Interferon alfa-2b

Identification

Name
Interferon alfa-2b
Accession Number
DB00105
Description

Interferon alpha 2b (human leukocyte clone hif-sn 206 protein moiety reduced). A type I interferon consisting of 165 amino acid residues with arginine 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.

Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Interferons
Protein Structure
Db00105
Protein Chemical Formula
C860H1353N229O255S9
Protein Average Weight
19271.0 Da
Sequences
>DB00105 sequence
CDLPQTHSLGSRRTLMLLAQMRRISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMI
QQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMNEDSILAVR
KYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE
Download FASTA Format
Synonyms
  • Interferon alfa-2b
  • Interferon alfa-2b, recombinant
  • Interferon alpha-2B
  • Interferon α-2b
  • Intron (Interferon α2b)
  • Intron A
  • Intron A (Interferon α2b)
  • r-INF-alpha
  • rIFN-alpha-2b
External IDs
  • 99210-65-8
  • SCH 30500
  • SCH-30500
  • YM 14090

Pharmacology

Indication

For the treatment of hairy cell leukemia, malignant melanoma, and AIDS-related Kaposi's sarcoma.

Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Upregulates 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 action

Interferon 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.

TargetActionsOrganism
AInterferon alpha/beta receptor 2
binder
Humans
AInterferon alpha/beta receptor 1
binder
Humans
Absorption

Absorption is high (greater than 80%) when administered intramuscularly or subcutaneously.

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half-life

The elimination half-life following both intramuscular and subcutaneous injections was approximately 2 to 3 hours. The elimination half-life was approximately 2 hours following intravenous injection.

Clearance
Not Available
Adverse Effects
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Toxicity

There is limited experience with overdosage. Postmarketing surveillance includes reports of patients receiving a single dose as great as 10 times the recommended dose. In general, the primary effects of an overdose are consistent with the effects seen with therapeutic doses of interferon alfa-2b. Hepatic enzyme abnormalities, renal failure, hemorrhage, and myocardial infarction have been reported with single administration overdoses and/or with longer durations of treatment than prescribed. Toxic effects after ingestion of interferon alfa-2b are not expected because interferons are poorly absorbed orally.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbataceptThe risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Abatacept.
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Interferon alfa-2b.
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Interferon alfa-2b.
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Interferon alfa-2b.
Acetylsalicylic acidThe risk or severity of bleeding can be increased when Acetylsalicylic acid is combined with Interferon alfa-2b.
AcyclovirThe metabolism of Acyclovir can be decreased when combined with Interferon alfa-2b.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Interferon alfa-2b.
Adenovirus type 7 vaccine liveThe risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Interferon alfa-2b.
AgomelatineThe metabolism of Agomelatine can be decreased when combined with Interferon alfa-2b.
AlbendazoleThe metabolism of Albendazole can be decreased when combined with Interferon alfa-2b.
Additional Data Available
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  • Severity
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  • Evidence Level
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  • Action
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Food Interactions
  • Avoid alcohol.

Products

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International/Other Brands
Locteron
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Intron AKit38 ug/1mLIntralesional; Intramuscular; Intravenous; SubcutaneousMerck Sharp & Dohme Corp.2014-08-11Not applicableUS flag
Intron AKit38 ug/1mLIntralesional; Intramuscular; Intravenous; SubcutaneousMerck Sharp & Dohme Limited1986-06-042016-07-31US flag
Intron AInjection, solution11.6 ug/0.5mLIntramuscular; SubcutaneousMerck Sharp & Dohme Corp.1986-06-04Not applicableUS flag
Intron ALiquid15000000 unitSubcutaneousMerck Ltd.1999-09-232018-12-20Canada flag
Intron AKit192 ug/1mLIntramuscular; Intravenous; SubcutaneousMerck Sharp & Dohme Limited1986-06-042016-07-31US flag
Intron ASolution6000000 unitIntramuscular; Intravenous; SubcutaneousMerck Ltd.1998-12-10Not applicableCanada flag
Intron AKit192 ug/1mLIntramuscular; Intravenous; SubcutaneousMerck Sharp & Dohme Corp.2014-08-11Not applicableUS flag
Intron AInjection, solution38.4 ug/0.2mLSubcutaneousSchering-Plough Corporation2008-05-222008-05-22US flag
Intron ALiquid50000000 unitSubcutaneousMerck Ltd.1999-09-232018-12-14Canada flag
Intron ASolution10000000 unitIntramuscular; Intravenous; SubcutaneousMerck Ltd.1998-12-10Not applicableCanada flag
Additional Data Available
  • Application Number
    Application Number
    Available for Purchase

