Interferon beta-1a

Identification

Summary

Interferon beta-1a is a form of recombinant human interferon used to slow disease progression and reduce the frequency of clinical symptoms in patients who have relapsing multiple sclerosis.

Brand Names

Avonex, Rebif

Generic Name

Interferon beta-1a

DrugBank Accession Number

DB00060

Background

Human interferon beta (166 residues), glycosylated, MW=22.5kD. It is produced by mammalian cells (Chinese Hamster Ovary cells) into which the human interferon beta gene has been introduced. The amino acid sequence is identical to that of natural human interferon beta.

Type

Biotech

Groups

Approved, Investigational

Biologic Classification

Protein Based Therapies
Interferons

Protein Structure

Protein Chemical Formula: C₉₀₈H₁₄₀₈N₂₄₆O₂₅₂S₇
Protein Average Weight: 20027.0 Da

Sequences

>DB00060 sequence
MSYNLLGFLQRSSNFQCQKLLWQLNGRLEYCLKDRMNFDIPEEIKQLQQFQKEDAALTIY
EMLQNIFAIFRQDSSSTGWNETIVENLLANVYHQINHLKTVLEEKLEKEDFTRGKLMSSL
HLKRYYGRILHYLKAKEYSHCAWTIVRVEILRNFYFINRLTGYLRN

Download FASTA Format

Synonyms

Interferon beta 1-a
Interferon beta 1a
Interferon beta-1a
Interferon beta-1a (recombinant human)
Interferon beta-1a (recombinant)
Interferon beta-1a,recombinant
Interferon beta, recombinant human
Interferon-beta-1a
SNG001

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Pharmacology

Indication

For treatment of relapsing/remitting multiple sclerosis, also for condyloma acuminatum

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Management of	Relapsing multiple sclerosis (rms)		••••••••••••	•••••		•••••••••• •••

Contraindications & Blackbox Warnings

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Pharmacodynamics

Interferon beta 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. Type I interferons also induce the synthesis of several key antiviral mediators including 2'-5' oligoadenylate synthetase (2'-5' A synthetase), beta-2 microglobulin and neopterin.

Mechanism of action

Interferon beta 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 beta binds more stably to type I interferon receptors than interferon alpha.

Target	Actions	Organism
AInterferon alpha/beta receptor 1	agonist	Humans
AInterferon alpha/beta receptor 2	Not Available	Humans

Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Not Available

Route of elimination

Not Available

Half-life

10 hrs

Clearance

33-55 L/hour [Healthy SC injection of 60 mcg]

Adverse Effects

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Toxicity

Not Available

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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Acenocoumarol	The metabolism of Acenocoumarol can be decreased when combined with Interferon beta-1a.
Acetaminophen	The metabolism of Acetaminophen can be decreased when combined with Interferon beta-1a.
Acyclovir	The metabolism of Acyclovir can be decreased when combined with Interferon beta-1a.
Adenovirus type 7 vaccine live	The therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Interferon beta-1a.
Agomelatine	The metabolism of Agomelatine can be decreased when combined with Interferon beta-1a.

Food Interactions

Avoid excessive or chronic alcohol consumption. Alcohol and interferon beta-1a can both cause hepatoxicity, therefore if they are used together they may have additive hepatoxic effects.

Products

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International/Other Brands

Betaferon (Bayer) / Blastoferon (Sidus) / Uribeta (Probiomed)

