Identification
NamePeginterferon alfa-2a
Accession NumberDB00008  (BTD00043, BIOD00043)
TypeBiotech
GroupsApproved, Investigational
Description

Peginterferon alfa-2a is a form of recombinant interferon 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 [3]. Treatment options for chronic Hepatitis C have advanced significantly since 2011, with the development of Direct Acting Antivirals (DAAs) resulting in less use of Peginterferon alfa-2a. Peginterferon alfa-2a is derived from the alfa-2a moeity of recombinant human interferon and acts by binding to human type 1 interferon receptors. Activation and dimerization of this receptor induces the body's innate antiviral response by activating the janus kinase/signal transducer and activator of transcription (JAK/STAT) pathway. Use of Peginterferon alfa-2a is associated with a wide range of severe adverse effects including the aggravation and development of endocrine and autoimmune disorders, retinopathies, cardiovascular and neuropsychiatric complications, and increased risk of hepatic decompensation in patients with cirrhosis. The use of Peginterferon alfa-2a has largely declined since newer interferon-free antiviral therapies have been developed.

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) no longer recommend Peginterferon alfa-2a for the treatment of Hepatitis C [1]. Peginterferon alfa-2a was used alongside Ribavirin with the intent to cure, or achieve a sustained virologic response (SVR), after 48 weeks of 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 [2].

Peginterferon alfa-2a is available as a fixed dose injector (tradename Pegasys) used for the treatment of chronic Hepatitis C. Approved in 2002 by the FDA, Pegasys is indicated for the treatment of HCV with Ribavirin or other antiviral drugs [FDA Label]. When combined together, Peginterferon alfa-2a and Ribavirin have been shown to achieve a SVR between 36% for genotype 1 and 59% for genotypes 2-6 after 48 weeks of treatment.

Protein structureDb00008
Related Articles
Protein chemical formulaNot Available
Protein average weight60000.0 Da
Sequences
>Peginterferon alfa-2a sequence
CDLPQTHSLGSRRTLMLLAQMRRISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMI
QQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMKEDSILAVR
KYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE
Download FASTA Format
Synonyms
Pegylated interferon alfa-2a
Pegylated interferon alpha2a
External IDs Not Available
Product Ingredients Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
PegasysInjection, solution180 ug/mLSubcutaneousGenentech, Inc.2002-10-16Not applicableUs
PegasysInjection, solution180 μgSubcutaneousRoche Registration Limited2002-06-20Not applicableEu
PegasysInjection, solution180 μgSubcutaneousRoche Registration Limited2002-06-20Not applicableEu
PegasysInjection, solution180 μgSubcutaneousRoche Registration Limited2002-06-20Not applicableEu
PegasysInjection, solution135 μgSubcutaneousRoche Registration Limited2002-06-20Not applicableEu
PegasysInjection, solution180 ug/.5mLSubcutaneousGenentech, Inc.2011-11-01Not applicableUs
PegasysInjection, solution180 μgSubcutaneousRoche Registration Limited2002-06-20Not applicableEu
PegasysInjection, solution135 μgSubcutaneousRoche Registration Limited2002-06-20Not applicableEu
PegasysInjection, solution135 μgSubcutaneousRoche Registration Limited2002-06-20Not applicableEu
PegasysInjection, solution180 ug/.5mLSubcutaneousGenentech, Inc.2011-03-29Not applicableUs
PegasysInjection, solution180 μgSubcutaneousRoche Registration Limited2002-06-20Not applicableEu
PegasysInjection, solution180 μgSubcutaneousRoche Registration Limited2002-06-20Not applicableEu
PegasysInjection, solution180 μgSubcutaneousRoche Registration Limited2002-06-20Not applicableEu
PegasysSolution180 mcgSubcutaneousHoffmann La Roche2003-08-14Not applicableCanada
PegasysInjection, solution135 μgSubcutaneousRoche Registration Limited2002-06-20Not applicableEu
PegasysInjection, solution135 μgSubcutaneousRoche Registration Limited2002-06-20Not applicableEu
PegasysInjection, solution180 μgSubcutaneousRoche Registration Limited2002-06-20Not applicableEu
PegasysInjection, solution135 μgSubcutaneousRoche Registration Limited2002-06-20Not applicableEu
PegasysInjection, solution90 μgSubcutaneousRoche Registration Limited2002-06-20Not applicableEu
PegasysInjection, solution135 ug/.5mLSubcutaneousGenentech, Inc.2011-11-01Not applicableUs
PegasysInjection, solution135 μgSubcutaneousRoche Registration Limited2002-06-20Not applicableEu
PegasysSolution180 mcgSubcutaneousHoffmann La Roche2003-08-14Not applicableCanada
PegasysInjection, solution135 μgSubcutaneousRoche Registration Limited2002-06-20Not applicableEu
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
Pegasys RbvHoffmann La Roche
Categories
UNIIQ46947FE7K
CAS number198153-51-4
Pharmacology
Indication