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code
    Available for Purchase

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Intron AInterferon alfa-2b (10000000 unit) + Water (1 ml)Liquid; Powder, for solutionIntralesional; Intramuscular; Intravenous; SubcutaneousMerck Ltd.1997-03-12Not applicableCanada flag
Intron AInterferon alfa-2b (18 miu) + Water (1 ml)Kit; Liquid; Powder, for solutionIntralesional; Intramuscular; Intravenous; SubcutaneousMerck Ltd.1998-03-112017-08-09Canada flag
Intron A - Kit (pws+diluent) 3000000iu/vialInterferon alfa-2b (3000000 unit) + Water (1 ml)Liquid; Powder, for solutionIntralesional; Intramuscular; SubcutaneousSchering Plough (Brinny) Co.1997-04-082000-07-11Canada flag
Intron A - Kit (pws+diluent) 5000000iu/vialInterferon alfa-2b (5000000 unit) + Water (1 ml)Liquid; Powder, for solutionIntralesional; Intramuscular; SubcutaneousSchering Plough (Brinny) Co.1998-12-312000-07-11Canada flag
Rebetron Ready To Use Solution (albumin(human)free) (6000000 Iu/ml and 200mg Capsules)Interferon alfa-2b (6000000 unit) + Ribavirin (200 mg)Capsule; Kit; LiquidOral; SubcutaneousSchering Plough1999-03-312004-10-27Canada flag
Rebetron Solution (albumin (human) Free) (18 Miu Multi-dose Pen / 200mg Capsules)Interferon alfa-2b (15000000 unit) + Ribavirin (200 mg)Capsule; Kit; LiquidOral; SubcutaneousSchering Plough1999-12-232004-10-27Canada flag

Categories

ATC Codes
L03AB05 — Interferon alfa-2b
Drug Categories
Chemical TaxonomyProvided by Classyfire
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

