Boceprevir: Uses, Functions, and Discontinuation
Hepatitis C is a serious condition that, for more than half of people infected, becomes a long-term, chronic infection that can even be life-threatening. While we did have medications for Hepatitis C in the early 2010s, some people’s conditions may not improve with treatment. However, researchers found that when Boceprevir was added to the existing combination of medications, their condition improved significantly. Here’s how it works.
What is Hepatitis C?
To understand boceprevir and how it works, we must first understand the condition that it treats: hepatitis C. This is a liver infection that is spread via contact with the blood of an infected individual. It’s often spread by the sharing of needles and various equipment used for the preparation and injection of drugs. The virus has nine distinct genotypes, but genotype 1 is the most common in the U.S.
Hepatitis C can be immediately treated and it may be a short-term illness. However, over half of those who become infected with this virus experience chronic infections. These long-term cases may result in life-threatening health problems, like liver cancer and cirrhosis.
Unfortunately, there’s no vaccine for hepatitis C. People who have chronic hepatitis C often feel fine and have no symptoms. They may only experience symptoms when they appear as part of advanced liver disease. However, many treatments can cure hepatitis C in 8 to 12 weeks, which is why testing is so important. We can prevent this infection by avoiding the behaviors that spread it, like sharing needles and injecting drugs.
What is Boceprevir?
Boceprevir is a hepatitis C virus (HCV) protease inhibitor and a direct-acting antiviral medication. It was one of the first direct-acting agents to be developed to treat the virus. It’s used to treat adults with chronic hepatitis C infections who have never been treated or who have tried a previous treatment and been unsuccessful. Boceprevir is effective when used in conjunction with two other medications – peginterferon and ribavirin. The combination of three medications is called triple therapy.
How Does Boceprevir Work?
Boceprevir specifically works for the treatment of hepatitis C, genotype 1. It’s a synthetic tripeptide that interferes with the nonstructural protein 3 and 4A complex (NS3/NS4A). It works by binding to the active center of the hepatitis C NS3/NS4A and preventing the polyprotein from maturing, which is mediated by protease.
This effectively disrupts the viral proteins from forming new proteins and replicating in hepatitis C genotype 1-infected host cells. NS3 is a serine protease and is crucial for the virus to replicate itself via proteolytic cleavages. Meanwhile, NS4A functions as an activating factor for NS3.
How Do We Use Boceprevir?
Boceprevir is only effective at treating hepatitis C when used in combination with peginterferon and ribavirin. On its own, boceprevir effectively and quickly inhibits hepatitis C RNA levels, but the virus rapidly develops a resistance in most patients. This is why it must be used in combination with the other medications, which have been shown to have a low rate of antiviral resistance and sustained inhibition of hepatitis C RNA.
While peginterferon and ribavirin alone only had a sustained virological response (SVR) of 40% to 50%, triple therapy including boceprevir had an SVR rate of 65% to 75% for patients with genotype 1.
This medication is prescribed by a doctor. The recommended dose is 800 mg. It’s taken orally every eight hours – three times per day. Treatment generally lasts for 44 to 44 weeks at a time.
Advancements in Hepatitis C Treatment
Although groundbreaking, boceprevir was only used under the brand name Victelis from 2012 to 2015, when the company that made the medication voluntarily discontinued it. This was not due to any issue with boceprevir, but rather because other regiments of antiviral agents that were more potent and better tolerated were developed. These new medications could be given without peginterferon.
It’s also worth noting that boceprevir had a wide variety of side effects which were hard to separate from the side effects of peginterferon and ribavirin. The triple therapy had high rates of unpleasant side effects like fatigue, headache, nausea, anemia, rash, itching, and neutropenia (low white blood cell count).
The medication also came with special considerations. It was advised that you don’t breastfeed or get pregnant while taking the medication because ribavirin can cause stillbirth or birth defects. There was some evidence that the birth control pill would not work while taking boceprevir, which meant that it was best for women to completely abstain from sex while taking the medication. Patients taking the medication also had to get consistent blood tests during treatment.
Boceprevir was an effective and exciting advancement in medicine. It was potentially life-saving, as it treated chronic hepatitis C in people who had failed previous treatments. However, newer treatments have proven to be more tolerable and effective, leading to the demise of boceprevir.
Be sure to work with your primary care physician before using this medication or schedule a consultation with one of our health consultants.
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FAQs: Understanding Boceprevir’s Role in Hepatitis C Treatment
Please note: Boceprevir is no longer recommended for hepatitis C treatment. Newer direct-acting antivirals offer better safety and efficacy. This FAQ is for historical understanding only.
In what context was Boceprevir used for hepatitis C?
Boceprevir, a protease inhibitor, was once part of combination therapy with peginterferon alfa and ribavirin. It was mainly for previously untreated patients with HCV genotype 1, the most common genotype of the hepatitis C infection (HCV).
Why was Boceprevir discontinued?
Boceprevir is no longer recommended due to the availability of newer direct-acting antiviral agents (DAAs). These DAAs have revolutionized HCV treatment, offering higher cure rates (sustained virologic response), shorter treatment regimens, and fewer side effects.
What are some challenges of Boceprevir therapy?
Boceprevir, when used in combination with peginterferon and ribavirin, was associated with significant adverse events. Monitoring for anemia, potential drug interactions, and the challenging dosing regimen (800 mg three times a day) were crucial.
How was Boceprevir’s effectiveness evaluated?
Clinical trials assessed Boceprevir in previously untreated and previously treated patients with HCV infection. The primary goal was to achieve undetectable HCV RNA after a sustained period, indicating a sustained virologic response (SVR).
What were the limitations of Boceprevir-based therapy?
Factors like HCV genotype, previous treatment status, and the presence of compensated liver disease influenced responses. Also, patients with renal or hepatic impairment might have required dose adjustments or alternative therapies.
Were there specific safety concerns with Boceprevir?
Yes, in addition to common side effects, Boceprevir, when used in combination with peginterferon and ribavirin could lead to serious adverse events. Anemia was a significant concern, requiring close monitoring. Some patients also experienced worsening liver function.
What factors influenced treatment success with Boceprevir?
Success rates with Boceprevir were influenced by:
- HCV genotype: Genotype 1 was most responsive
- Prior treatment experience: Previously untreated patients saw better outcomes
- Liver health: Compensated liver disease improved chances of success
- Drug interactions: Careful review of all medications was essential to avoid complications
How long was a typical treatment regimen with Boceprevir?
Boceprevir-based therapy was lengthy. Treatment week duration depended on individual factors and response, but could extend to 24, 28, or even 48 weeks in some cases.
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Resources:
https://www.ncbi.nlm.nih.gov/books/NBK548247/
https://pubchem.ncbi.nlm.nih.gov/compound/Boceprevir
https://go.drugbank.com/drugs/DB08873
https://medlineplus.gov/druginfo/meds/a611039.html
https://www.hepatitisc.uw.edu/page/treatment/drugs/boceprevir-drug