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Identification
NamePeginterferon alfa-2a
Accession NumberDB00008  (BTD00043, BIOD00043)
TypeBiotech
GroupsApproved, Investigational
DescriptionHuman interferon 2a, is a covalent conjugate of recombinant alfa-2a interferon with a single branched bis-monomethoxy polyethylene glycol (PEG) chain. The PEG moiety is linked at a single site to the interferon alfa moiety via a stable amide bond to lysine. Peginterferon alfa-2a has an approximate molecular weight of 60,000 daltons. Interferon alfa-2a is produced using recombinant DNA technology in which a cloned human leukocyte interferon gene is inserted into and expressed in Escherichia coli. The resultant protein is 165 amino acids. The PEG strand protects the molecule in vivo from proteolytic breakdown, substantially increases its in vivo half-life, and reduces immunogenicity by wrapping around and physically hindering access to the protein portion of the molecule.
Protein structureDb00008
Related Articles
Protein chemical formulaNot Available
Protein average weight60000.0 Da
Sequences
>Peginterferon alfa-2a sequence
CDLPQTHSLGSRRTLMLLAQMRRISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMI
QQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMKEDSILAVR
KYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE
Download FASTA Format
SynonymsNot Available
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
PegasysInjection, solution90 μgSubcutaneousRoche Registration Limited  2002-06-20Not applicableEu
PegasysInjection, solution135 μgSubcutaneousRoche Registration Limited  2002-06-20Not applicableEu
PegasysInjection, solution180 μgSubcutaneousRoche Registration Limited  2002-06-20Not applicableEu
PegasysInjection, solution180 ug/mLSubcutaneousGenentech, Inc.2002-10-16Not applicableUs
PegasysInjection, solution135 μgSubcutaneousRoche Registration Limited  2002-06-20Not applicableEu
PegasysInjection, solution180 μgSubcutaneousRoche Registration Limited  2002-06-20Not applicableEu
PegasysSolution180 mcgSubcutaneousHoffmann La Roche2003-08-14Not applicableCanada
PegasysInjection, solution180 μgSubcutaneousRoche Registration Limited  2002-06-20Not applicableEu
PegasysInjection, solution135 μgSubcutaneousRoche Registration Limited  2002-06-20Not applicableEu
PegasysInjection, solution180 ug/.5mLSubcutaneousGenentech, Inc.2011-03-29Not applicableUs
PegasysInjection, solution180 μgSubcutaneousRoche Registration Limited  2002-06-20Not applicableEu
PegasysInjection, solution180 μgSubcutaneousRoche Registration Limited  2002-06-20Not applicableEu
PegasysSolution180 mcgSubcutaneousHoffmann La Roche2003-08-14Not applicableCanada
PegasysInjection, solution180 μgSubcutaneousRoche Registration Limited  2002-06-20Not applicableEu
PegasysInjection, solution135 μgSubcutaneousRoche Registration Limited  2002-06-20Not applicableEu
PegasysInjection, solution135 ug/.5mLSubcutaneousGenentech, Inc.2011-11-01Not applicableUs
PegasysInjection, solution180 μgSubcutaneousRoche Registration Limited  2002-06-20Not applicableEu
PegasysInjection, solution180 μgSubcutaneousRoche Registration Limited  2002-06-20Not applicableEu
PegasysInjection, solution135 μgSubcutaneousRoche Registration Limited  2002-06-20Not applicableEu
PegasysInjection, solution135 μgSubcutaneousRoche Registration Limited  2002-06-20Not applicableEu
PegasysInjection, solution135 μgSubcutaneousRoche Registration Limited  2002-06-20Not applicableEu
PegasysInjection, solution180 ug/.5mLSubcutaneousGenentech, Inc.2011-11-01Not applicableUs
PegasysInjection, solution135 μgSubcutaneousRoche Registration Limited  2002-06-20Not 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
SaltsNot Available
Categories
UNIIQ46947FE7K
CAS number198153-51-4
Pharmacology
IndicationFor treatment of hairy cell leukemia, malignant melanoma, and AIDS-related Kaposi's sarcoma.
