Identification

Name
Peginterferon alfa-2a
Accession Number
DB00008  (BTD00043, BIOD00043)
Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Interferons
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 [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 structure
Db00008
Protein chemical formula
Not Available
Protein average weight
60000.0 Da
Sequences
>Peginterferon alfa-2a sequence
CDLPQTHSLGSRRTLMLLAQMRRISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMI
QQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMKEDSILAVR
KYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE
Download FASTA Format
Synonyms
  • Pegylated interferon alfa-2a
  • Pegylated interferon alpha2a
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
PegasysInjection, solution180 μgSubcutaneousRoche Registration Gmb H2002-06-20Not applicableEu
PegasysInjection, solution180 μgSubcutaneousRoche Registration Gmb H2002-06-20Not applicableEu
PegasysInjection, solution135 μgSubcutaneousRoche Registration Gmb H2002-06-20Not applicableEu
PegasysSolution180 mcgSubcutaneousHoffmann La Roche2003-08-14Not applicableCanada
PegasysInjection, solution135 μgSubcutaneousRoche Registration Gmb H2002-06-20Not applicableEu
PegasysInjection, solution180 μgSubcutaneousRoche Registration Gmb H2002-06-20Not applicableEu
PegasysInjection, solution135 ug/0.5mLSubcutaneousGenentech, Inc.2011-11-012019-01-31Us
PegasysSolution180 mcgSubcutaneousHoffmann La Roche2003-08-142017-07-27Canada
PegasysInjection, solution135 μgSubcutaneousRoche Registration Gmb H2002-06-20Not applicableEu
PegasysInjection, solution135 μgSubcutaneousRoche Registration Gmb H2002-06-20Not applicableEu
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Pegasys RbvPeginterferon alfa-2a (180 mcg) + Ribavirin (200 mg)Solution; TabletOral; SubcutaneousHoffmann La Roche2004-05-26Not applicableCanada
Pegasys RbvPeginterferon alfa-2a (180 mcg) + Ribavirin (200 mg)Solution; TabletOral; SubcutaneousHoffmann La Roche2004-05-26Not applicableCanada
Categories
UNII
Q46947FE7K
CAS number
198153-51-4

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 [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 [Label].

Associated Conditions
Pharmacodynamics

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

Mechanism of action

Peginterferon alfa-2a is derived from recombinant human interferon's alfa-2a moeity [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.

TargetActionsOrganism
AInterferon alpha/beta receptor 2
agonist
Human
AInterferon alpha/beta receptor 1
agonist
Human
Absorption

Peginterferon alfa-2a reaches peak plasma concentration 72-96 hours after subcutaneous administration [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 distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life

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

Clearance

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

Toxicity

Peginterferon alfa-2a may manifest neuropsychiatric complications include suicide, suicidal ideation, homicidal ideation, depression, relapse of drug addiction, and drug overdose [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
Pathways
Not 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 > TEffect Directly StudiedPatients with this genotype in IFNL3 have a reduced likelihood of achieving sustained virologic response to peginterferon alfa-2a therapy.Details

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Peginterferon alfa-2a.
(S)-WarfarinThe risk or severity of bleeding can be increased when (S)-Warfarin is combined with Peginterferon alfa-2a.
2-MethoxyethanolThe risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with 2-Methoxyethanol.
3-isobutyl-1-methyl-7H-xanthineThe metabolism of 3-isobutyl-1-methyl-7H-xanthine can be decreased when combined with Peginterferon alfa-2a.
4-hydroxycoumarinThe risk or severity of bleeding can be increased when 4-hydroxycoumarin is combined with Peginterferon alfa-2a.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Peginterferon alfa-2a.
7-DeazaguanineThe metabolism of 7-Deazaguanine can be decreased when combined with Peginterferon alfa-2a.
7,9-DimethylguanineThe metabolism of 7,9-Dimethylguanine can be decreased when combined with Peginterferon alfa-2a.
8-azaguanineThe metabolism of 8-azaguanine can be decreased when combined with Peginterferon alfa-2a.
8-chlorotheophyllineThe metabolism of 8-chlorotheophylline can be decreased when combined with Peginterferon alfa-2a.
Food Interactions
  • Recommended adequate hydration.

