Interferon alfa-2b

Identification

Summary

Interferon alfa-2b is a form of recombinant human interferon used to treat hepatitis B and C infection, genital warts, hairy cell leukemia, follicular lymphoma, malignant melanoma, and AIDs-related Kaposi's sarcoma.

Brand Names

Intron A

Generic Name

Interferon alfa-2b

DrugBank Accession Number

DB00105

Background

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

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 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

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Pharmacology

Indication

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

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Patient Characteristics	Dose Form
Used in combination to treat	Chronic hepatitis c virus (hcv) infection	Regimen in combination with: Ribavirin (DB00811)	••••••••••••	•••••••••• ••••••••••• ••••• •••••••	•••••••••• ••••••• ••••••••
Used in combination to treat	Chronic hepatitis c virus (hcv) infection	Regimen in combination with: Ribavirin (DB00811)	••••••••••••	••••••••••• ••••• •••••••	•••••••••• ••••••• ••••••••
Treatment of	Chronic hepatitis c virus (hcv) infection		••••••••••••	••••••••••• ••••• •••••••	•••••••••• ••••••• ••••••••
Treatment of	Condylomata acuminata (external)		••••••••••••		•••••••••• ••••••• ••••••••
Adjunct therapy in treatment of	Follicular non-hodgkin's lymphoma		••••••••••••		•••••••••• ••••••• ••••••••

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.

Target	Actions	Organism
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.

Pathways

Not Available

Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">

Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">

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.

Drug	Interaction
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Abatacept	The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Abatacept.
Abciximab	The risk or severity of bleeding can be increased when Abciximab is combined with Interferon alfa-2b.
Acenocoumarol	The metabolism of Acenocoumarol can be decreased when combined with Interferon alfa-2b.
Acetaminophen	The metabolism of Acetaminophen can be decreased when combined with Interferon alfa-2b.
Acetylsalicylic acid	The risk or severity of bleeding can be increased when Acetylsalicylic acid is combined with Interferon alfa-2b.

Food Interactions

Avoid alcohol.

Products

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International/Other Brands

Locteron

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Intron A	Injection, solution	38.4 ug/0.2mL	Subcutaneous	Schering-Plough Corporation	2008-05-22	2008-05-22
Intron A	Liquid	25000000 unit / mL	Subcutaneous	Merck Ltd.	1999-09-23	2019-02-20
Intron A	Injection, powder, for solution; Kit	192 ug/1mL	Intramuscular; Intravenous; Subcutaneous	Merck Sharp & Dohme Llc	2014-08-11	Not applicable
Intron A	Solution	6000000 unit / mL	Intramuscular; Intravenous; Subcutaneous	Merck Ltd.	1998-12-10	2021-08-31
Intron A	Liquid	50000000 unit / mL	Subcutaneous	Merck Ltd.	1999-09-23	2018-12-14

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
Intron A	Interferon alfa-2b (18 miu / vial) + Water (1 mL / vial)	Kit; Liquid; Powder, for solution	Intralesional; Intramuscular; Intravenous; Subcutaneous	Merck Ltd.	1998-03-11	2017-08-09
Intron A	Interferon alfa-2b (10000000 unit / vial) + Water (1 mL / vial)	Liquid; Powder, for solution	Intralesional; Intramuscular; Intravenous; Subcutaneous	Merck Ltd.	1997-03-12	2021-11-10
Intron A - Kit (pws+diluent) 3000000iu/vial	Interferon alfa-2b (3000000 unit / vial) + Water (1 mL / vial)	Liquid; Powder, for solution	Intralesional; Intramuscular; Subcutaneous	Schering Plough (Brinny) Co.	1997-04-08	2000-07-11
Intron A - Kit (pws+diluent) 5000000iu/vial	Interferon alfa-2b (5000000 unit / vial) + Water (1 mL / vial)	Liquid; Powder, for solution	Intralesional; Intramuscular; Subcutaneous	Schering Plough (Brinny) Co.	1998-12-31	2000-07-11
Rebetron Ready To Use Solution (albumin(human)free) (6000000 Iu/ml and 200mg Capsules)	Interferon alfa-2b (6000000 unit / mL) + Ribavirin (200 mg / cap)	Capsule; Kit; Liquid	Oral; Subcutaneous	Schering Plough	1999-03-31	2004-10-27

Chemical Identifiers

UNII: 43K1W2T1M6
CAS number: 98530-12-2

References

General References

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. [Article]
FDA Approved Drug Products: INTRON (Interferon alfa-2b) injection [Link]

External Links

UniProt: P01563
PubChem Substance: 46507075
RxNav: 5880
Therapeutic Targets Database: DAP001285
PharmGKB: PA164783990
RxList: RxList Drug Page
Wikipedia: Interferon_alfa-2b

FDA label

Download (3.52 MB)

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Completed	Prevention	Advanced Fibrosis / Cirrhosis of the Liver / Hepatitis C Virus (HCV) Infection	1
4	Completed	Treatment	Chronic Hepatitis B Infection	1
4	Completed	Treatment	Chronic Hepatitis C Virus (HCV) Infection	2
4	Completed	Treatment	Conjunctival Intraepithelial Neoplasia / Corneal Intraepithelial Neoplasia	1
4	Completed	Treatment	Herpangina	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Physicians Total Care Inc.
Schering Corp.
Schering-Plough Inc.

