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Identification
NameInterferon Alfa-2a, Recombinant
Accession NumberDB00034  (BTD00095, BTD00012, BIOD00095, BIOD00012, DB00037)
TypeBiotech
GroupsApproved
Description

Interferon a (human leukocyte protein moiety reduced). A type I interferon consisting of 165 amino acid residues with lysine in position 23. This protein is produced by recombinant DNA technology and resembles interferon secreted by leukocytes. It is used extensively as an antiviral or antineoplastic agent. An oral form is being developed by Amarillo Biosciences.

Protein structureDb00034
Related Articles
Protein chemical formulaC860H1353N227O255S9
Protein average weight19241.1 Da
Sequences
>DB00034 sequence
CDLPQTHSLGSRRTLMLLAQMRKISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMI
QQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMKEDSILAVR
KYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE
Download FASTA Format
Synonyms
Interferon alfa-2a
Interferon alfa-2a (recombinant)
Interferon alfa-2a, recombinant
Interferon alfa-2a,recombinant
Interferon alpha-2a
Interferon-alfa-2a
Recombinant human interferon alfa-2a
Recombinant human interferon-alfa-2a
rIFN-alpha-2a
SH-polypeptide-46
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Roferon A Soln Inj 6 Millionliquid6000000 unitintramuscular; subcutaneousHoffmann La Roche Limited1989-12-311997-08-26Canada
Roferon A Sterile Pws 18m Unit/vialpowder for solution18000000 unitintramuscular; subcutaneousHoffmann La Roche Limited1991-12-311996-09-30Canada
Roferon A Sterile Pws 3m Unit/vialpowder for solution3000000 unitintramuscular; subcutaneousHoffmann La Roche Limited1991-12-311996-09-30Canada
Roferon A Sterile Pws 9m Unit/vialpowder for solution9000000 unitintramuscular; subcutaneousHoffmann La Roche Limited1991-12-311996-09-30Canada
Roferon-A Solution Inj. 9million I.U./0.9mlsolution9000000 unitintramuscular; subcutaneousHoffmann La Roche Limited1993-12-311997-08-26Canada
Roferon-A Sol Inj 3million Iu/vialliquid3000000 unitintramuscular; subcutaneousHoffmann La Roche Limited1989-12-311997-08-25Canada
Roferon-A Soln-liq Im Sc 4.5million I.u/mlliquid4.5 mintramuscular; subcutaneousHoffmann La Roche Limited1997-04-251999-11-02Canada
Roferon-A Soln-liq Im Sc 9million I.U./mlsolution9 mintramuscular; subcutaneousHoffmann La Roche Limited1997-04-292004-11-01Canada
Roferon-A Solution 18 Million I.U./3mlsolution18 mintramuscular; subcutaneousHoffmann La Roche Limited1997-01-152005-07-14Canada
Roferon-A Solution 3 Million I.U./mlsolution3 mintramuscular; subcutaneousHoffmann La Roche Limited1997-02-252005-07-14Canada
Roferon-A Solution 6 Million I.U./mlsolution6 mintramuscular; subcutaneousHoffmann La Roche Limited1997-02-242000-07-27Canada
Roferon-A Solution Inj 36000000unit/mlsolution36000000 unitintramuscular; subcutaneousHoffmann La Roche Limited1992-12-311997-06-18Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
Roferon AHoffmann-La Roche Inc
VeldonaAmarillo Biosciences
Brand mixturesNot Available
SaltsNot Available
Categories
UNII47RRR83SK7
CAS number76543-88-9
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, hairy cell leukemia, AIDS-related Kaposi's sarcoma, and chronic myelogenous leukemia. Also for the treatment of oral warts arising from HIV infection.
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.
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AbsorptionAbsorption is high (greater than 80%) when administered intramuscularly or subcutaneously.
Volume of distribution
  • 0.223 to 0.748 L/kg [healthy people]
Protein bindingNot Available
MetabolismNot Available
Route of eliminationAlpha-interferons are totally filtered through the glomeruli and undergo rapid proteolytic degradation during tubular reabsorption, rendering a negligible reappearance of intact alfa interferon in the systemic circulation.
Half lifeThe IM half-life of interferon alfa-2a is 6 hours to 8 hours; the half-life for IV infusion is 3.7 hours to 8.5 hours (mean 5.1 hours).
Clearance
  • 2.14 – 3.62 mL/min/kg [healthy]
ToxicityInterferon alfa-2 may cause serious adverse effects such as anemia; autoimmune diseases, including vasculitis, arthritis, hemolytic anemia, and erythematosus syndrome; cardiotoxicity; hepatotoxicity; hyperthyroidism or hypothyroidism; transient ischemic attacks; leukopenia; neurotoxicity; peripheral neuropathy; and thrombocytopenia. Some lesser side effects that may not need medical attention include blurred vision, change in taste or metallic taste, cold sores or stomatitis, diarrhea, dizziness, dry mouth, dry skin or itching, flu-like syndrome, increased sweating, leg cramps, loss of appetite, nausea or vomiting, skin rash, unusual tiredness, weight loss, and partial loss of hair.
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
Liquidintramuscular; subcutaneous6000000 unit
Powder for solutionintramuscular; subcutaneous18000000 unit
Powder for solutionintramuscular; subcutaneous3000000 unit
Powder for solutionintramuscular; subcutaneous9000000 unit
Solutionintramuscular; subcutaneous9000000 unit
Liquidintramuscular; subcutaneous3000000 unit
Liquidintramuscular; subcutaneous4.5 m
Solutionintramuscular; subcutaneous9 m
Solutionintramuscular; subcutaneous18 m
Solutionintramuscular; subcutaneous3 m
Solutionintramuscular; subcutaneous6 m
Solutionintramuscular; subcutaneous36000000 unit
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2172664 No2000-10-032016-03-26Canada
Properties
StateLiquid
Experimental Properties
PropertyValueSource
water solubility100 mg/mlNot Available
hydrophobicity-0.336Not Available
isoelectric point5.99Not Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesL03AB04
AHFS CodesNot Available
PDB Entries
FDA labelDownload (204 KB)
MSDSNot Available
Interactions
Drug InteractionsNot Available
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
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. Cironi P, Swinburne IA, Silver PA: Enhancement of cell type specificity by quantitative modulation of a chimeric ligand. J Biol Chem. 2008 Mar 28;283(13):8469-76. doi: 10.1074/jbc.M708502200. Epub 2008 Jan 29. [PubMed:18230610 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
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. Cironi P, Swinburne IA, Silver PA: Enhancement of cell type specificity by quantitative modulation of a chimeric ligand. J Biol Chem. 2008 Mar 28;283(13):8469-76. doi: 10.1074/jbc.M708502200. Epub 2008 Jan 29. [PubMed:18230610 ]
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Drug created on June 13, 2005 07:24 / Updated on April 29, 2016 15:45