References

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
UniProt
P01563
Genbank
J00207
PubChem Substance
46504860
ChEMBL
CHEMBL1201560
Therapeutic Targets Database
DAP001278
PharmGKB
PA164749390
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Peginterferon_alfa-2a
ATC Codes
L03AB61 — Peginterferon alfa-2a, combinationsL03AB11 — Peginterferon alfa-2a
AHFS Codes
  • 08:18.20 — Interferons
FDA label
Download (1.13 MB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0TerminatedTreatmentChronic Hepatitis C Virus (HCV) Infection / Genotype 1 / Relapses1
1Active Not RecruitingTreatmentEssential Thrombocythemia (ET) / Polycythemia Vera (PV)1
1Active Not RecruitingTreatmentSolid Cancers1
1CompletedNot AvailableHealthy Volunteers1
1CompletedBasic ScienceHealthy Volunteers / Hepatitis C Viral Infection1
1CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection3
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentHepatitis B Chronic Infection5
1RecruitingTreatmentHealthy Volunteers1
1RecruitingTreatmentHepatitis B Virus (HBV)1
1, 2CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Genotype 11
1, 2CompletedTreatmentChronic Hepatitis D Infection1
1, 2CompletedTreatmentHepatitis B Chronic Infection3
1, 2CompletedTreatmentHepatitis C Viral Infection2
1, 2CompletedTreatmentHepatitis C Viral Infection / Human Immunodeficiency Virus (HIV)1
1, 2Not Yet RecruitingTreatmentHepatitis B Chronic Infection1
1, 2RecruitingTreatmentAgnogenic Myeloid Metaplasia1
1, 2RecruitingTreatmentHuman Immunodeficiency Virus (HIV) Infections1
1, 2RecruitingTreatmentLeukemia Acute Myeloid Leukemia (AML)1
1, 2TerminatedTreatmentHepatitis B Chronic Infection1
1, 2Unknown StatusTreatmentChronic Hepatitis C Virus (HCV) Infection1
1, 2Unknown StatusTreatmentChronic Hepatitis C Virus Genotype I1
1, 2Unknown StatusTreatmentHepatitis B Chronic Infection1
1, 2WithdrawnTreatmentChronic Lymphocytic Leukaemia (CLL)1
2Active Not RecruitingTreatmentHepatitis B Chronic Infection1
2Active Not RecruitingTreatmentMyeloproliferative Disorders1
2Active Not RecruitingTreatmentSquamous Cell Carcinoma (SCC) / Squamous Cell Carcinoma of Skin1
2CompletedNot AvailableHepatitis C Viral Infection1
2CompletedDiagnosticHepatitis C Infection With HIV Co-Infection1
2CompletedTreatmentBlast Crisis / Chronic Myeloid Leukemia (CML) / Leukemia, Lymphocytic, Acute / Philadelphia Chromosome1
2CompletedTreatmentChronic Hepatitis C Virus1
2CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection41
2CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Hepatitis C Viral Infection1
2CompletedTreatmentChronic Hepatitis D Infection2
2CompletedTreatmentGenotype 1 Chronic Hepatitis C1
2CompletedTreatmentGliomas1
2CompletedTreatmentHemophilia / Hepatitis C Viral Infection / Human Immunodeficiency Virus (HIV) Infections1
2CompletedTreatmentHepatitis B Chronic Infection5
2CompletedTreatmentHepatitis B Virus (HBV)1
2CompletedTreatmentHepatitis C Infection3
2CompletedTreatmentHepatitis C Infection / Human Immunodeficiency Virus (HIV) Infections1
2CompletedTreatmentHepatitis C Viral Infection6
2CompletedTreatmentHepatitis C Viral Infection / Human Immunodeficiency Virus (HIV) Infections3
2CompletedTreatmentHepatitis C Viral Infection / Human Immunodeficiency Virus (HIV) Infections / Liver Diseases1
2CompletedTreatmentHepatitis C Viral Infection / Pain, Chronic1