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Avonex	Injection, solution	30 mcg/0.5ml	Intramuscular	Biogen Netherlands B.V.	2016-09-08	Not applicable
Avonex	Injection, solution	30 ug/0.5mL	Intramuscular	Biogen Inc.	2003-05-23	Not applicable
Avonex	Injection, powder, for solution	30 mcg	Intramuscular	Biogen Netherlands B.V.	2016-09-08	2019-07-26
Avonex	Injection, solution	30 mcg/0.5ml	Intramuscular	Biogen Netherlands B.V.	2016-09-08	Not applicable
Avonex	Injection, solution	30 mcg/0.5ml	Intramuscular	Biogen Netherlands B.V.	2016-09-08	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
Avonex	Interferon beta-1a (30 ug/1mL) + Isopropyl alcohol (0.70 mL/1mL)	Kit	Intramuscular	Biogen Inc.	2014-08-29	2020-02-29
Avonex	Interferon beta-1a (30 ug/0.5mL) + Isopropyl alcohol (0.70 mL/1mL)	Kit	Intramuscular	Biogen Inc.	2014-08-29	Not applicable
Avonex	Interferon beta-1a (30 ug/0.5mL) + Isopropyl alcohol (0.70 mL/1mL)	Kit	Intramuscular	Biogen Inc.	2014-08-29	Not applicable
Avonex	Interferon beta-1a (30 mcg / kit) + Water (1.1 mL / kit)	Powder, for solution	Intramuscular	Biogen	1998-06-19	2010-10-30
REBIF	Interferon beta-1a (8.8 mcg/0.1ml) + Interferon beta-1a (22 mcg/0.25ml) + Interferon beta-1a (24 M UI/ml)	Injection, solution	Cutaneous; Parenteral	Merck Europe B.V.	2014-07-08	Not applicable

Chemical Identifiers

UNII: XRO4566Q4R
CAS number: 145258-61-3

References

Synthesis Reference

Heinz-Jurgen Friesen, Sidney Pestka, "Preparation of homogeneous human fibroblast interferon." U.S. Patent US4289689, issued December, 1968.

US4289689

General References

Not Available

External Links

UniProt: P01574
Genbank: V00534
PubChem Substance: 46504899
RxNav: 75917
ChEMBL: CHEMBL1201562
Therapeutic Targets Database: DAP001282
PharmGKB: PA450037
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
Wikipedia: Interferon_beta-1a

FDA label

Download (63 KB)

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	Not Available	Multiple Sclerosis	1
4	Completed	Basic Science	Multiple Sclerosis	1
4	Completed	Other	Multiple Sclerosis	1
4	Completed	Treatment	Acute Brainstem/Cerebellar Syndrome / Multiple Sclerosis / Optic Neuritis / Transverse Myelitis	1
4	Completed	Treatment	Clinically Isolated Syndrome (CIS) / Relapsing Multiple Sclerosis (RMS)	1

Pharmacoeconomics

Manufacturers

Biogen Idec

Packagers

Biogen Idec Inc.
EMD Canada Inc.
Merck KGaA
Merck Serono SPA
Pierre Fabre
Vetter Pharma Fertigung GmbH and Co. KG

Dosage Forms

Form	Route	Strength
Injection	Intramuscular	30 µg
Injection, powder, for solution	Intramuscular	30 mcg
Injection, powder, for solution	Intramuscular	30 MCG/0.5ML
Injection, powder, lyophilized, for solution	Intramuscular	30 ug/1mL
Injection, solution	Intramuscular	30 MCG/0.5ML
Kit	Intramuscular
Powder, for solution	Intramuscular
Powder, for solution	Intramuscular	60 mcg / mL
Solution	Intramuscular	30 MCG/0.5ML
Solution	Intramuscular	30 mcg / 0.5 mL
Solution	Intramuscular	30.000 mcg
Injection	Intramuscular	30 mcg/0.5ml
Injection, solution	Intramuscular	30 ug/0.5mL
Solution	Intramuscular	30 mcg
Solution	Subcutaneous
Injection, solution	Cutaneous; Parenteral
Injection, solution	Parenteral; Subcutaneous	22 MCG
Injection, solution	Parenteral; Subcutaneous	44 MCG
Injection, solution	Subcutaneous	22 ug/0.5mL
Injection, solution	Subcutaneous	22 µg/0.5ml
Injection, solution	Subcutaneous	22 MCG
Injection, solution	Subcutaneous	44 µg/0.5ml
Injection, solution	Subcutaneous	44 MCG
Injection, solution	Subcutaneous	44 ug/0.5mL
Injection, solution	Subcutaneous	8.8 MCG
Kit	Subcutaneous
Kit; liquid; powder	Intralesional; Subcutaneous
Kit; liquid; powder, for solution	Subcutaneous
Solution	Subcutaneous	132 mcg / 1.5 mL
Solution	Subcutaneous	22 mcg / 0.5 mL
Solution	Subcutaneous	44 mcg / 0.5 mL
Solution	Subcutaneous	66 mcg / 1.5 mL
Solution	Subcutaneous	8.8 mcg / 0.2 mL
Injection, solution		22 mcg/0.5ml
Injection, solution		44 mcg/0.5ml
Injection, solution	Subcutaneous	132 mcg/1.5ml
Injection	Intramuscular
Solution		22 mcg/0.5ml
Injection, solution	Subcutaneous
Solution		44 mcg/0.5ml
Injection, solution	Subcutaneous	66 mcg/1.5ml
Solution	Subcutaneous	66.000 µg
Injection, solution	Subcutaneous	22 mcg/0.5mL
Injection, solution	Subcutaneous	44 mcg/0.5mL
Injection, powder, for solution	Intramuscular
Solution	Parenteral	30.000 mcg