Peginterferon alfa-2a is indicated for the treatment of HCV in combination with other antiviral drugs in patients over 5 years of age with compensated liver disease [FDA Label]. May be used as a monotherapy in patients with contraindications to or significant intolerance to other anti-viral therapies.

Peginterferon alfa-2a is also indicated as a monotherapy for adult patients with HBeAg positive and HBeAg negative chronic hepatitis B infection who have compensated liver disease and evidence of viral replication and liver inflammation [FDA Label].

Structured Indications
Pharmacodynamics

Peginterferon alfa-2a induces the body's innate antiviral response [FDA Label].

Mechanism of action

Peginterferon alfa-2a is derived from recombinant human interferon's alfa-2a moeity [FDA Label]. It binds to and activates human type 1 interferon receptors causing them to dimerize. This activates the JAK/STAT pathway. Activation of the JAK/STAT pathway increases expression of multiple genes in multiple tissues involved in the innate antiviral response.

TargetKindPharmacological actionActionsOrganismUniProt ID
Interferon alpha/beta receptor 2Proteinyes
agonist
HumanP48551 details
Interferon alpha/beta receptor 1Proteinyes
agonist
HumanP17181 details
Related Articles
Absorption

Peginterferon alfa-2a reaches peak plasma concentration 72-96 hours after subcutaneous administration [FDA Label]. Trough concentrations at week 48 are approximately 2 fold higher than week 1. The peak to trough ratio at week 48 is 2.

Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half life

The mean terminal half-life of peginterferon alfa-2a is 164 in a range of 84-353 hours [FDA Label].

Clearance

The mean systemic clearance of peginterferon alfa-2a is 94 milliliters per hour [FDA Label].

Toxicity

Peginterferon alfa-2a may manifest neuropsychiatric complications include suicide, suicidal ideation, homicidal ideation, depression, relapse of drug addiction, and drug overdose [FDA Label]. Hypertension, supraventricular arrhythmias, chest pain, and myocardial infarction have been observed in patients using Peginterferon alfa-2a. Peginterferon alfa-2a may produce myelosuppression as well as the development or aggravation of autoimmune disorders including myositis, hepatitis, thrombotic thrombocytopenic purpura, idiopathic thrombocytopenic purpura, psoriasis, rheumatoid arthritis, interstitial nephritis, thyroiditis, and systemic lupus erythematosus. Peginterferon alfa-2a causes or aggravates hypothyroidism and hyperthyroidism. Hyperglycemia, hypoglycemia, and diabetes mellitus have been observed to develop in patients treated with Peginterferon alfa-2a. Peginterferon alfa-2a may decrease or produce loss of vision, retinopathy including macular edema, retinal artery or vein thrombosis, retinal hemorrhages and cotton wool spots, optic neuritis, papilledema and serous retinal detachment. Peginterferon mayy be related to increased ischemic and hemorrhagic cerebrovascular events. Patients with cirrhosis on Peginterferon alfa-2a are at risk of hepatic decompensation. Dyspnea, pulmonary infiltrates, pneumonia, bronchiolitis obliterans, interstitial pneumonitis, pulmonary hypertension and sarcoidosis may be induced or aggravated by Peginterferon alfa-2a. Serious and severe infections (bacterial, viral, or fungal) have been reported during treatment with Peginterferon alfa-2a. Ulcerative and hemorrhagic/ischemic colitis have been observed within 12 weeks of starting Peginterferon alfa-2a treatment. Pancreatitis and peripheral nephropathy have also been reported. Peginterferon alfa-2a is associated with growth inhibition in pediatric patients. Use of Peginterferon alfa-2a while pregant may result in delopmental abnormalities or death of the fetus.