Structured Indications
Clinical Trials
PhaseStatusPurposeConditionsCount
0TerminatedTreatmentChronic Hepatitis C (CHC) / Genotype 1 / Relapses1
1Active Not RecruitingBasic ScienceHepatitis C1
1Active Not RecruitingTreatmentChronic Hepatitis B Infection2
1CompletedNot AvailableHealthy Subjects1
1CompletedTreatmentChronic Viral Hepatitis C1
1CompletedTreatmentHepatitis B,Chronic2
1CompletedTreatmentHepatitis C, Chronic2
1RecruitingTreatmentEssential Thrombocythemia (ET) / Polycythemia Vera (PV)1
1, 2CompletedTreatmentChronic Hepatitis C Infection / Genotype 11
1, 2CompletedTreatmentHepatitis B,Chronic1
1, 2CompletedTreatmentHepatitis C1
1, 2Not Yet RecruitingTreatmentChronic Hepatitis B Infection1
1, 2Not Yet RecruitingTreatmentInfection, Human Immunodeficiency Virus1
1, 2RecruitingTreatmentAcute Myeloid Leukaemias (AML)1
1, 2RecruitingTreatmentChronic Hepatitis B Infection1
1, 2RecruitingTreatmentChronic Hepatitis C Virus Genotype I1
1, 2TerminatedTreatmentChronic Hepatitis B Infection1
1, 2WithdrawnTreatmentChronic Lymphocytic Leukaemia (CLL)1
2Active Not RecruitingTreatmentChronic Hepatitis C (CHC)1
2Active Not RecruitingTreatmentHepatitis C, Chronic1
2Active Not RecruitingTreatmentHepatitis D1
2Active Not RecruitingTreatmentMyeloproliferative Disorders1
2CompletedNot AvailableHepatitis C1
2CompletedDiagnosticHCV-HIV Co-Infection1
2CompletedTreatmentBlast Crisis / Leukemia, Lymphocytic, Acute / Leukemia,Myeloid, Chronic / Philadelphia Chromosome1
2CompletedTreatmentChronic Hepatitis B Infection1
2CompletedTreatmentChronic Hepatitis C (CHC)8
2CompletedTreatmentGenotype 1 Chronic Hepatitis C1
2CompletedTreatmentHCV Infections1
2CompletedTreatmentHemophilia / Hepatitis C / Infection, Human Immunodeficiency Virus1
2CompletedTreatmentHepatitis B Virus (HBV)1
2CompletedTreatmentHepatitis B,Chronic2
2CompletedTreatmentHepatitis C4
2CompletedTreatmentHepatitis C Infection3
2CompletedTreatmentHepatitis C Infection / Infection, Human Immunodeficiency Virus1
2CompletedTreatmentHepatitis C Virus (HCV)6
2CompletedTreatmentHepatitis C, Chronic19
2CompletedTreatmentHepatitis C / Infection, Human Immunodeficiency Virus2
2CompletedTreatmentHepatitis C / Infection, Human Immunodeficiency Virus / Liver Diseases1
2CompletedTreatmentHepatitis C / Thalassemias1
2CompletedTreatmentHepatitis / Hepatitis C1
2CompletedTreatmentHepatocellular Carcinomas1
2CompletedTreatmentInfection, Human Immunodeficiency Virus1
2Not Yet RecruitingTreatmentHepatitis C, Chronic1
2RecruitingTreatmentChronic Hepatitis B Infection3
2RecruitingTreatmentChronic Hepatitis C Infection1
2RecruitingTreatmentHigh Risk Essential Thrombocythemia / High Risk Polycythemia Vera1
2RecruitingTreatmentMyelofibrosis1
2RecruitingTreatmentSquamous Cell Carcinoma (SCC) / Squamous Cell Carcinoma of Skin1
2TerminatedTreatmentHepatitis C2
2TerminatedTreatmentLeukemias1
2WithdrawnTreatmentChronic Hepatitis C Virus Genotype 11
2WithdrawnTreatmentHepatitis C, Chronic1
2WithdrawnTreatmentHepatitis C / Hepatitis C Virus (HCV)1
2, 3CompletedTreatmentHepatitis C Virus (HCV) / Infection, Human Immunodeficiency Virus / Liver Cirrhosis1
2, 3RecruitingTreatmentChronic Hepatitis C (CHC) / Insulin Resistance1
2, 3WithdrawnTreatmentHepatitis C1
3Active Not RecruitingTreatmentChronic Hepatitis B Infection2
3Active Not RecruitingTreatmentChronic Hepatitis C (CHC)1