2CompletedTreatmentHepatitis C Viral Infection / Thalassaemic disorders1
2CompletedTreatmentHepatitis C Virus (HCV) Infection7
2CompletedTreatmentHepatitis C Virus (HCV) Infection / Hepatitis C Virus Infection1
2CompletedTreatmentHepatitis D1
2CompletedTreatmentHepatitis D, Chronic1
2CompletedTreatmentHepatitis / Hepatitis C Viral Infection1
2CompletedTreatmentHepatocellular,Carcinoma1
2CompletedTreatmentHigh Risk Essential Thrombocythemia / High Risk Polycythemia Vera1
2CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections2
2RecruitingTreatmentChronic Hepatitis C Virus (HCV) Infection1
2RecruitingTreatmentChronic Viral Hepatitis B With Delta-agent1
2TerminatedTreatmentAgnogenic Myeloid Metaplasia1
2TerminatedTreatmentCancer, Breast / Metastatic Cancers1
2TerminatedTreatmentHepatitis C Infection / Thrombocytopenias1
2TerminatedTreatmentHepatitis C Viral Infection3
2TerminatedTreatmentHepatitis D / Viral Hepatitis B1
2TerminatedTreatmentLeukemias1
2Unknown StatusTreatmentChronic Hepatitis C Virus (HCV) Infection2
2WithdrawnTreatmentChronic Hepatitis C Virus (HCV) Infection1
2WithdrawnTreatmentChronic Hepatitis C Virus Genotype 11
2WithdrawnTreatmentHepatitis B Chronic Infection1
2WithdrawnTreatmentHepatitis C Viral Infection / Hepatitis C Virus (HCV) Infection1
2, 3CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection2
2, 3CompletedTreatmentHepatitis C Virus (HCV) Infection / Human Immunodeficiency Virus (HIV) Infections / Liver Cirrhosis1
2, 3CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Viral Hepatitis B1
2, 3CompletedTreatmentChronic Chronic myelogenous leukemia / Malignant Melanoma / Renal Cell Adenocarcinoma1
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, 3WithdrawnTreatmentHepatitis C Viral Infection1
3Active Not RecruitingTreatmentEssential Thrombocythemia (ET) / Polycythemia Vera (PV) / Primary Myelofibrosis1
3Active Not RecruitingTreatmentHepatitis B Chronic Infection1
3CompletedPreventionChronic Hepatitis C Virus (HCV) Infection / Fibrosis, Liver / Hepatic Cirrhosis / Liver Cirrhosis1
3CompletedPreventionDepression1
3CompletedTreatmentAntiviral Treatment of Chronic Hepatitis B1
3CompletedTreatmentChronic HCV Infection1
3CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection21
3CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Hepatitis C Viral Infection2
3CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Hepatitis C Virus (HCV) Infection1
3CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Human Immunodeficiency Virus (HIV) Infections1
3CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Infection NOS1
3CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Liver Cirrhosis1
3CompletedTreatmentCoinfection / Hepatitis C Viral Infection / Human Immunodeficiency Virus (HIV) Infections1
3CompletedTreatmentGenotype 1 Chronic Hepatitis C / Treatment Naive1
3CompletedTreatmentHepatitis B Chronic Infection5
3CompletedTreatmentHepatitis C Viral Infection14
3CompletedTreatmentHepatitis C Virus (HCV) Infection5
3CompletedTreatmentHepatitis C, Genotype 11
3CompletedTreatmentHepatitis D, Chronic2
3CompletedTreatmentHepatitis / Hepatitis C Viral Infection1
3CompletedTreatmentHigh Risk Essential Thrombocythemia / High Risk Polycythemia Vera1
3CompletedTreatmentChronic Chronic myelogenous leukemia1
3Not Yet RecruitingTreatmentHepatitis Delta Virus1
3RecruitingTreatmentChronic Myeloid Leukemia (CML)2