Affected organisms
  • Humans and other mammals
PathwaysNot Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Interferon lambda-3---(T;T) / (C;T) / (G;G) / (G;T)C > T / T > G Effect Directly StudiedLower odds of response Details
Interactions
Drug Interactions
DrugInteractionDrug group
AldesleukinThe risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Aldesleukin.Approved
Ambroxol acefyllinateThe metabolism of Ambroxol acefyllinate can be decreased when combined with Peginterferon alfa-2a.Experimental
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Peginterferon alfa-2a.Approved
BCG vaccineThe therapeutic efficacy of Bcg can be decreased when used in combination with Peginterferon alfa-2a.Investigational
ClozapineThe risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Clozapine.Approved
DyphyllineThe metabolism of Dyphylline can be decreased when combined with Peginterferon alfa-2a.Approved
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Peginterferon alfa-2a.Withdrawn
MethadoneThe serum concentration of Methadone can be increased when it is combined with Peginterferon alfa-2a.Approved
PegloticaseThe therapeutic efficacy of Peginterferon alfa-2a can be decreased when used in combination with Pegloticase.Approved
RibavirinThe risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Ribavirin.Approved
TelbivudineThe risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Telbivudine.Approved, Investigational
TheophyllineThe metabolism of Theophylline can be decreased when combined with Peginterferon alfa-2a.Approved
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Peginterferon alfa-2a.Approved
ZidovudineThe risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Zidovudine.Approved
Food Interactions
  • Recommended adequate hydration.
References
Synthesis ReferenceNot Available
General References
  1. Bagaglio S, Uberti-Foppa C, Morsica G: Resistance Mechanisms in Hepatitis C Virus: implications for Direct-Acting Antiviral Use. Drugs. 2017 May 12. doi: 10.1007/s40265-017-0753-x. [PubMed:28497432 ]
  2. Myers RP, Shah H, Burak KW, Cooper C, Feld JJ: An update on the management of chronic hepatitis C: 2015 Consensus guidelines from the Canadian Association for the Study of the Liver. Can J Gastroenterol Hepatol. 2015 Jan-Feb;29(1):19-34. Epub 2015 Jan 13. [PubMed:25585348 ]
  3. American Association for the Study of Liver Diseases; Infectious Diseases Society of America. HCV guidance. http://hcvguidelines.org. Accessed June 12, 2017. [Link]
External Links
ATC CodesL03AB61 — Peginterferon alfa-2a, combinationsL03AB11 — Peginterferon alfa-2a
AHFS Codes
  • 08:18.20
PDB Entries
FDA labelDownload (1.13 MB)
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
0TerminatedTreatmentChronic Hepatitis C Virus (HCV) Infection / Genotype 1 / Relapses1
1Active Not RecruitingTreatmentChronic Hepatitis B Infection2
1CompletedNot AvailableHealthy Volunteers1
1CompletedBasic ScienceChronic Hepatitis C Infection / Healthy Volunteers1
1CompletedTreatmentChronic Viral Hepatitis C1
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentHepatitis B,Chronic2
1CompletedTreatmentHepatitis C, Chronic2
