Drug information of boceprevir
Boceprevir is a direct acting antiviral medication used as part of combination therapy to treat chronic Hepatitis C. Boceprevir is an inhibitor of NS3/4A, a serine protease enzyme, encoded by HCV genotypes 1 and 4. These enzymes are essential for viral replication and serve to cleave the virally encoded polyprotein into mature proteins like NS4A, NS4B, NS5A and NS5B.
Mechanism of effect
Binds reversibly to nonstructural protein 3 (NS 3) serine protease and inhibits replication of the hepatitis C virus.
Boceprevir is classified as a direct-acting antiviral (DAA) and prevents viral replication in HCV genotype 1.
Absorption: Food enhances absorption by up to 65%
Protein binding: ~75%
Metabolism: Primarily hepatic via aldo-ketoreductase pathway to inactive metabolites.
Half-life elimination: Adults: ~3.4 hours
Excretion: Feces (79%); urine (9%)
Chronic Hepatitis C
Discontinued; sale and distribution of boceprevir had been discontinued in the United States by December 2015.
Indicated for treatment of chronic hepatitis C (CHC) genotype 1 infection in combination with peginterferon alfa and ribavirin
Indication is specifically for adults with compensated liver disease, including cirrhosis, who are previously untreated or who have failed previous interferon and ribavirin therapy
Initiate therapy with peginterferon alfa and ribavirin for 4 weeks, then
Add boceprevir 800 mg PO q8hr with food.
Renal or Hepatic Impairment
No dose adjustment for boceprevir is required
See peginterferon alfa and ribavirin monographs for recommended dose adjustments
Must be administered in combination with peginterferon alfa and ribavirin
Administer with a meal.
Side effectsanemia , Diarrhea , Headache , nausea , vomiting , rash , vertigo , Chills , anorexia , dry skin , tiredness , Restlessness
InteractionsMidazolam , Amiodarone , Erythromycin , Budesonide , Digoxin , Cisapride , Venlafaxine , eplerenone , Doxazosin , Ethinyl Estradiol , Alfentanil , nasal Mometasone , Maraviroc , Halofantrine , Fesoterodine , Alfuzosin , trabectedine , Duvelisib , Apalutamide , elagolix , Avanafil , Levomilnacipran , ELBASVIR/GRAZOPREVIR , Larotrectinib , gilteritinib , glasdegib , Eliglustat , Bepridil , Gefitinib , Dasatinib , voxelotor , Fidaxomicin , Capmatinib , Dienestrol
Concerns related to adverse effects:
Anemia: Has been reported with peginterferon alfa and ribavirin; addition of boceprevir is associated with further hemoglobin decreases.
Hypersensitivity: Serious acute hypersensitivity reactions (eg, angioedema, urticaria) have been reported with boceprevir, peginterferon alfa, and ribavirin combination therapy. Discontinuation of combination therapy and institution of supportive measures may be necessary.
Pancytopenia: Serious cases have been reported in patients receiving boceprevir in combination with peginterferon alfa and ribavirin. Complete blood counts with differential should be obtained at pretreatment, and at weeks 2, 4, 8, and 12, as well as other time points during treatment.
Pregnancy: Combination therapy with ribavirin and interferons may cause birth defects; avoid pregnancy in females and female partners of male patients during therapy and for 6 months following treatment; two forms of effective contraception should be used. Combination therapy with ribavirin and peginterferon alfa-2a is contraindicated in pregnancy.
Points of recommendation
Patient may experience headache, change in taste, hair loss, diarrhea, lack of appetite, dry mouth, dry skin, joint pain, nausea, vomiting, or insomnia. Have patient report immediately to prescriber signs of infection, signs of bleeding, severe loss of strength and energy, pale skin, severe dizziness, passing out, or shortness of breath.