3RecruitingTreatmentHepatitis B Chronic Infection1
3TerminatedTreatmentChronic Hepatitis C Virus (HCV) Infection3
3TerminatedTreatmentHepatitis B Chronic Infection1
3TerminatedTreatmentHepatitis B Chronic Infection / Human Immunodeficiency Virus (HIV) Infections1
3TerminatedTreatmentHepatitis C Infection With HIV Co-Infection1
3TerminatedTreatmentHepatitis C Viral Infection2
3TerminatedTreatmentHepatitis C Viral Infection / Liver Diseases1
3TerminatedTreatmentViral Hepatitis B1
3Unknown StatusTreatmentChronic Hepatitis C Virus (HCV) Infection1
3Unknown StatusTreatmentHepatitis B Chronic Infection2
3WithdrawnTreatmentChronic Hepatitis C Virus (HCV) Infection2
3WithdrawnTreatmentHepatitis C Viral Infection1
3WithdrawnTreatmentHepatitis C Virus (HCV) Infection1
4Active Not RecruitingTreatmentHepatitis B Chronic Infection2
4Active Not RecruitingTreatmentViral Hepatitis B1
4CompletedNot AvailableHepatitis B Chronic Infection1
4CompletedNot AvailableHepatitis, Viral, Non-A, Non-B, Parenterally-Transmitted1
4CompletedBasic ScienceChronic Hepatitis C Virus (HCV) Infection / Liver Diseases / Virus Diseases1
4CompletedDiagnosticChronic Hepatitis C Virus (HCV) Infection1
4CompletedPreventionHepatitis C Viral Infection / Transplantation, Liver1
4CompletedTreatmentAnemias1
4CompletedTreatmentAntiviral Agents / Chronic Liver Diseases (CLD) / Hepatitis C Virus (HCV) Infection / Therapeutic Uses / Virus Hepatitis1
4CompletedTreatmentAsian Americans / Chronic Hepatitis C Virus (HCV) Infection / Novel Genotypes / Treatments1
4CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection35
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 / Human Immunodeficiency Virus (HIV)1
4CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Human Immunodeficiency Virus (HIV) Infections1
4CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection / Neoplasms1
4CompletedTreatmentChronic Hepatitis C, Genotype 11
4CompletedTreatmentFatty Liver / Hepatitis C Viral Infection1
4CompletedTreatmentFibrosis, Liver1
4CompletedTreatmentHepatitis B Chronic Infection16
4CompletedTreatmentHepatitis C Viral Infection6
4CompletedTreatmentHepatitis C Viral Infection / Human Immunodeficiency Virus (HIV) Infections2
4CompletedTreatmentHepatitis C Viral Infection / Human Immunodeficiency Virus (HIV) / Human Immunodeficiency Virus (HIV) Infections1
4CompletedTreatmentHepatitis C, Acute2
4CompletedTreatmentIL28B Polymorphism / Sustained Virologic Response1
4Not Yet RecruitingTreatmentViral Hepatitis B1
4RecruitingPreventionHepatitis B Chronic Infection1
4RecruitingTreatmentHepatic Carcinoma / Hepatitis B Chronic Infection1
4RecruitingTreatmentHepatitis B Chronic Infection8
4RecruitingTreatmentHepatitis, Chronic1
4TerminatedTreatmentChronic Hepatitis C Virus (HCV) Infection1
4TerminatedTreatmentChronic Hepatitis C Virus (HCV) Infection / Fatty Liver1
4TerminatedTreatmentHepatitis C Viral Infection2
4Unknown StatusTreatmentChronic Hepatitis C Virus (HCV) Infection3
4Unknown StatusTreatmentChronic Hepatitis C Virus (HCV) Infection / Hepatitis C Infection With HIV Co-Infection1
4Unknown StatusTreatmentChronic Hepatitis C Virus (HCV) Infection / Hepatocellular,Carcinoma1
4Unknown StatusTreatmentHepatitis B Chronic Infection2
4Unknown StatusTreatmentHepatitis C Viral Infection1
4WithdrawnTreatmentHepatitis B Chronic Infection1
4WithdrawnTreatmentHepatitis C Viral Infection1
