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Identification
NamePeginterferon alfa-2b
Accession NumberDB00022  (BTD00048, BIOD00048)
TypeBiotech
GroupsApproved
Description

Peginterferon alfa-2b is a covalent conjugate of recombinant alfa-2b interferon with monomethoxy polyethylene glycol (PEG). The average molecular weight of the PEG portion of the molecule is 12,000 daltons. The average molecular weight of the PEG-Intron molecule is approximately 31,000 daltons. The specific activity of peginterferon alfa-2b is approximately 0.7 × 108 IU/mg protein. Interferon alfa-2b is a water-soluble protein with a molecular weight of 19,271 daltons produced by recombinant DNA techniques. It is obtained from the bacterial fermentation of a strain of Escherichia coli bearing a genetically engineered plasmid containing an interferon gene from human leukocytes. 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 structureDb00022
Related Articles
Protein chemical formulaNot Available
Protein average weight31000.0 Da
Sequences
>DB00022 sequence
CDLPQTHSLGSRRTLMLLAQMRRISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMI
QQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMKEDSILAVR
KYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE
Download FASTA Format
SynonymsNot Available
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
PegintronkitMerck Sharp & Dohme Corp.2014-08-11Not applicableUs
PegintronkitMerck Sharp & Dohme Corp.2014-08-11Not applicableUs
PegintronkitMerck Sharp & Dohme Corp.2001-01-19Not applicableUs
PegintronkitMerck Sharp & Dohme Corp.2001-01-19Not applicableUs
PegintronkitMerck Sharp & Dohme Corp.2014-08-11Not applicableUs
Pegintroninjection, powder, lyophilized, for solution50 ug/.5mLsubcutaneousMerck Sharp & Dohme Corp.2001-01-19Not applicableUs
PegintronkitMerck Sharp & Dohme Corp.2014-08-11Not applicableUs
Pegintroninjection, powder, lyophilized, for solution80 ug/.5mLsubcutaneousMerck Sharp & Dohme Corp.2001-01-19Not applicableUs
PegintronkitMerck Sharp & Dohme Corp.2001-01-19Not applicableUs
Pegintroninjection, powder, lyophilized, for solution120 ug/.5mLsubcutaneousMerck Sharp & Dohme Corp.2001-01-19Not applicableUs
PegintronkitMerck Sharp & Dohme Corp.2001-01-19Not applicableUs
Pegintroninjection, powder, lyophilized, for solution150 ug/.5mLsubcutaneousMerck Sharp & Dohme Corp.2001-01-19Not applicableUs
SylatronkitMerck Sharp & Dohme Corp.2011-03-29Not applicableUs
SylatronkitMerck Sharp & Dohme Corp.2011-03-29Not applicableUs
SylatronkitMerck Sharp & Dohme Corp.2011-03-29Not applicableUs
SylatronkitMerck Sharp & Dohme Corp.2014-08-30Not applicableUs
SylatronkitMerck Sharp & Dohme Corp.2011-03-29Not applicableUs
SylatronkitMerck Sharp & Dohme Corp.2011-03-29Not applicableUs
Unitron Pegpowder for solution222 mcgsubcutaneousMerck Canada Inc2001-03-272012-02-01Canada
Unitron Pegpowder for solution177.6 mcgsubcutaneousMerck Canada Inc2001-03-272012-02-01Canada
Unitron Pegpowder for solution118.4 mcgsubcutaneousMerck Canada Inc2001-03-272012-02-01Canada
Unitron Pegpowder for solution74 mcgsubcutaneousMerck Canada Inc2001-03-272012-02-01Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
PEG-IntronSchering Corp
Brand mixtures
NameLabellerIngredients
PegetronMerck Canada Inc
Victrelis TripleMerck Canada Inc
SaltsNot Available
Categories
UNIIG8RGG88B68
CAS number215647-85-1
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
Pharmacology
IndicationFor the treatment of chronic hepatitis C in patients not previously treated with interferon alpha who have compensated liver disease and are at least 18 years of age.
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.
Related Articles
AbsorptionFollowing a single subcutaneous dose of peginterferon alfa-2b, the mean absorption half-life (t½ ka) was 4.6 hours.
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationRenal elimination accounts for 30% of the clearance.
Half lifeThe mean elimination half-life is approximately 40 hours (range 22 to 60 hours) in patients with HCV infection.