Prices

Unit description	Cost	Unit
Avonex 4 30 mcg/vial Kit 1 Box = 4 Vials ( 0.5ml Per Vial)	3252.29USD	box
Avonex Prefilled (1 Box = 1 Kit = Four 30 mcg/0.5ml Syringes) Box	3252.29USD	box
Avonex admin pack 30 mcg vial	781.8USD	vial
Rebif 22 mcg/0.5 ml syringe	247.79USD	syringe
Rebif 44 mcg/0.5 ml syringe	247.79USD	syringe

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

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
CA1341604	No	2010-05-04	2027-05-04

Properties

State

Liquid

Experimental Properties

Property	Value	Source
hydrophobicity	-0.427	Not Available
isoelectric point	8.93	Not Available

Targets

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Details1. Interferon alpha/beta receptor 1

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Agonist

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

Russell-Harde D, Wagner TC, Perez HD, Croze E: Formation of a uniquely stable type I interferon receptor complex by interferon beta is dependent upon particular interactions between interferon beta and its receptor and independent of tyrosine phosphorylation. Biochem Biophys Res Commun. 1999 Feb 16;255(2):539-44. [Article]
van Koetsveld PM, Vitale G, de Herder WW, Feelders RA, van der Wansem K, Waaijers M, van Eijck CH, Speel EJ, Croze E, van der Lely AJ, Lamberts SW, Hofland LJ: Potent inhibitory effects of type I interferons on human adrenocortical carcinoma cell growth. J Clin Endocrinol Metab. 2006 Nov;91(11):4537-43. Epub 2006 Aug 15. [Article]
Dupont SA, Goelz S, Goyal J, Green M: Mechanisms for regulation of cellular responsiveness to human IFN-beta1a. J Interferon Cytokine Res. 2002 Apr;22(4):491-501. [Article]
Runkel L, De Dios C, Karpusas M, Baker D, Li Z, Zafari M, Betzenhauser M, Muldowney C, Miller S, Redlich PN, Grossberg SE, Whitty A, Hochman PS: Mapping of IFN-beta epitopes important for receptor binding and biologic activation: comparison of results achieved using antibody-based methods and alanine substitution mutagenesis. J Interferon Cytokine Res. 2001 Nov;21(11):931-41. [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

van Koetsveld PM, Vitale G, de Herder WW, Feelders RA, van der Wansem K, Waaijers M, van Eijck CH, Speel EJ, Croze E, van der Lely AJ, Lamberts SW, Hofland LJ: Potent inhibitory effects of type I interferons on human adrenocortical carcinoma cell growth. J Clin Endocrinol Metab. 2006 Nov;91(11):4537-43. Epub 2006 Aug 15. [Article]
Runkel L, De Dios C, Karpusas M, Baker D, Li Z, Zafari M, Betzenhauser M, Muldowney C, Miller S, Redlich PN, Grossberg SE, Whitty A, Hochman PS: Mapping of IFN-beta epitopes important for receptor binding and biologic activation: comparison of results achieved using antibody-based methods and alanine substitution mutagenesis. J Interferon Cytokine Res. 2001 Nov;21(11):931-41. [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 February 20, 2024 23:55

Interferon beta-1a

Identification

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Targets

References

References

Enzymes

References