Not AvailableActive Not RecruitingOtherChronic Hepatitis B (HBeAg-negative)1
Not AvailableActive Not RecruitingTreatmentViral Hepatitis B1
Not AvailableCompletedNot AvailableChronic Hepatitis C Virus (HCV) Infection14
Not AvailableCompletedNot AvailableChronic Hepatitis C Virus (HCV) Infection / Cognition Disorders / Fatigue Syndrome, Chronic / Major Depressive Disorder (MDD)1
Not AvailableCompletedNot AvailableChronic Hepatitis C Virus (HCV) Infection / Hepatitis C Viral Infection1
Not AvailableCompletedNot AvailableHepatitis B Chronic Infection6
Not AvailableCompletedNot AvailableHepatitis C Viral Infection2
Not AvailableCompletedNot AvailableHepatitis C Viral Infection / Human Immunodeficiency Virus (HIV) / Infection NOS1
Not AvailableCompletedBasic ScienceChronic Hepatitis C Virus (HCV) Infection / Human Immunodeficiency Virus (HIV)1
Not AvailableCompletedTreatmentChronic Hepatitis C Virus (HCV) Infection1
Not AvailableCompletedTreatmentHepatitis B Chronic Infection1
Not AvailableCompletedTreatmentHepatitis C Viral Infection / Human Immunodeficiency Virus (HIV) Infections1
Not AvailableNo Longer AvailableNot AvailableChronic Hepatitis C Virus (HCV) Infection1
Not AvailableNot Yet RecruitingNot AvailableHepatitis B Chronic Infection1
Not AvailableRecruitingNot AvailableViral Hepatitis B1
Not AvailableRecruitingTreatmentHepatitis B Chronic Infection2
Not AvailableTerminatedNot AvailableChronic Hepatitis C Virus (HCV) Infection2
Not AvailableUnknown StatusBasic ScienceChronic HCV Infection / Nonalcoholic Steatohepatitis1
Not AvailableUnknown StatusTreatmentViral Hepatitis B1
Not AvailableWithdrawnBasic ScienceHepatitis C Viral Infection1
Not AvailableWithdrawnTreatmentChronic Hepatitis C Virus (HCV) Infection1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • F Hoffmann La Roche Ltd.
  • F Hoffmann-La Roche Ltd.
Dosage forms
FormRouteStrength
Injection, solutionSubcutaneous135 ug/0.5mL
Injection, solutionSubcutaneous135 μg
Injection, solutionSubcutaneous180 ug/1mL
Injection, solutionSubcutaneous180 ug/0.5mL
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)
CA2172664No2000-10-032016-03-26Canada
CA2203480No2009-06-302017-04-23Canada

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)61 °CBeldarrain, A. et al., Biochemistry 38:7865-7873 (1999)
isoelectric point5.99Not Available

Taxonomy

Description
Not Available
Kingdom
Organic Compounds
Super Class
Organic Acids
Class
Carboxylic Acids and Derivatives
Sub Class
Amino Acids, Peptides, and Analogues
Direct Parent
Peptides
Alternative Parents
Not Available
Substituents
Not Available
Molecular Framework
Not Available
External Descriptors
Not 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 direc...
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 JA...
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]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

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 un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Begre S, von Bardeleben U, Ladewig D, Jaquet-Rochat S, Cosendai-Savary L, Golay KP, Kosel M, Baumann P, Eap CB: Paroxetine increases steady-state concentrations of (R)-methadone in CYP2D6 extensive but not poor metabolizers. J Clin Psychopharmacol. 2002 Apr;22(2):211-5. [PubMed:11910269]
  2. Peg-interferon FDA label [File]

Drug created on June 13, 2005 07:24 / Updated on November 14, 2018 12:38