Clearance
  • Oral cl=22 mL/hr∙kg [patients with HCV infection]
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Capsule; powder for solutionoral; subcutaneous
Injection, powder, lyophilized, for solutionsubcutaneous120 ug/.5mL
Injection, powder, lyophilized, for solutionsubcutaneous150 ug/.5mL
Injection, powder, lyophilized, for solutionsubcutaneous50 ug/.5mL
Injection, powder, lyophilized, for solutionsubcutaneous80 ug/.5mL
Kit
Powder for solutionsubcutaneous118.4 mcg
Powder for solutionsubcutaneous177.6 mcg
Powder for solutionsubcutaneous222 mcg
Powder for solutionsubcutaneous74 mcg
Prices
Unit descriptionCostUnit
Peg-Intron Redipen Pak 4 4 50 mcg/0.5ml Kit Box2428.8USD kit
Peg-Intron Redipen 150 mcg/0.5ml Kit702.87USD kit
Peg-Intron 150 mcg Kit671.74USD kit
Peg-Intron Redipen 120 mcg/0.5ml Kit669.39USD kit
Peg-Intron redipen 150 mcg640.61USD redipen
Peg-Intron redipen 150 mcg 4pk640.6USD redipen
Peg-Intron 120 mcg Kit639.74USD kit
Peg-Intron Redipen 80 mcg/0.5ml Kit637.49USD kit
Peg-Intron redipen 120 mcg610.09USD redipen
Peg-Intron 80 mcg Kit609.26USD kit
Peg-Intron 50 mcg/0.5ml Kit607.19USD kit
Peg-Intron redipen 80 mcg581.02USD redipen
Peg-Intron 50 mcg kit553.4USD kit
Peg-Intron redipen 50 mcg553.4USD redipen
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1341567 No2008-02-192025-02-19Canada
CA2329474 No0002-02-262016-10-31Canada
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point61 °CBeldarrain, A. et al., Biochemistry 38:7865-7873 (1999)
isoelectric point5.99Not Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesL03AB10L03AB60
AHFS Codes
  • 08:18.20
PDB Entries
FDA labelDownload (50.9 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Peginterferon alfa-2b.
AldesleukinThe risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Aldesleukin.
AlosetronThe serum concentration of Alosetron can be increased when it is combined with Peginterferon alfa-2b.
AminophyllineThe serum concentration of Aminophylline can be increased when it is combined with Peginterferon alfa-2b.
AmitriptylineThe serum concentration of Amitriptyline can be decreased when it is combined with Peginterferon alfa-2b.
AmoxapineThe serum concentration of Amoxapine can be decreased when it is combined with Peginterferon alfa-2b.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Peginterferon alfa-2b.
AsenapineThe serum concentration of Asenapine can be increased when it is combined with Peginterferon alfa-2b.
AtomoxetineThe serum concentration of Atomoxetine can be decreased when it is combined with Peginterferon alfa-2b.
BetaxololThe serum concentration of Betaxolol can be increased when it is combined with Peginterferon alfa-2b.
BortezomibThe serum concentration of Bortezomib can be increased when it is combined with Peginterferon alfa-2b.
BrexpiprazoleThe serum concentration of Brexpiprazole can be decreased when it is combined with Peginterferon alfa-2b.
BromazepamThe serum concentration of Bromazepam can be increased when it is combined with Peginterferon alfa-2b.
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Peginterferon alfa-2b.
CaptoprilThe serum concentration of Captopril can be decreased when it is combined with Peginterferon alfa-2b.
CarvedilolThe serum concentration of Carvedilol can be decreased when it is combined with Peginterferon alfa-2b.
ChloroquineThe serum concentration of Chloroquine can be decreased when it is combined with Peginterferon alfa-2b.
ChlorphenamineThe serum concentration of Chlorphenamine can be decreased when it is combined with Peginterferon alfa-2b.
ChlorpromazineThe serum concentration of Chlorpromazine can be decreased when it is combined with Peginterferon alfa-2b.
ClomipramineThe serum concentration of Clomipramine can be decreased when it is combined with Peginterferon alfa-2b.
ClozapineThe risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Clozapine.
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Peginterferon alfa-2b.
DacarbazineThe serum concentration of Dacarbazine can be increased when it is combined with Peginterferon alfa-2b.
DesipramineThe serum concentration of Desipramine can be decreased when it is combined with Peginterferon alfa-2b.
DextromethorphanThe serum concentration of Dextromethorphan can be decreased when it is combined with Peginterferon alfa-2b.
DoxepinThe serum concentration of Doxepin can be decreased when it is combined with Peginterferon alfa-2b.
DoxorubicinThe serum concentration of Doxorubicin can be decreased when it is combined with Peginterferon alfa-2b.
DuloxetineThe serum concentration of Duloxetine can be increased when it is combined with Peginterferon alfa-2b.
EliglustatThe serum concentration of Eliglustat can be decreased when it is combined with Peginterferon alfa-2b.
FlecainideThe serum concentration of Flecainide can be decreased when it is combined with Peginterferon alfa-2b.
FluoxetineThe serum concentration of Fluoxetine can be decreased when it is combined with Peginterferon alfa-2b.
FluphenazineThe serum concentration of Fluphenazine can be decreased when it is combined with Peginterferon alfa-2b.
FlutamideThe serum concentration of Flutamide can be increased when it is combined with Peginterferon alfa-2b.
FluvoxamineThe serum concentration of Fluvoxamine can be decreased when it is combined with Peginterferon alfa-2b.
GefitinibThe serum concentration of Gefitinib can be decreased when it is combined with Peginterferon alfa-2b.
HaloperidolThe serum concentration of Haloperidol can be decreased when it is combined with Peginterferon alfa-2b.
