Interferon alfa-2a

Identification

Summary

Interferon alfa-2a is a form of recombinant human interferon used to stimulate the innate antiviral response in the treatment of hepatitis B and C viruses.

Generic Name

Interferon alfa-2a

DrugBank Accession Number

DB00034

Background

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.

Type

Biotech

Groups

Approved, Investigational

Biologic Classification

Protein Based Therapies
Interferons

Protein Structure

Protein Chemical Formula: C₈₆₀H₁₃₅₃N₂₂₇O₂₅₅S₉
Protein Average Weight: 19241.1 Da

Sequences

>DB00034 sequence
CDLPQTHSLGSRRTLMLLAQMRKISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMI
QQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMKEDSILAVR
KYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE

Download FASTA Format

Synonyms

Interferon alfa-2a
Interferon alfa-2a (genetical recombination)
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 IDs

RO 22-8181
RO-22-8181
RO-228181

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Pharmacology

Indication

For 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.

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Patient Characteristics	Dose Form
Treatment of	Chronic hepatitis c virus (hcv) infection		••••••••••••	•••••• ••••• ••••••••	•••••••••
Used as adjunct in combination to treat	Chronic hepatitis c virus (hcv) infection	Regimen in combination with: Ribavirin (DB00811)	••••••••••••	•••••••••• •• •••••••••• •••• •••••••• ••••••••• • •••••••	•••••••••
Treatment of	Chronic myeloid leukemia (cml)		••••••••••••		•••••••••
Treatment of	Cutaneous t-cell lymphoma (ctcl)		••••••••••••		•••••••••
Treatment of	Hairy cell leukemia (hcl)		••••••••••••		•••••••••

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 1	Not Available	Humans
AInterferon alpha/beta receptor 2	Not Available	Humans

Absorption

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

Volume of distribution

0.223 to 0.748 L/kg [healthy people]

Protein binding

Not Available

Metabolism

Not Available

Route of elimination

Alpha-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-life

The 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]

Adverse Effects

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Toxicity

Interferon 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.

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.

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

Food Interactions

Avoid alcohol.

Products

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International/Other Brands

Roferon A (Hoffmann-La Roche Inc) / Veldona (Amarillo Biosciences)

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Roferon A Soln Inj 6 Million	Liquid	6000000 unit / mL	Intramuscular; Subcutaneous	Hoffmann La Roche	1989-12-31	1997-08-26
Roferon A Sterile Pws 18m Unit/vial	Powder, for solution	18000000 unit / vial	Intramuscular; Subcutaneous	Hoffmann La Roche	1991-12-31	1996-09-30
Roferon A Sterile Pws 3m Unit/vial	Powder, for solution	3000000 unit / vial	Intramuscular; Subcutaneous	Hoffmann La Roche	1991-12-31	1996-09-30
Roferon A Sterile Pws 9m Unit/vial	Powder, for solution	9000000 unit / vial	Intramuscular; Subcutaneous	Hoffmann La Roche	1991-12-31	1996-09-30
Roferon-A	Injection, solution	11.1 ug/0.5mL	Subcutaneous	Genentech, Inc.	1986-06-04	2008-10-31

Chemical Identifiers

UNII: 47RRR83SK7
CAS number: 76543-88-9

References

General References

IlacaBak: Interferon alfa 2a ATC Sınıflaması [Link]

External Links

UniProt: P01563
Genbank: J00207
PubChem Substance: 46506712
RxNav: 5879
Therapeutic Targets Database: DAP000801
PharmGKB: PA164779048
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
Wikipedia: Peginterferon_alfa-2a

FDA label

Download (204 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Completed	Treatment	Chronic Hepatitis B Infection	1
4	Completed	Treatment	Chronic Hepatitis C Virus (HCV) Infection / End Stage Renal Disease (ESRD)	1
3	Completed	Treatment	Behçet's Disease / Uveitis	1
3	Completed	Treatment	Hepatitis C Virus (HCV) Infection	1
3	Completed	Treatment	Lymphoma	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

F Hoffmann La Roche Ltd.
F Hoffmann-La Roche Ltd.

Dosage Forms

Form	Route	Strength
Solution	Subcutaneous	3000000 IU
Injection	Subcutaneous
Injection, solution	Intramuscular; Parenteral; Subcutaneous
Injection, solution	Parenteral; Subcutaneous
Injection, solution	Subcutaneous
Liquid	Intramuscular; Subcutaneous	6000000 unit / mL
Powder, for solution	Intramuscular; Subcutaneous	18000000 unit / vial
Powder, for solution	Intramuscular; Subcutaneous	3000000 unit / vial
Powder, for solution	Intramuscular; Subcutaneous	9000000 unit / vial
Injection, solution	Subcutaneous	11.1 ug/0.5mL
Injection, solution	Subcutaneous	22.2 ug/0.5mL
Injection, solution	Subcutaneous	33.3 ug/0.5mL
Injection, solution	Subcutaneous	3000000 IU
Injection, solution	Subcutaneous	4500000 MIU
Injection, solution	Subcutaneous	6000000 IU
Injection, solution	Subcutaneous	9000000 IU
Injection	Intramuscular; Subcutaneous	3 MIU/0.5ml
Liquid	Intramuscular; Subcutaneous	3000000 unit / mL
Liquid	Intramuscular; Subcutaneous	4500000 IU/mL
Solution	Intramuscular; Subcutaneous	9000000 IU/ml
Solution	Intramuscular; Subcutaneous	18000000 IU/3mL
Solution	Intramuscular; Subcutaneous	3 m / mL
Solution	Intramuscular; Subcutaneous	6000000 IU/mL
Solution	Intramuscular; Subcutaneous	36000000 unit / mL
Solution	Intramuscular; Subcutaneous	9000000 unit / .9 mL

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
CA2172664	No	2000-10-03	2016-03-26

Properties

State

Liquid

Experimental Properties

Property	Value	Source
water solubility	100 mg/ml	Not Available
hydrophobicity	-0.336	Not Available
isoelectric point	5.99	Not Available

Targets

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Details1. Interferon alpha/beta receptor 1

Kind: Protein
Organism: Humans
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 JA...
Gene Name: IFNAR1
Uniprot ID: P17181
Uniprot Name: Interferon alpha/beta receptor 1
Molecular Weight: 63524.81 Da

References

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. [Article]
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. [Article]

Details2. Interferon alpha/beta receptor 2

Kind: Protein
Organism: Humans
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 direc...
Gene Name: IFNAR2
Uniprot ID: P48551
Uniprot Name: Interferon alpha/beta receptor 2
Molecular Weight: 57758.24 Da

References

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. [Article]
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. [Article]

Enzymes

Details1. Cytochrome P450 1A2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

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

Delaporte E, Renton KW: Cytochrome P4501A1 and cytochrome P4501A2 are downregulated at both transcriptional and post-transcriptional levels by conditions resulting in interferon-alpha/beta induction. Life Sci. 1997;60(10):787-96. doi: 10.1016/s0024-3205(97)00006-4. [Article]

Drug created at June 13, 2005 13:24 / Updated at April 09, 2024 18:10

Interferon alfa-2a

Identification

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Targets

References

References

Enzymes

References