3Active Not RecruitingTreatmentHepatitis B,Chronic1
3Active Not RecruitingTreatmentHepatitis D, Chronic1
3Active Not RecruitingTreatmentHepatitis / Hepatitis C1
3CompletedPreventionChronic Hepatitis C (CHC) / Fibrosis, Liver / Hepatic Cirrhosis / Liver Cirrhosis1
3CompletedPreventionDepression1
3CompletedTreatmentAntiviral Treatment of Chronic Hepatitis B1
3CompletedTreatmentChronic Hepatitis B Infection2
3CompletedTreatmentChronic Hepatitis C (CHC)5
3CompletedTreatmentCoinfection / Hepatitis C / Infection, Human Immunodeficiency Virus1
3CompletedTreatmentHCV Infections / Hepatitis C, Chronic1
3CompletedTreatmentHepatitis B,Chronic3
3CompletedTreatmentHepatitis C7
3CompletedTreatmentHepatitis C Virus (HCV)2
3CompletedTreatmentHepatitis C, Chronic7
3CompletedTreatmentHepatitis C, Chronic / Infection NOS1
3CompletedTreatmentHepatitis C, Genotype 11
3CompletedTreatmentHepatitis C / Hepatitis C, Chronic1
3RecruitingTreatmentChronic Hepatitis C (CHC)1
3RecruitingTreatmentChronic Myeloid Leukemia (CML)1
3RecruitingTreatmentEssential Thrombocythemia (ET) / Polycythemia Vera (PV) / Primary Myelofibrosis1
3RecruitingTreatmentHepatitis B,Chronic1
3RecruitingTreatmentHigh Risk Essential Thrombocythemia / High Risk Polycythemia Vera1
3TerminatedTreatmentChronic Hepatitis C (CHC)1
3TerminatedTreatmentHepatitis B1
3TerminatedTreatmentHepatitis C, Chronic1
3WithdrawnTreatmentChronic Hepatitis C (CHC)1
3WithdrawnTreatmentHepatitis C1
3WithdrawnTreatmentHepatitis C, Chronic1
4Active Not RecruitingPreventionChronic Hepatitis B Infection1
4Active Not RecruitingTreatmentChronic Hepatitis B Infection1
4Active Not RecruitingTreatmentChronic Hepatitis C (CHC) / Co-Infection HIV-HCV1
4Active Not RecruitingTreatmentChronic Hepatitis C (CHC) / Hepatocellular Carcinomas1
4Active Not RecruitingTreatmentHepatitis, Chronic1
4CompletedNot AvailableHepatitis B,Chronic1
4CompletedNot AvailableHepatitis, Viral, Non-A, Non-B, Parenterally-Transmitted1
4CompletedBasic ScienceHepatitis C, Chronic / Liver Diseases / Virus Diseases1
4CompletedDiagnosticChronic Hepatitis C (CHC)1
4CompletedPreventionHepatitis C / Liver Transplant1
4CompletedTreatmentAcute Hepatitis C2
4CompletedTreatmentAnemias1
4CompletedTreatmentAntiviral Agents / Chronic Liver Diseases (CLD) / Hepatitis C Virus (HCV) / Therapeutic Uses / Viral Hepatitis1
4CompletedTreatmentAsian Americans / Chronic Hepatitis C (CHC) / Novel Genotypes / Treatments1
4CompletedTreatmentChronic Hepatitis B Infection1
4CompletedTreatmentChronic Hepatitis C (CHC)9
4CompletedTreatmentChronic Hepatitis C (CHC) / End Stage Renal Disease (ESRD)1
4CompletedTreatmentChronic Hepatitis C (CHC) / Genotyping1
4CompletedTreatmentChronic Hepatitis C (CHC) / Neoplasms1
4CompletedTreatmentChronic Hepatitis C, Genotype 11
4CompletedTreatmentFatty Liver / Hepatitis C1
4CompletedTreatmentHepatitis B,Chronic12
4CompletedTreatmentHepatitis C4
4CompletedTreatmentHepatitis C, Chronic26
4CompletedTreatmentHepatitis C, Chronic / Infection, Human Immunodeficiency Virus1
4CompletedTreatmentHepatitis C / Human Immunodeficiency Virus (HIV) / Infection, Human Immunodeficiency Virus1
4CompletedTreatmentHepatitis C / Infection, Human Immunodeficiency Virus2
4CompletedTreatmentIL28B Polymorphism / Sustained Virologic Response1
4Not Yet RecruitingTreatmentHepatitis B1
4Not Yet RecruitingTreatmentHepatitis C1
