Interferon alfa-2b
Identification
- Name
- Interferon alfa-2b
- Accession Number
- DB00105 (BTD00066, BIOD00066, DB05600)
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Interferons - 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.
- 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 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
- Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Unlock Additional DataIntron A Solution 10000000 unit Intramuscular; Intravenous; Subcutaneous Merck Ltd. 1998-12-10 Not applicable Canada 
Intron A 69 ug/1mL Intramuscular; Intravenous; Subcutaneous Merck Sharp & Dohme Corp. 2014-08-11 Not applicable US 
Intron A Injection, solution 11.6 ug/0.2mL Subcutaneous Schering-Plough Corporation 2008-05-22 2008-05-22 US Intron A Solution 6000000 unit Intramuscular; Intravenous; Subcutaneous Merck Ltd. 1998-12-10 Not applicable Canada Intron A 38 ug/1mL Intralesional; Intramuscular; Intravenous; Subcutaneous Merck Sharp & Dohme Corp. 2014-08-11 Not applicable US Intron A Kit 192 ug/1mL Intramuscular; Intravenous; Subcutaneous Merck Sharp & Dohme Limited 1986-06-04 2016-07-31 US Intron A Liquid 50000000 unit Subcutaneous Merck Ltd. 1999-09-23 2018-12-14 Canada Intron A Injection, solution 19.2 ug/0.5mL Intralesional; Intramuscular; Subcutaneous Merck Sharp & Dohme Corp. 1986-06-04 Not applicable US Intron A Kit 69 ug/1mL Intramuscular; Intravenous; Subcutaneous Merck Sharp & Dohme Limited 1986-06-04 2016-07-31 US Intron A Liquid 25000000 unit Subcutaneous Merck Ltd. 1999-09-23 2019-02-20 Canada Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Intron A Interferon alfa-2b (10000000 unit) + Water (1 ml) Liquid; Powder, for solution Intralesional; Intramuscular; Intravenous; Subcutaneous Merck Ltd. 1997-03-12 Not applicable Canada Intron A Interferon alfa-2b (18 miu) + Water (1 ml) Kit; Liquid; Powder, for solution Intralesional; Intramuscular; Intravenous; Subcutaneous Merck Ltd. 1998-03-11 Not applicable Canada Intron A - Kit (pws+diluent) 3000000iu/vial Interferon alfa-2b (3000000 unit) + Water (1 ml) Liquid; Powder, for solution Intralesional; Intramuscular; Subcutaneous Schering Plough (Brinny) Co. 1997-04-08 2000-07-11 Canada Intron A - Kit (pws+diluent) 5000000iu/vial Interferon alfa-2b (5000000 unit) + Water (1 ml) Liquid; Powder, for solution Intralesional; Intramuscular; Subcutaneous Schering Plough (Brinny) Co. 1998-12-31 2000-07-11 Canada Rebetron Ready To Use Solution (albumin(human)free) (6000000 Iu/ml and 200mg Capsules) Interferon alfa-2b (6000000 unit) + Ribavirin (200 mg) Capsule; Kit; Liquid Oral; Subcutaneous Schering Plough 1999-03-31 2004-10-27 Canada Rebetron Solution (albumin (human) Free) (18 Miu Multi-dose Pen / 200mg Capsules) Interferon alfa-2b (15000000 unit) + Ribavirin (200 mg) Capsule; Kit; Liquid Oral; Subcutaneous Schering Plough 1999-12-23 2004-10-27 Canada - International/Other Brands
- Locteron
- Categories
- Adjuvants, Immunologic
- Alfa Interferons
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
- Cytochrome P-450 Enzyme Inhibitors
- Hepatotoxic Agents
- Immunosuppressive Agents
- Interferon alpha
- Interferons
- Myelosuppressive Agents
- UNII
- 43K1W2T1M6
- CAS number
- 98530-12-2
Pharmacology
- Indication
For the treatment of hairy cell leukemia, malignant melanoma, and AIDS-related Kaposi's sarcoma.
- Associated Conditions
- 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 binderHumans AInterferon alpha/beta receptor 1 binderHumans - 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
- 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
Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.
Learn moreStructured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.
Learn moreStructured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.
Learn moreInteractions
- 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.
Drug Interaction Unlock Additional Data(R)-warfarin The metabolism of (R)-warfarin can be decreased when combined with Interferon alfa-2b. (S)-Warfarin The risk or severity of bleeding can be increased when (S)-Warfarin is combined with Interferon alfa-2b. 2-Methoxyethanol The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with 2-Methoxyethanol. 3-isobutyl-1-methyl-7H-xanthine The metabolism of 3-isobutyl-1-methyl-7H-xanthine can be decreased when combined with Interferon alfa-2b. 4-hydroxycoumarin The risk or severity of bleeding can be increased when 4-hydroxycoumarin is combined with Interferon alfa-2b. 6-O-benzylguanine The metabolism of 6-O-benzylguanine can be decreased when combined with Interferon alfa-2b. 7-Deazaguanine The metabolism of 7-Deazaguanine can be decreased when combined with Interferon alfa-2b. 7,9-Dimethylguanine The metabolism of 7,9-Dimethylguanine can be decreased when combined with Interferon alfa-2b. 8-azaguanine The metabolism of 8-azaguanine can be decreased when combined with Interferon alfa-2b. 8-chlorotheophylline The metabolism of 8-chlorotheophylline can be decreased when combined with Interferon alfa-2b. Additional Data Available- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - Severity
- Evidence Level
- ActionAction
An effect category for each drug interaction. Know how this interaction affects the subject drug.
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- Food Interactions
- Avoid alcohol.
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. [PubMed:8994971]
- External Links
- UniProt
- P01563
- PubChem Substance
- 46507075
- Therapeutic Targets Database
- DAP001285
- PharmGKB
- PA164783990
- RxList
- RxList Drug Page
- Wikipedia
- Interferon_alfa-2b
- ATC Codes
- L03AB05 — Interferon alfa-2b
- AHFS Codes
- 10:00.00 — Antineoplastic Agents
- 08:18.20 — Interferons
- FDA label
- Download (3.52 MB)
Clinical Trials
- Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Physicians Total Care Inc.
- Schering Corp.
- Schering-Plough Inc.
- Dosage forms
Form Route Strength 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 Liquid Subcutaneous 25000000 unit Liquid Subcutaneous 50000000 unit Liquid; powder, for solution Intralesional; Intramuscular; Intravenous; Subcutaneous Solution Intramuscular; Intravenous; Subcutaneous 10000000 unit Solution Intramuscular; Intravenous; Subcutaneous 6000000 unit Liquid; powder, for solution Intralesional; Intramuscular; Subcutaneous Liquid Intralesional; Intramuscular; Subcutaneous Liquid Subcutaneous Capsule; kit; liquid Oral; 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) Unlock Additional DataCA1341567 No 2008-02-19 2025-02-19 Canada CA2201749 No 1999-06-15 2015-10-10 Canada Additional Data Available- Filed On
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
Taxonomy
- 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
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
- 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]
- 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]
- 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]
- 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
- 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]
- 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]
- 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]
- 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
- 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]
- 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]
- PEG-Intron package insert [File]
Drug created on June 13, 2005 07:24 / Updated on January 20, 2020 02:39