Chemical Identifiers

UNII
43K1W2T1M6
CAS number
98530-12-2

References

General References
  1. Radhakrishnan R, Walter LJ, Hruza A, Reichert P, Trotta PP, Nagabhushan TL, Walter MR: Zinc mediated dimer of human interferon-alpha 2b revealed by X-ray crystallography. Structure. 1996 Dec 15;4(12):1453-63. [PubMed:8994971]
UniProt
P01563
PubChem Substance
46507075
RxNav
5880
Therapeutic Targets Database
DAP001285
PharmGKB
PA164783990
RxList
RxList Drug Page
Wikipedia
Interferon_alfa-2b
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
  • 08:18.20 — Interferons
FDA label
Download (3.52 MB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedPreventionAdvanced Fibrosis / Hepatitis C Virus (HCV) Infection / Liver Cirrhosis1
4CompletedTreatmentChronic Hepatitis C Virus (HCV) Infection2
4CompletedTreatmentConjunctival Intraepithelial Neoplasia / Corneal Intraepithelial Neoplasia1
4CompletedTreatmentHepatitis B Chronic Infection1
4CompletedTreatmentHerpangina1
4RecruitingTreatmentEssential Thrombocytopenia1
4TerminatedTreatmentChronic Hepatitis C Virus (HCV) Infection2
4TerminatedTreatmentChronic Hepatitis C Virus (HCV) Infection / Insulin Resistance1
4TerminatedTreatmentMalignant Lymphomas / Precancerous/Nonmalignant Condition1
4Unknown StatusTreatmentLymphoma, T-Cell, Cutaneous / Mycosis Fungoides (MF)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Physicians Total Care Inc.
  • Schering Corp.
  • Schering-Plough Inc.
Dosage Forms
FormRouteStrength
Injection, powder, lyophilized, for solution0.3 mg
Injection, powder, for solution5 MU
Injection, solution10 MU/1mL
Injection, powder, for solution10 MU
Injection, powder, for solution3 MU
Injection, solutionIntralesional; Intramuscular; Subcutaneous19.2 ug/0.5mL
Injection, solutionIntramuscular; Subcutaneous11.6 ug/0.5mL
Injection, solutionSubcutaneous11.6 ug/0.2mL
Injection, solutionSubcutaneous19.2 ug/0.2mL
Injection, solutionSubcutaneous38.4 ug/0.2mL
KitIntralesional; Intramuscular; Intravenous; Subcutaneous38 ug/1mL
KitIntramuscular; Intravenous; Subcutaneous192 ug/1mL
KitIntramuscular; Intravenous; Subcutaneous69 ug/1mL
Kit; liquid; powder, for solutionIntralesional; Intramuscular; Intravenous; Subcutaneous
LiquidSubcutaneous15000000 unit
LiquidSubcutaneous25000000 unit
LiquidSubcutaneous50000000 unit
Liquid; powder, for solutionIntralesional; Intramuscular; Intravenous; Subcutaneous
SolutionIntramuscular; Intravenous; Subcutaneous10000000 unit
SolutionIntramuscular; Intravenous; Subcutaneous6000000 unit
Liquid; powder, for solutionIntralesional; Intramuscular; Subcutaneous
LiquidIntralesional; Intramuscular; Subcutaneous
Injection, solution6 unit/1mL
Injection, solution18 MU/1.2mL
Injection, solution30 MU/1.2mL
Injection, solution5 MU/0.5mL
LiquidSubcutaneous
Injection, solution10 miu/1ml
SolutionIntramuscular; Intravenous; Subcutaneous18 miu
SolutionIntramuscular; Intravenous; Subcutaneous30 miu
SolutionIntramuscular; Intravenous; Subcutaneous60 miu
Capsule; kit; liquidOral; Subcutaneous
Prices
Unit descriptionCostUnit
Intron-A 10000000 unit/0.2ml Kit (each Box Contains One 6 Dose 1.5ml Pen)1110.84USD box
Intron a 10 million unit pen1068.12USD pen
Intron-A 5000000 unit/0.2ml Kit Box683.34USD box
Intron a 5 million unit/ml pen657.06USD pen
Intron a 3 million unit/ml pen394.21USD pen
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
CA1341567No2008-02-192025-02-19Canada flag
CA2201749No1999-06-152015-10-10Canada flag
Additional Data Available
  • Filed On
    Filed On
    Available for Purchase

    The date on which a patent was filed with the relevant government.

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Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)61 °CBeldarrain, A. et al., Biochemistry 38:7865-7873 (1999)
hydrophobicity-0.339Not Available
isoelectric point5.99Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Binder
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. 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. Eid P, Tovey MG: Characterization of a domain of a human type I interferon receptor protein involved in ligand binding. J Interferon Cytokine Res. 1995 Mar;15(3):205-11. [PubMed:7584665]
  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
Humans
Pharmacological action
Yes
Actions
Binder
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. 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. Khine AA, Lingwood CA: Functional significance of globotriaosyl ceramide in interferon-alpha(2)/type 1 interferon receptor-mediated antiviral activity. J Cell Physiol. 2000 Jan;182(1):97-108. [PubMed:10567921]
  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
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
The package insert states that 1 dose of this agent does not inhibit CYP1A2, however, after multiple doses, inhibition may occur [A39128, A39129].
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. Islam M, Frye RF, Richards TJ, Sbeitan I, Donnelly SS, Glue P, Agarwala SS, Kirkwood JM: Differential effect of IFNalpha-2b on the cytochrome P450 enzyme system: a potential basis of IFN toxicity and its modulation by other drugs. Clin Cancer Res. 2002 Aug;8(8):2480-7. [PubMed:12171873]
  2. Wong SF, Jakowatz JG, Taheri R: Potential drug-drug interaction between interferon alfa-2b and gemfibrozil in a patient with malignant melanoma. Clin Ther. 2005 Dec;27(12):1942-8. doi: 10.1016/j.clinthera.2005.12.002. [PubMed:16507380]
  3. PEG-Intron package insert [File]

Drug created on June 13, 2005 07:24 / Updated on November 30, 2020 13:38

Th 1