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
Db00060
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
  • SNG001

Pharmacology

Indication

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

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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.

TargetActionsOrganism
AInterferon alpha/beta receptor 1
agonist
Humans
AInterferon alpha/beta receptor 2Not AvailableHumans
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
Adverseeffects
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Toxicity

Not Available

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
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Interferon beta-1a.
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Interferon beta-1a.
AcyclovirThe metabolism of Acyclovir can be decreased when combined with Interferon beta-1a.
Adenovirus type 7 vaccine liveThe therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Interferon beta-1a.
AgomelatineThe metabolism of Agomelatine can be decreased when combined with Interferon beta-1a.
AlbendazoleThe metabolism of Albendazole can be decreased when combined with Interferon beta-1a.
AlosetronThe metabolism of Alosetron can be decreased when combined with Interferon beta-1a.
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Interferon beta-1a.
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Interferon beta-1a.
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Interferon beta-1a.
Interactions
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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

Products2
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International/Other Brands
Betaferon (Bayer) / Blastoferon (Sidus) / Uribeta (Probiomed)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AvonexInjection, solution30 mcg/0.5mlIntramuscularBiogen Netherlands B.V.2016-09-08Not applicableEU flag
AvonexPowder, for solution60 mcg / mLIntramuscularBiogenNot applicableNot applicableCanada flag
AvonexInjection, solution30 mcg/0.5mlIntramuscularBiogen Netherlands B.V.2016-09-08Not applicableEU flag
AvonexSolution30 mcg / 0.5 mLIntramuscularBiogen2005-12-02Not applicableCanada flag
AvonexInjection, powder, for solution30 mcgIntramuscularBiogen Netherlands B.V.2016-09-082019-07-26EU flag
AvonexInjection, powder, lyophilized, for solution30 ug/1mLIntramuscularBiogen Inc.1996-05-172016-07-31US flag
AvonexInjection, solution30 mcg/0.5mlIntramuscularBiogen Netherlands B.V.2016-09-08Not applicableEU flag
AvonexInjection, solution30 ug/0.5mLIntramuscularBiogen Inc.2003-05-23Not applicableUS flag
AvonexInjection, solution30 mcg/0.5mlIntramuscularBiogen Netherlands B.V.2016-09-08Not applicableEU flag
Avonex PenInjection, solution30 ug/0.5mLIntramuscularBiogen Inc.2003-05-23Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
AvonexInterferon beta-1a (30 ug/0.5mL) + Isopropyl alcohol (0.70 mL/1mL)KitIntramuscularBiogen Inc.2014-08-29Not applicableUS flag
AvonexInterferon beta-1a (30 ug/0.5mL) + Isopropyl alcohol (0.70 mL/1mL)KitIntramuscularBiogen Inc.2014-08-29Not applicableUS flag
AvonexInterferon beta-1a (30 mcg / kit) + Water (1.1 mL / kit)Powder, for solutionIntramuscularBiogen1998-06-192010-10-30Canada flag
AvonexInterferon beta-1a (30 ug/1mL) + Isopropyl alcohol (0.70 mL/1mL)KitIntramuscularBiogen Inc.2014-08-29Not applicableUS flag
RebifInterferon beta-1a (11 mcg) + Sodium chloride (2 mL)Kit; Liquid; PowderIntralesional; SubcutaneousEmd Serono, A Division Of Emd Inc., Canada1998-04-032011-05-09Canada flag
RebifInterferon beta-1a (8.8 ug/0.2mL) + Interferon beta-1a (22 ug/0.5mL)KitSubcutaneousEMD Serono, Inc.2004-12-17Not applicableUS flag
RebifInterferon beta-1a (8.8 mcg / 0.2 mL) + Interferon beta-1a (22 mcg / 0.5 mL)Kit; Liquid; Powder, for solutionSubcutaneousEmd Serono, A Division Of Emd Inc., Canada2006-06-192013-08-09Canada flag
RebifInterferon beta-1a (8.8 ug/0.2mL) + Interferon beta-1a (22 ug/0.5mL)KitSubcutaneousEMD Serono, Inc.2004-12-17Not applicableUS flag
RebifInterferon beta-1a (8.8 mcg / 0.2 mL) + Interferon beta-1a (22 mcg / 0.5 mL)Kit; Liquid; Powder, for solutionSubcutaneousEmd Serono, A Division Of Emd Inc., Canada2006-06-192013-08-09Canada flag
Rebif RebidoseInterferon beta-1a (8.8 ug/0.2mL) + Interferon beta-1a (22 ug/0.5mL)KitSubcutaneousEMD Serono, Inc.2012-12-21Not applicableUS flag