1RecruitingTreatmentEssential Thrombocythemia (ET) / Polycythemia Vera (PV)1
1RecruitingTreatmentHealthy Volunteers1
1RecruitingTreatmentSolid Cancers1
1, 2CompletedTreatmentChronic Hepatitis B Infection1
1, 2CompletedTreatmentChronic Hepatitis C Infection2
1, 2CompletedTreatmentChronic Hepatitis C Infection / Genotype 11
1, 2CompletedTreatmentChronic Hepatitis C Infection / HIV Disease1
1, 2CompletedTreatmentHepatitis B,Chronic1
1, 2Not Yet RecruitingTreatmentChronic Hepatitis B Infection2
1, 2RecruitingTreatmentAcute Myeloid Leukaemias (AML)1
1, 2RecruitingTreatmentAgnogenic Myeloid Metaplasia1
1, 2RecruitingTreatmentHuman Immunodeficiency Virus (HIV) Infections1
1, 2TerminatedTreatmentChronic Hepatitis B Infection1
1, 2Unknown StatusTreatmentChronic Hepatitis B Infection1
1, 2Unknown StatusTreatmentChronic Hepatitis C Virus (HCV) Infection1
1, 2Unknown StatusTreatmentChronic Hepatitis C Virus Genotype I1
1, 2WithdrawnTreatmentChronic Lymphocytic Leukaemia (CLL)1
2Active Not RecruitingTreatmentAgnogenic Myeloid Metaplasia1
2Active Not RecruitingTreatmentChronic Hepatitis B Infection2
2Active Not RecruitingTreatmentHepatitis D1
2Active Not RecruitingTreatmentMyeloproliferative Disorders1
2Active Not RecruitingTreatmentSquamous Cell Carcinoma (SCC) / Squamous Cell Carcinoma of Skin1
2CompletedNot AvailableChronic Hepatitis C Infection1
2CompletedDiagnosticHCV-HIV Co-Infection1
2CompletedTreatmentBlast Crisis / Leukemia, Lymphocytic, Acute / Leukemia,Myeloid, Chronic / Philadelphia Chromosome1
2CompletedTreatmentChronic Hepatitis B Infection1
2CompletedTreatmentChronic Hepatitis C Infection9
2CompletedTreatmentChronic Hepatitis C Infection / Hemophilia / Human Immunodeficiency Virus (HIV) Infections1
2CompletedTreatmentChronic Hepatitis C Infection / Hepatitis1
2CompletedTreatmentChronic Hepatitis C Infection / Hepatitis C Chronic1
2CompletedTreatmentChronic Hepatitis C Infection / Human Immunodeficiency Virus (HIV) Infections3
2CompletedTreatmentChronic Hepatitis C Infection / Human Immunodeficiency Virus (HIV) Infections / Liver Diseases1
2CompletedTreatmentChronic Hepatitis C Infection / Pain, Chronic1
2CompletedTreatmentChronic Hepatitis C Infection / Thalassaemic disorders1
2CompletedTreatmentChronic Hepatitis C Virus1
2CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection13
2CompletedTreatmentChronic Hepatitis D Infection1
2CompletedTreatmentGenotype 1 Chronic Hepatitis C1
2CompletedTreatmentGliomas1
2CompletedTreatmentHCV Infections1
2CompletedTreatmentHepatitis B Virus (HBV)1
2CompletedTreatmentHepatitis B,Chronic2
2CompletedTreatmentHepatitis C Infection3
2CompletedTreatmentHepatitis C Infection / Human Immunodeficiency Virus (HIV) Infections1
2CompletedTreatmentHepatitis C Virus (HCV)6
2CompletedTreatmentHepatitis C Virus (HCV) / Hepatitis C Virus Infection1
2CompletedTreatmentHepatitis C, Chronic25
2CompletedTreatmentHepatitis D, Chronic1
2CompletedTreatmentHepatocellular,Carcinoma1
2CompletedTreatmentHigh Risk Essential Thrombocythemia / High Risk Polycythemia Vera1
2CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections2
2Not Yet RecruitingTreatmentHepatitis B,Chronic1
2RecruitingTreatmentChronic Hepatitis B Infection1