4RecruitingTreatmentChronic Hepatitis B Infection3
4RecruitingTreatmentChronic Hepatitis C (CHC)2
4RecruitingTreatmentFibrosis, Liver1
4RecruitingTreatmentHepatitis C, Chronic / HIV Disease1
4RecruitingTreatmentHepatitis B,Chronic2
4RecruitingTreatmentHepatitis C1
4TerminatedTreatmentChronic Hepatitis C (CHC)1
4TerminatedTreatmentHepatitis C2
4WithdrawnTreatmentHepatitis B,Chronic1
Not AvailableActive Not RecruitingNot AvailableHepatitis C / HIV Disease / Infection NOS1
Not AvailableCompletedNot AvailableHepatitis B,Chronic1
Not AvailableCompletedNot AvailableHepatitis C2
Not AvailableCompletedNot AvailableHepatitis C, Chronic5
Not AvailableCompletedBasic ScienceChronic Hepatitis C (CHC) / Human Immunodeficiency Virus (HIV)1
Not AvailableCompletedTreatmentChronic Hepatitis C (CHC)1
Not AvailableEnrolling by InvitationNot AvailableChronic Hepatitis C (CHC)1
Not AvailableNot Yet RecruitingTreatmentHepatitis B1
Not AvailableRecruitingNot AvailableChronic Hepatitis B Infection1
Not AvailableRecruitingBasic ScienceChronic HCV Infection / Nonalcoholic Steatohepatitis1
Not AvailableRecruitingTreatmentHepatitis B1
Not AvailableTerminatedTreatmentChronic Hepatitis C (CHC)1
Not AvailableWithdrawnBasic ScienceHepatitis C1
PharmacodynamicsUpregulates the expression of MHC I proteins, allowing for increased presentation of peptides derived from viral antigens. This enhances the activation of CD8+ T cells that are the precursors for cytotoxic T lymphocytes (CTLs) and makes the macrophage a better target for CTL-mediated killing. Interferon alpha also induce the synthesis of several key antiviral mediators, including 2'-5' oligoadenylate synthetase (2'-5' A synthetase) and protein kinase R.
Mechanism of actionInterferon alpha binds to type I interferon receptors (IFNAR1 and IFNAR2c) which, upon dimerization, activate two Jak (Janus kinase) tyrosine kinases (Jak1 and Tyk2). These transphosphorylate themselves and phosphorylate the receptors. The phosphorylated INFAR receptors then bind to Stat1 and Stat2 (signal transducers and activators of transcription) which dimerize and activate multiple (~100) immunomodulatory and antiviral proteins. Interferon alpha binds less stably to type I interferon receptors than interferon beta.
TargetKindPharmacological actionActionsOrganismUniProt ID
Interferon alpha/beta receptor 2Proteinyes
agonist
HumanP48551 details
Interferon alpha/beta receptor 1Proteinyes
agonist
HumanP17181 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeTerminal half life is 80 hours (range 50 to 140 hours).
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
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
BCGThe 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 ReferencesNot Available
External Links
ATC CodesL03AB61L03AB11
AHFS Codes
  • 08:18.20
PDB Entries
FDA labelNot Available
MSDSNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, solutionSubcutaneous135 ug/.5mL
Injection, solutionSubcutaneous135 μg
Injection, solutionSubcutaneous180 ug/mL
Injection, solutionSubcutaneous180 μg
Injection, solutionSubcutaneous180 ug/.5mL
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 point61 °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
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
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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23