IloperidoneThe serum concentration of Iloperidone can be decreased when it is combined with Peginterferon alfa-2b.
ImipramineThe serum concentration of Imipramine can be decreased when it is combined with Peginterferon alfa-2b.
LidocaineThe serum concentration of Lidocaine can be increased when it is combined with Peginterferon alfa-2b.
MaprotilineThe serum concentration of Maprotiline can be decreased when it is combined with Peginterferon alfa-2b.
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Peginterferon alfa-2b.
MethadoneThe serum concentration of Methadone can be increased when it is combined with Peginterferon alfa-2b.
MethamphetamineThe serum concentration of Methamphetamine can be decreased when it is combined with Peginterferon alfa-2b.
MetoprololThe serum concentration of Metoprolol can be decreased when it is combined with Peginterferon alfa-2b.
MexiletineThe serum concentration of Mexiletine can be decreased when it is combined with Peginterferon alfa-2b.
MirtazapineThe serum concentration of Mirtazapine can be decreased when it is combined with Peginterferon alfa-2b.
NefazodoneThe serum concentration of Nefazodone can be decreased when it is combined with Peginterferon alfa-2b.
NortriptylineThe serum concentration of Nortriptyline can be decreased when it is combined with Peginterferon alfa-2b.
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Peginterferon alfa-2b.
ParoxetineThe serum concentration of Paroxetine can be decreased when it is combined with Peginterferon alfa-2b.
PegloticaseThe therapeutic efficacy of Peginterferon alfa-2b can be decreased when used in combination with Pegloticase.
PerphenazineThe serum concentration of Perphenazine can be decreased when it is combined with Peginterferon alfa-2b.
PimozideThe serum concentration of Pimozide can be decreased when it is combined with Peginterferon alfa-2b.
PipotiazineThe serum concentration of Pipotiazine can be decreased when it is combined with Peginterferon alfa-2b.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Peginterferon alfa-2b.
PrimaquineThe serum concentration of Primaquine can be decreased when it is combined with Peginterferon alfa-2b.
ProcainamideThe serum concentration of Procainamide can be decreased when it is combined with Peginterferon alfa-2b.
PromazineThe serum concentration of Promazine can be decreased when it is combined with Peginterferon alfa-2b.
PromethazineThe serum concentration of Promethazine can be decreased when it is combined with Peginterferon alfa-2b.
PropranololThe serum concentration of Propranolol can be decreased when it is combined with Peginterferon alfa-2b.
ProtriptylineThe serum concentration of Protriptyline can be decreased when it is combined with Peginterferon alfa-2b.
RamelteonThe serum concentration of Ramelteon can be increased when it is combined with Peginterferon alfa-2b.
RasagilineThe serum concentration of Rasagiline can be increased when it is combined with Peginterferon alfa-2b.
RibavirinThe risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Ribavirin.
RisperidoneThe serum concentration of Risperidone can be decreased when it is combined with Peginterferon alfa-2b.
RopiniroleThe serum concentration of Ropinirole can be increased when it is combined with Peginterferon alfa-2b.
RopivacaineThe serum concentration of Ropivacaine can be increased when it is combined with Peginterferon alfa-2b.
StiripentolThe serum concentration of Stiripentol can be increased when it is combined with Peginterferon alfa-2b.
TamoxifenThe serum concentration of Tamoxifen can be decreased when it is combined with Peginterferon alfa-2b.
TasimelteonThe serum concentration of Tasimelteon can be increased when it is combined with Peginterferon alfa-2b.
TelbivudineThe risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Telbivudine.
TetrabenazineThe serum concentration of Tetrabenazine can be decreased when it is combined with Peginterferon alfa-2b.
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Peginterferon alfa-2b.
ThioridazineThe serum concentration of Thioridazine can be decreased when it is combined with Peginterferon alfa-2b.
ThiothixeneThe serum concentration of Thiothixene can be increased when it is combined with Peginterferon alfa-2b.
TimololThe serum concentration of Timolol can be decreased when it is combined with Peginterferon alfa-2b.
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Peginterferon alfa-2b.
TolterodineThe serum concentration of Tolterodine can be decreased when it is combined with Peginterferon alfa-2b.
TrifluoperazineThe serum concentration of Trifluoperazine can be increased when it is combined with Peginterferon alfa-2b.
TrimipramineThe serum concentration of Trimipramine can be decreased when it is combined with Peginterferon alfa-2b.
VenlafaxineThe serum concentration of Venlafaxine can be decreased when it is combined with Peginterferon alfa-2b.
VortioxetineThe serum concentration of Vortioxetine can be decreased when it is combined with Peginterferon alfa-2b.
ZidovudineThe risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Zidovudine.
ZuclopenthixolThe serum concentration of Zuclopenthixol can be decreased when it is combined with Peginterferon alfa-2b.
Food InteractionsNot Available

Targets

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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. 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 ]
  4. 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 ]
  5. 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 ]
  6. 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 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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. 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 ]
  4. 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 ]
  5. 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 ]
  6. 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 March 22, 2016 20:55