2RecruitingTreatmentChronic Hepatitis C Infection1
2RecruitingTreatmentChronic Hepatitis D Infection1
2TerminatedTreatmentCancer, Breast / Metastatic Cancers1
2TerminatedTreatmentChronic Hepatitis C Infection3
2TerminatedTreatmentHepatitis C Infection / Thrombocytopenias1
2TerminatedTreatmentHepatitis D / Viral Hepatitis B1
2TerminatedTreatmentLeukemias1
2Unknown StatusTreatmentHepatitis C, Chronic2
2WithdrawnTreatmentChronic Hepatitis C Infection / Hepatitis C Virus (HCV)1
2WithdrawnTreatmentChronic Hepatitis C Virus Genotype 11
2WithdrawnTreatmentHepatitis C, Chronic1
2, 3CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection2
2, 3CompletedTreatmentChronic Myelogenous Leukemia (CML) / Malignant Melanoma / Renal Cell Adenocarcinoma1
2, 3CompletedTreatmentHepatitis C Virus (HCV) / Human Immunodeficiency Virus (HIV) Infections / Liver Cirrhosis1
2, 3CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Viral Hepatitis B1
2, 3RecruitingTreatmentCarrier of Viral Hepatitis Type B / Chronic Hepatitis, B Virus1
2, 3Unknown StatusTreatmentChronic Hepatitis C Virus (HCV) Infection1
2, 3Unknown StatusTreatmentChronic Hepatitis C Virus (HCV) Infection / Insulin Resistance1
2, 3WithdrawnTreatmentChronic Hepatitis C Infection1
3Active Not RecruitingTreatmentChronic Hepatitis C Infection / Hepatitis1
3Active Not RecruitingTreatmentEssential Thrombocythemia (ET) / Polycythemia Vera (PV) / Primary Myelofibrosis1
3Active Not RecruitingTreatmentHepatitis B,Chronic1
3Active Not RecruitingTreatmentHepatitis D, Chronic1
3Active Not RecruitingTreatmentHigh Risk Essential Thrombocythemia / High Risk Polycythemia Vera1
3CompletedPreventionChronic Hepatitis C Virus (HCV) Infection / Fibrosis, Liver / Hepatic Cirrhosis / Liver Cirrhosis1
3CompletedPreventionDepressive State1
3CompletedTreatmentAntiviral Treatment of Chronic Hepatitis B1
3CompletedTreatmentChronic Hepatitis B Infection2
3CompletedTreatmentChronic Hepatitis C Infection13
3CompletedTreatmentChronic Hepatitis C Infection / Coinfection / Human Immunodeficiency Virus (HIV) Infections1
3CompletedTreatmentChronic Hepatitis C Infection / Hepatitis C, Chronic2
3CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection11
3CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Liver Cirrhosis1
3CompletedTreatmentGenotype 1 Chronic Hepatitis C / Treatment Naive1
3CompletedTreatmentHCV Infections / Hepatitis C, Chronic1
3CompletedTreatmentHepatitis B,Chronic3
3CompletedTreatmentHepatitis C Virus (HCV)5
3CompletedTreatmentHepatitis C, Chronic10
3CompletedTreatmentHepatitis C, Chronic / Human Immunodeficiency Virus (HIV) Infections1
3CompletedTreatmentHepatitis C, Chronic / Infection NOS1
3CompletedTreatmentHepatitis C, Genotype 11
3CompletedTreatmentHepatitis D, Chronic1
3CompletedTreatmentMyelogenous Leukemia, Chronic1
3RecruitingTreatmentChronic Myeloid Leukemia (CML)2
3RecruitingTreatmentHepatitis B,Chronic1
3TerminatedTreatmentChronic Hepatitis B Infection / Human Immunodeficiency Virus (HIV) Infections1
3TerminatedTreatmentChronic Hepatitis C Infection2
3TerminatedTreatmentChronic Hepatitis C Infection / Liver Diseases1
3TerminatedTreatmentChronic Hepatitis C Virus (HCV) Infection1