Dosage Forms

Form	Route	Strength
Injection, powder, lyophilized, for solution		0.3 mg
Injection, powder, for solution		10 MIU/1vial
Injection, powder, for solution		3 miu/1vial
Injection, powder, for solution		5 miu/1vial
Injection, powder, for solution; kit	Intralesional; Intramuscular; Intravenous; Subcutaneous	38 ug/1mL
Injection, powder, for solution; kit	Intramuscular; Intravenous; Subcutaneous	192 ug/1mL
Injection, powder, for solution; kit	Intramuscular; Intravenous; Subcutaneous	69 ug/1mL
Injection, solution	Intralesional; Intramuscular; Subcutaneous	19.2 ug/0.5mL
Injection, solution	Intramuscular; Subcutaneous	11.6 ug/0.5mL
Injection, solution	Subcutaneous	11.6 ug/0.2mL
Injection, solution	Subcutaneous	19.2 ug/0.2mL
Injection, solution	Subcutaneous	38.4 ug/0.2mL
Kit	Intralesional; Intramuscular; Intravenous; Subcutaneous	38 ug/1mL
Kit	Intramuscular; Intravenous; Subcutaneous	192 ug/1mL
Kit	Intramuscular; Intravenous; Subcutaneous	69 ug/1mL
Kit; liquid; powder, for solution	Intralesional; Intramuscular; Intravenous; Subcutaneous
Liquid	Subcutaneous	15000000 unit / mL
Liquid	Subcutaneous	25000000 unit / mL
Liquid	Subcutaneous	50000000 unit / mL
Liquid; powder, for solution	Intralesional; Intramuscular; Intravenous; Subcutaneous
Solution	Intramuscular; Intravenous; Subcutaneous	10000000 unit / mL
Solution	Intramuscular; Intravenous; Subcutaneous	6000000 unit / mL
Liquid; powder, for solution	Intralesional; Intramuscular; Subcutaneous
Liquid	Intralesional; Intramuscular; Subcutaneous	5000000 unit / mL
Liquid	Subcutaneous	10000000 unit / vial
Liquid	Subcutaneous	3000000 unit / vial
Liquid	Subcutaneous	5000000 unit / vial
Injection	Subcutaneous	18 miu
Injection	Subcutaneous	30 miu
Injection	Parenteral	3000000 IU
Injection	Parenteral	5000000 IU
Injection, solution		10 miu/1ml
Solution	Intramuscular; Intravenous; Subcutaneous	18 miu
Solution	Intramuscular; Intravenous; Subcutaneous	30 miu
Solution	Intramuscular; Intravenous; Subcutaneous	60 miu
Injection	Subcutaneous	18000000 IU
Injection	Subcutaneous	30000000 IU
Injection	Subcutaneous	60000000 IU
Injection, powder, for solution	Intravenous; Parenteral; Subcutaneous	3000.000 IU
Injection, powder, for solution	Intravenous; Parenteral; Subcutaneous	30000.000 IU
Injection, powder, for solution	Intravenous; Subcutaneous	1000.000 IU/0.5ml
Injection, powder, for solution	Intravenous; Subcutaneous	10000.000 IU/0.5ml
Injection, powder, for solution	Intravenous; Subcutaneous	18000.000 IU
Injection, powder, for solution	Intravenous; Subcutaneous	5000.000 IU
Injection, solution	Intravenous; Parenteral; Subcutaneous	25000.000 IU/2.5ml
Injection, solution	Intravenous; Parenteral; Subcutaneous	25000.000 IU
Injection, solution	Intravenous; Parenteral; Subcutaneous	3000.000 IU
Injection, solution	Intravenous; Subcutaneous	10000.000 IU/0.5ml
Injection, solution	Intravenous; Subcutaneous	10000000 IU/ml
Injection, solution	Intravenous; Subcutaneous	18000.000 IU/3ml
Injection, solution	Intravenous; Subcutaneous	18000.000 IU
Injection, solution	Intravenous; Subcutaneous	18000000 IU/3ml
Injection, solution	Intravenous; Subcutaneous	25000000 IU/2.5ml
Injection, solution	Intravenous; Subcutaneous	3000000 IU/0.5ml
Injection, solution	Intravenous; Subcutaneous	5000.000 IU
Injection, solution	Intravenous; Subcutaneous	5000000 IU/0.5ml
Injection, solution	Parenteral; Subcutaneous	18000.000 IU
Injection, solution	Parenteral; Subcutaneous	30000.000 IU
Injection, solution	Parenteral; Subcutaneous	60000.000 IU
Injection, solution	Subcutaneous	18000.000 IU
Capsule; kit; liquid	Oral; Subcutaneous
Injection, powder, for solution	Subcutaneous
Injection, powder, for solution	Subcutaneous	10 MIU
Injection, solution	Subcutaneous

Prices

Unit description	Cost	Unit
Intron-A 10000000 unit/0.2ml Kit (each Box Contains One 6 Dose 1.5ml Pen)	1110.84USD	box
Intron a 10 million unit pen	1068.12USD	pen
Intron-A 5000000 unit/0.2ml Kit Box	683.34USD	box
Intron a 5 million unit/ml pen	657.06USD	pen
Intron a 3 million unit/ml pen	394.21USD	pen

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
CA1341567	No	2008-02-19	2025-02-19
CA2201749	No	1999-06-15	2015-10-10

Properties

State

Liquid

Experimental Properties

Property	Value	Source
melting point (°C)	61 °C	Beldarrain, A. et al., Biochemistry 38:7865-7873 (1999)
hydrophobicity	-0.339	Not Available
isoelectric point	5.99	Not Available

Targets

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Details1. Interferon alpha/beta receptor 2

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

Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
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. [Article]
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. [Article]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]

Details2. Interferon alpha/beta receptor 1

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

Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
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. [Article]
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. [Article]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]

Enzymes

Details1. Cytochrome P450 1A2

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

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. [Article]
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. [Article]
PEG-Intron package insert [File]

Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:54

Interferon alfa-2b

Identification

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Targets

References

References

Enzymes

References