Categories

ATC Codes
L03AB07 — Interferon beta-1a
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
Affected organisms
Not Available

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
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
PhaseStatusPurposeConditionsCount
4CompletedNot AvailableMultiple Sclerosis1
4CompletedBasic ScienceMultiple Sclerosis1
4CompletedOtherMultiple Sclerosis1
4CompletedTreatmentAcute Brainstem/Cerebellar Syndrome / Multiple Sclerosis / Optic Neuritis / Transverse Myelitis1
4CompletedTreatmentClinically Isolated Syndrome (CIS) / Relapsing Multiple Sclerosis (RMS)1
4CompletedTreatmentMultiple Sclerosis5
4CompletedTreatmentMultiple Sclerosis, Relapsing Forms of Multiple Sclerosis1
4CompletedTreatmentMultiple Sclerosis / Relapsing-Remitting1
4CompletedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)16
4Enrolling by InvitationTreatmentCoronavirus Disease 2019 (COVID‑19)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
FormRouteStrength
InjectionIntramuscular30 µg
Injection, powder, for solutionIntramuscular30 mcg
Injection, powder, for solutionIntramuscular30 MCG/0.5ML
Injection, powder, lyophilized, for solutionIntramuscular30 ug/1mL
Injection, solutionIntramuscular30 MCG/0.5ML
KitIntramuscular
Powder, for solutionIntramuscular
Powder, for solutionIntramuscular60 mcg / mL
SolutionIntramuscular30 mcg / 0.5 mL
SolutionIntramuscular30 MCG/0.5ML
Injection, solutionIntramuscular30 ug/0.5mL
SolutionIntramuscular30 mcg
SolutionSubcutaneous
Injection, solutionCutaneous; Parenteral
Injection, solutionParenteral; Subcutaneous22 MCG
Injection, solutionParenteral; Subcutaneous44 MCG
Injection, solutionSubcutaneous22 MCG/0.5ML
Injection, solutionSubcutaneous22 MCG
Injection, solutionSubcutaneous22 ug/0.5mL
Injection, solutionSubcutaneous22 µg/0.5ml
Injection, solutionSubcutaneous44 MCG
Injection, solutionSubcutaneous44 ug/0.5mL
Injection, solutionSubcutaneous44 µg/0.5ml
Injection, solutionSubcutaneous44 MCG/0.5ML
Injection, solutionSubcutaneous8.8 MCG
KitSubcutaneous
Kit; liquid; powderIntralesional; Subcutaneous
Kit; liquid; powder, for solutionSubcutaneous
SolutionSubcutaneous132 mcg / 1.5 mL
SolutionSubcutaneous22 mcg / 0.5 mL
SolutionSubcutaneous44 mcg / 0.5 mL
SolutionSubcutaneous66 mcg / 1.5 mL
SolutionSubcutaneous8.8 mcg / 0.2 mL
Injection, solution22 mcg/0.5ml
Injection, solution44 mcg/0.5ml
InjectionIntramuscular
Solution22 mcg/0.5ml
Injection, solutionSubcutaneous
Solution44 mcg/0.5ml
Injection, powder, for solutionIntramuscular
Prices
Unit descriptionCostUnit
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) Box3252.29USD box
Avonex admin pack 30 mcg vial781.8USD vial
Rebif 22 mcg/0.5 ml syringe247.79USD syringe
Rebif 44 mcg/0.5 ml syringe247.79USD syringe
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
CA1341604No2010-05-042027-05-04Canada flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource
hydrophobicity-0.427Not Available
isoelectric point8.93Not Available

Targets

Drugtargets2
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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
  1. 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]
  2. 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]
  3. 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]
  4. 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]
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
  1. 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]
  2. 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

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
  1. 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 on June 13, 2005 13:24 / Updated on October 22, 2021 23:18