3TerminatedTreatmentHIV/HCV Coinfection1
3TerminatedTreatmentHepatitis B,Chronic1
3TerminatedTreatmentHepatitis C, Chronic2
3TerminatedTreatmentViral Hepatitis B1
3Unknown StatusTreatmentChronic Hepatitis B Infection2
3Unknown StatusTreatmentChronic Hepatitis C Virus (HCV) Infection1
3WithdrawnTreatmentChronic Hepatitis C Infection1
3WithdrawnTreatmentChronic Hepatitis C Virus (HCV) Infection1
3WithdrawnTreatmentHepatitis C Virus (HCV)1
3WithdrawnTreatmentHepatitis C, Chronic1
4Active Not RecruitingTreatmentChronic Hepatitis B Infection2
4Active Not RecruitingTreatmentHepatitis B,Chronic1
4Active Not RecruitingTreatmentViral Hepatitis B1
4CompletedNot AvailableHepatitis B,Chronic1
4CompletedNot AvailableHepatitis, Viral, Non-A, Non-B, Parenterally-Transmitted1
4CompletedBasic ScienceHepatitis C, Chronic / Liver Diseases / Virus Diseases1
4CompletedDiagnosticChronic Hepatitis C Virus (HCV) Infection1
4CompletedPreventionChronic Hepatitis C Infection / Transplantation, Liver1
4CompletedTreatmentAcute Hepatitis C2
4CompletedTreatmentAnemias1
4CompletedTreatmentAntiviral Agents / Chronic Liver Diseases (CLD) / Hepatitis C Virus (HCV) / Therapeutic Uses / Virus Hepatitis1
4CompletedTreatmentAsian Americans / Chronic Hepatitis C Virus (HCV) Infection / Novel Genotypes / Treatments1
4CompletedTreatmentChronic Hepatitis B Infection2
4CompletedTreatmentChronic Hepatitis C Infection6
4CompletedTreatmentChronic Hepatitis C Infection / Fatty Liver1
4CompletedTreatmentChronic Hepatitis C Infection / Human Immunodeficiency Virus (HIV) Infections2
4CompletedTreatmentChronic Hepatitis C Infection / Human Immunodeficiency Virus (HIV) / Human Immunodeficiency Virus (HIV) Infections1
4CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection9
4CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / End Stage Renal Disease (ESRD)1
4CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Genotyping1
4CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Neoplasms1
4CompletedTreatmentChronic Hepatitis C, Genotype 11
4CompletedTreatmentHepatitis C, Chronic / HIV Disease1
4CompletedTreatmentHepatitis B,Chronic13
4CompletedTreatmentHepatitis C, Chronic25
4CompletedTreatmentHepatitis C, Chronic / Human Immunodeficiency Virus (HIV) Infections1
4CompletedTreatmentIL28B Polymorphism / Sustained Virologic Response1
4Not Yet RecruitingTreatmentViral Hepatitis B1
4RecruitingPreventionChronic Hepatitis B Infection1
4RecruitingTreatmentChronic Hepatitis B Infection8
4RecruitingTreatmentChronic Hepatitis C Infection1
4RecruitingTreatmentFibrosis, Liver1
4RecruitingTreatmentHepatitis, Chronic1
4TerminatedTreatmentChronic Hepatitis C Infection2
4TerminatedTreatmentChronic Hepatitis C Infection / Fatty Liver1
4TerminatedTreatmentChronic Hepatitis C Virus (HCV) Infection1
4Unknown StatusTreatmentChronic Hepatitis C Infection1
4Unknown StatusTreatmentChronic Hepatitis C Virus (HCV) Infection3
4Unknown StatusTreatmentChronic Hepatitis C Virus (HCV) Infection / Co-Infection HIV-HCV1
4Unknown StatusTreatmentChronic Hepatitis C Virus (HCV) Infection / Hepatocellular,Carcinoma1
4Unknown StatusTreatmentHepatitis B,Chronic2
4WithdrawnTreatmentChronic Hepatitis C Infection1
