier is indicated for the treatment of HCV genotypes 1 and 4 with or without ribavirin depending on the presence of resistance-associated amino acid substitutions in the NS5A protein and previous treatment failure with ribavirin, peginterferon alfa-2a, peginterferon alfa-2b, or other NS3/4A inhibitors like boceprevir, simeprevir, or telaprevir. Elbasvir and grazoprevir are used with or without ribavirin with the intent to cure, or achieve a sustained virologic response (SVR), and have been shown to achieve a SVR between 94% and 97% for genotype 1 and 97% and 100% for genotype 4 after 12 weeks of treatment.. SVR and eradication of HCV infection are associated with significant long-term health benefits including reduced liver-related damage, improved quality of life, reduced incidence of hepatocellular carcinoma, and reduced all-cause mortality.

In a computational target-based drug repurposing investigation published in April 2020, elbasvir was predicted to bind stably and preferentially to three proteins necessary for viral replication of SARS-CoV-2, the human coronavirus responsible for the COVID-19 pandemic. While these results are suggestive of antiviral efficacy, follow-up clinical trials are required to validate elbasvir as a potential therapy against SARS-CoV-2.

Elbasvir
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Elbasvir
Generic	Elbasvir
Elbasvir Other Names	Elbasvir
Type
Formula	C₄₉H₅₅N₉O₇
Weight	Average: 882.035 Monoisotopic: 881.422445147
Protein binding	Elbasvir is more than 99.9% bound to plasma proteins. It binds both human serum albumin and α1-acid glycoprotein.
Groups	Approved
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Elbasvir is an antiviral and NS5A inhibitor used to treat hepatitis C infections.

Elbasvir, when used in combination with grazoprevir as the combination product Zepatier, is indicated for use with or without ribavirin for the treatment of chronic HCV genotypes 1 or 4 infection in adults.

Elbasvir is also used to associated treatment for these conditions: Chronic Hepatitis C Genotype 1, Chronic hepatitis C genotype 1a, Chronic hepatitis C genotype 1b, Chronic hepatitis C genotype 3, Chronic hepatitis C genotype 4

How Elbasvir works

Elbasvir is an inhibitor of the HCV non-structural protein 5A. While the precise role of this protein is unknown, it is essential to viral replication and virion assembly. Potential modes of action of NS5A inhibitors like elbasvir include blocking signaling interactions, redistribution of NS5A from the endoplasmic reticulum to the surface of lipid droplets, and modification of the HCV replication complex.

Computational target-based in silico research suggests that elbasvir may carry activity at several proteins required for replication of SARS-CoV-2 - namely RNA-dependent RNA polymerase, helicase, and papain-like proteinase - although specific activity has yet to be affirmed by follow-up clinical studies.

Toxicity

The most commonly reported adverse reactions of all intensity (greater than or equal to 5% in placebo-controlled trials) were fatigue, headache, and nausea.

Food Interaction

Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of elbasvir. Co-administration of Elbasvir with St. John's Wort is contraindicated.
Exercise caution with grapefruit products. Grapefruit inhibits CYP3A, which may increase the serum levels of elbasvir, a CYP3A substrate.
Take at the same time every day.
Take with or without food.

Volume of Distribution

Elbasvir has an estimated apparent volume of distribution of 680 liters. It is thought to distribute into most tissues including the liver.

Elimination Route

Elbasvir reaches peak plasma concentration 3-6 hours after administration and has an absolute bioavailability of 32%. When co-administered with food, the peak concentration of elbasvir increases 1.5-fold, but this increase in exposure is not likely to be clinically relevant.