Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Boceprevir
Drug ID BADD_D00283
Description Boceprevir 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, and affecting 72% of all chronic HCV patients [L852]. Treatment options for chronic Hepatitis C have advanced significantly since 2011, with the development of Direct Acting Antivirals (DAAs) such as Boceprevir. Boceprevir is an inhibitor of NS3/4A, a serine protease enzyme, encoded by HCV genotypes 1 and 4 [synthesis]. These enzymes are essential for viral replication and serve to cleave the virally encoded polyprotein into mature proteins like NS4A, NS4B, NS5A and NS5B [FDA Label]. The barrier for develoment of resistance to NS3/4A inhibitors is lower than that of NS5B inhibitors, another class of DAAs [A19593]. Subtitutions at amino acid positions 155, 156, or 168 are known to confer resistance. The substitutions of the enzyme's catalytic triad consisting of H58, D82, and S139 are also likely to alter the affinity of the drug for NS3/4A or the activity of the enzyme itself. Despite this disadvantage Boceprevir is still effective against HCV when paired with [DB00811], [DB00008], and [DB00022]. In a joint recommendation published in 2016, the American Association for the Study of Liver Diseases (AASLD) and the Infectious Diseases Society of America (IDSA) do not reccomend Boceprevir in combination with [DB00811], [DB00008], and [DB00022] as first line therapy for Hepatitis C [A19593]. Boceprevir, [DB00811], [DB00008], and [DB00022] are used with the intent to cure, or achieve a sustained virologic response (SVR), after 48 weeks of daily therapy. SVR and eradication of HCV infection is 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 [A19626]. Boceprevir is available as a fixed dose product (tradename Victrelis) used for the treatment of chronic Hepatitis C. Approved in May 2011 by the FDA, Victrelis is indicated for the treatment of HCV genotype 1 in combination with [DB00811], [DB00008], and [DB00022] [FDA Label]. Victrelis is no longer widely used as interferon-free therapies have been developed.
Indications and Usage Boceprevir, when used in combination with [DB00811], [DB00008], and [DB00022] is indicated for use in the treatment of chronic HCV genotype 1 infection in adults [FDA Label].
Marketing Status Discontinued
ATC Code J05AP03
DrugBank ID DB08873
KEGG ID D08876
MeSH ID C512204
PubChem ID 10324367
TTD Drug ID D0V3YT
NDC Product Code Not Available
Synonyms N-(3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl)-3-(2-((((1,1-dimethylethyl)amino)carbonyl)amino)-3,3-dimethyl-1-oxobutyl)-6,6-dimethyl-3-azabicyclo(3.1.0)hexan-2-carboxamide | boceprevir | victrelis | Sch 503034 | Sch503034 | Sch-503034
Chemical Information
Molecular Formula C27H45N5O5
CAS Registry Number 394730-60-0
SMILES CC1(C2C1C(N(C2)C(=O)C(C(C)(C)C)NC(=O)NC(C)(C)C)C(=O)NC(CC3CCC3)C(=O)C(=O)N)C
Chemical Structure
ADR Related Proteins Induced by Drug
ADR Term Protein Name UniProt AC TTD Target ID PMID
Not AvailableNot AvailableNot AvailableNot AvailableNot Available
ADRs Induced by Drug
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Abdominal discomfort07.01.06.001--Not Available
Abdominal distension07.01.04.001--
Abdominal pain07.01.05.002--
Abdominal pain lower07.01.05.010--Not Available
Abdominal pain upper07.01.05.003--
Abnormal sensation in eye06.01.01.001--Not Available
Acute myocardial infarction24.04.04.001; 02.02.02.001--Not Available
Aggression19.05.01.001--Not Available
Agitation19.06.02.001; 17.02.05.012--
Agranulocytosis01.02.03.001--Not Available
Alopecia23.02.02.001--
Amenorrhoea05.05.01.002; 21.01.02.001--
Amnesia19.20.01.001; 17.03.02.001--
Anaemia01.03.02.001--
Anger19.04.02.001--Not Available
Angioedema23.04.01.001; 10.01.05.009--Not Available
Anxiety19.06.02.002--
Apathy19.04.04.002--Not Available
Aphthous ulcer07.05.06.002--Not Available
Arrhythmia02.03.02.001--Not Available
Arthralgia15.01.02.001--
Arthritis15.01.01.001--
Aspermia21.03.03.004--Not Available
Asthenia08.01.01.001--Not Available
Atrial fibrillation02.03.03.002--
Back pain15.03.04.005--
Bipolar I disorder19.16.01.002--Not Available
Blood triglycerides increased13.12.03.001--Not Available
Blood uric acid increased13.02.04.001--Not Available
Body temperature increased13.15.01.001--Not Available
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