4WithdrawnTreatmentHepatitis B,Chronic1
Not AvailableActive Not RecruitingNot AvailableChronic Hepatitis B (HBeAg-negative)1
Not AvailableActive Not RecruitingNot AvailableHepatitis B,Chronic1
Not AvailableActive Not RecruitingTreatmentViral Hepatitis B1
Not AvailableCompletedNot AvailableChronic Hepatitis B Infection1
Not AvailableCompletedNot AvailableChronic Hepatitis C Infection2
Not AvailableCompletedNot AvailableChronic Hepatitis C Infection / HIV Disease / Infection NOS1
Not AvailableCompletedNot AvailableChronic Hepatitis C Infection / Hepatitis C, Chronic1
Not AvailableCompletedNot AvailableChronic Hepatitis C Virus (HCV) Infection2
Not AvailableCompletedNot AvailableCognition Disorders / Fatigue Syndrome, Chronic / Hepatitis C, Chronic / Major Depressive Disorder (MDD)1
Not AvailableCompletedNot AvailableHepatitis B,Chronic4
Not AvailableCompletedNot AvailableHepatitis C, Chronic11
Not AvailableCompletedBasic ScienceChronic Hepatitis C Virus (HCV) Infection / Human Immunodeficiency Virus (HIV)1
Not AvailableCompletedTreatmentChronic Hepatitis B Infection1
Not AvailableCompletedTreatmentChronic Hepatitis C Infection / Human Immunodeficiency Virus (HIV) Infections1
Not AvailableCompletedTreatmentChronic Hepatitis C Virus (HCV) Infection1
Not AvailableNo Longer AvailableNot AvailableHepatitis C, Chronic1
Not AvailableNot Yet RecruitingNot AvailableChronic Hepatitis B Infection1
Not AvailableRecruitingNot AvailableViral Hepatitis B1
Not AvailableRecruitingTreatmentChronic Hepatitis B Infection2
Not AvailableTerminatedNot AvailableHepatitis C, Chronic2
Not AvailableTerminatedTreatmentChronic Hepatitis C Virus (HCV) Infection1
Not AvailableUnknown StatusBasic ScienceChronic HCV Infection / Nonalcoholic Steatohepatitis1
Not AvailableUnknown StatusTreatmentViral Hepatitis B1
Not AvailableWithdrawnBasic ScienceChronic Hepatitis C Infection1
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, solutionSubcutaneous135 μg
Injection, solutionSubcutaneous135 ug/.5mL
Injection, solutionSubcutaneous180 ug/mL
Injection, solutionSubcutaneous180 ug/.5mL
Injection, solutionSubcutaneous180 μg
Injection, solutionSubcutaneous90 μg
SolutionSubcutaneous180 mcg
Solution; tabletOral; Subcutaneous
Prices
Unit descriptionCostUnit
Pegasys (1 Kit = Four 180 mcg/ml Vials Prefilled Syringes) Box2634.53USD box
Pegasys 180 mcg/0.5 ml conv.pk2533.2USD each
Pegasys 180 mcg/ml vial642.64USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2172664 No2000-10-032016-03-26Canada
CA2203480 No2009-06-302017-04-23Canada
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point (°C)61 °CBeldarrain, A. et al., Biochemistry 38:7865-7873 (1999)
isoelectric point5.99Not Available
Taxonomy
DescriptionNot Available
KingdomOrganic Compounds
Super ClassOrganic Acids
ClassCarboxylic Acids and Derivatives
Sub ClassAmino Acids, Peptides, and Analogues
Direct ParentPeptides
Alternative ParentsNot Available
SubstituentsNot Available
Molecular FrameworkNot Available
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Type i interferon receptor activity
Specific Function:
Associates with IFNAR1 to form the type I interferon receptor. Receptor for interferons alpha and beta. Involved in IFN-mediated STAT1, STAT2 and STAT3 activation. Isoform 1 and isoform 2 are directly involved in signal transduction due to their association with the TYR kinase, JAK1. Isoform 3 is a potent inhibitor of type I IFN receptor activity.
Gene Name:
IFNAR2
Uniprot ID:
P48551
Uniprot Name:
Interferon alpha/beta receptor 2
Molecular Weight:
57758.24 Da
References
  1. Dhalluin C, Ross A, Huber W, Gerber P, Brugger D, Gsell B, Senn H: Structural, kinetic, and thermodynamic analysis of the binding of the 40 kDa PEG-interferon-alpha2a and its individual positional isomers to the extracellular domain of the receptor IFNAR2. Bioconjug Chem. 2005 May-Jun;16(3):518-27. [PubMed:15898717 ]
  2. Yano H, Ogasawara S, Momosaki S, Akiba J, Kojiro S, Fukahori S, Ishizaki H, Kuratomi K, Basaki Y, Oie S, Kuwano M, Kojiro M: Growth inhibitory effects of pegylated IFN alpha-2b on human liver cancer cells in vitro and in vivo. Liver Int. 2006 Oct;26(8):964-75. [PubMed:16953837 ]
  3. Ishii K, Shinohara M, Sawa M, Kogame M, Higami K, Sano M, Morita T, Sumino Y: Interferon alpha receptor 2 expression by peripheral blood monocytes in patients with a high viral load of hepatitis C virus genotype 1 showing substitution of amino Acid 70 in the core region. Intervirology. 2010;53(2):105-10. doi: 10.1159/000264200. Epub 2009 Dec 3. [PubMed:19955815 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Type i interferon receptor activity
Specific Function:
Associates with IFNAR2 to form the type I interferon receptor. Receptor for interferons alpha and beta. Binding to type I IFNs triggers tyrosine phosphorylation of a number of proteins including JAKs, TYK2, STAT proteins and IFNR alpha- and beta-subunits themselves. Can also transduce IFNB signals without the help of IFNAR2, and not activating the Jak-STAT pathway.
Gene Name:
IFNAR1
Uniprot ID:
P17181
Uniprot Name:
Interferon alpha/beta receptor 1
Molecular Weight:
63524.81 Da
References
  1. Dhalluin C, Ross A, Huber W, Gerber P, Brugger D, Gsell B, Senn H: Structural, kinetic, and thermodynamic analysis of the binding of the 40 kDa PEG-interferon-alpha2a and its individual positional isomers to the extracellular domain of the receptor IFNAR2. Bioconjug Chem. 2005 May-Jun;16(3):518-27. [PubMed:15898717 ]
  2. Yano H, Ogasawara S, Momosaki S, Akiba J, Kojiro S, Fukahori S, Ishizaki H, Kuratomi K, Basaki Y, Oie S, Kuwano M, Kojiro M: Growth inhibitory effects of pegylated IFN alpha-2b on human liver cancer cells in vitro and in vivo. Liver Int. 2006 Oct;26(8):964-75. [PubMed:16953837 ]
  3. Ishii K, Shinohara M, Sawa M, Kogame M, Higami K, Sano M, Morita T, Sumino Y: Interferon alpha receptor 2 expression by peripheral blood monocytes in patients with a high viral load of hepatitis C virus genotype 1 showing substitution of amino Acid 70 in the core region. Intervirology. 2010;53(2):105-10. doi: 10.1159/000264200. Epub 2009 Dec 3. [PubMed:19955815 ]
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Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Uniprot Name:
Cytochrome P450 1A2
Molecular Weight:
58293.76 Da
Drug created on June 13, 2005 07:24 / Updated on July 11, 2017 16:38