Identification

Name
Interferon beta-1a
Accession Number
DB00060  (BTD00093, BIOD00093)
Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Interferons
Description

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.

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 (recombinant human)
  • Interferon beta-1a,recombinant
  • Interferon-beta-1a
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AvonexInjection, powder, lyophilized, for solution30 ug/mLIntramuscularBiogen Idec Limited1996-05-172015-12-29Us
AvonexPowder, for solution60 mcgIntramuscularBiogenNot applicableNot applicableCanada
AvonexKitIntramuscularBiogen2014-08-29Not applicableUs
AvonexInjection, solution30 ug/.5mLIntramuscularBiogen Idec Limited2003-05-232015-12-29Us
AvonexKitIntramuscularBiogen2014-08-29Not applicableUs
AvonexSolution30 mcgIntramuscularBiogen2005-12-02Not applicableCanada
AvonexKitIntramuscularBiogen2014-08-29Not applicableUs
Avonex PenInjection, solution30 ug/.5mLIntramuscularBiogen Idec Limited2003-05-232015-12-29Us
RebifInjection, solution44 ug/.5mLSubcutaneousEmd Serono2002-03-07Not applicableUs
RebifInjection, solution22 ug/.5mLSubcutaneousEmd Serono2002-03-07Not applicableUs
International/Other Brands
Betaferon (Bayer) / Blastoferon (Sidus) / Uribeta (Probiomed)
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
AvonexInterferon beta-1a (30 mcg) + Water (1.1 ml)Powder, for solutionIntramuscularBiogen1998-06-192010-10-30Canada
RebifInterferon beta-1a (11 mcg) + Sodium Chloride (2 ml)Kit; Liquid; PowderIntralesional; SubcutaneousEmd Serono, A Division Of Emd Inc., Canada1998-04-032011-05-09Canada
RebifInterferon beta-1a (22 mcg) + Interferon beta-1a (8.8 mcg)Kit; Liquid; Powder, for solutionSubcutaneousEmd Serono, A Division Of Emd Inc., Canada2006-06-192013-08-09Canada
RebifInterferon beta-1a (22 mcg) + Interferon beta-1a (8.8 mcg)Kit; Liquid; Powder, for solutionSubcutaneousEmd Serono, A Division Of Emd Inc., Canada2006-06-192013-08-09Canada
Categories
UNII
XRO4566Q4R
CAS number
145258-61-3

Pharmacology

Indication

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

Structured Indications
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
Human
AInterferon alpha/beta receptor 2Not AvailableHuman
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]
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Interferon beta-1a.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Interferon beta-1a.Experimental
Ambroxol acefyllinateThe metabolism of Ambroxol acefyllinate can be decreased when combined with Interferon beta-1a.Experimental, Investigational
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Interferon beta-1a.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Interferon beta-1a.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Interferon beta-1a.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Interferon beta-1a.Approved, Investigational
CymarinCymarin may decrease the cardiotoxic activities of Interferon beta-1a.Experimental
DeslanosideDeslanoside may decrease the cardiotoxic activities of Interferon beta-1a.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Interferon beta-1a.Approved, Investigational
DigoxinDigoxin may decrease the cardiotoxic activities of Interferon beta-1a.Approved
Digoxin Immune Fab (Ovine)Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Interferon beta-1a.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Interferon beta-1a.Approved, Investigational
DyphyllineThe metabolism of Dyphylline can be decreased when combined with Interferon beta-1a.Approved
GitoformateGitoformate may decrease the cardiotoxic activities of Interferon beta-1a.Experimental
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Interferon beta-1a.Experimental
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Interferon beta-1a.Experimental
OleandrinOleandrin may decrease the cardiotoxic activities of Interferon beta-1a.Experimental, Investigational
OuabainOuabain may decrease the cardiotoxic activities of Interferon beta-1a.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Interferon beta-1a.Approved, Vet Approved
PeruvosidePeruvoside may decrease the cardiotoxic activities of Interferon beta-1a.Experimental
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Interferon beta-1a.Experimental
TheophyllineThe metabolism of Theophylline can be decreased when combined with Interferon beta-1a.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Interferon beta-1a.Approved, Investigational
ZidovudineThe risk or severity of adverse effects can be increased when Interferon beta-1a is combined with Zidovudine.Approved
Food Interactions
Not Available

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
ChEMBL
CHEMBL1201562
Therapeutic Targets Database
DAP001282
PharmGKB
PA450037
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Interferon_beta-1a
ATC Codes
L03AB07 — Interferon beta-1a
AHFS Codes
  • 92:20.00 — Immunomodulatory Agents
FDA label
Download (63 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedTreatmentDisseminated Sclerosis1
1CompletedNot AvailableDisseminated Sclerosis1
1CompletedNot AvailableHealthy Volunteers1
1CompletedBasic ScienceDisseminated Sclerosis2
1CompletedBasic ScienceHealthy Volunteers1
1CompletedTreatmentCerebrovascular Accidents1
1CompletedTreatmentDisseminated Sclerosis1
1CompletedTreatmentHealthy Volunteers3
1CompletedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)2
1RecruitingTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
2Active Not RecruitingTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
2CompletedNot AvailableDisseminated Sclerosis1
2CompletedBasic ScienceDisseminated Sclerosis1
2CompletedPreventionAsthma Bronchial1
2CompletedPreventionDisseminated Sclerosis1
2CompletedTreatmentActive Ulcerative Colitis1
2CompletedTreatmentAlzheimer's Disease (AD)1
2CompletedTreatmentAsthma Bronchial1
2CompletedTreatmentDisseminated Sclerosis5
2CompletedTreatmentPolyradiculoneuropathy, Chronic Inflammatory Demyelinating1
2CompletedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)3
2CompletedTreatmentUlcerative Colitis (UC)2
2TerminatedTreatmentCrohn's Disease (CD)1
2Unknown StatusTreatmentDisseminated Sclerosis1
2WithdrawnTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
2, 3Active Not RecruitingNot AvailableDisseminated Sclerosis1
2, 3RecruitingTreatmentDisseminated Sclerosis / Relapsing Remitting Multiple Sclerosis (RRMS)1
2, 3RecruitingTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
3Active Not RecruitingTreatmentDisseminated Sclerosis1
3Active Not RecruitingTreatmentRelapsing Multiple Sclerosis (RMS) / Relapsing Remitting Multiple Sclerosis (RRMS)2
3CompletedNot AvailableDisseminated Sclerosis2
3CompletedPreventionDisseminated Sclerosis1
3CompletedTreatmentChronic Hepatitis C Infection1
3CompletedTreatmentClinically Isolated Syndrome (CIS)1
3CompletedTreatmentClinically Isolated Syndrome (CIS) / Disseminated Sclerosis1
3CompletedTreatmentDisseminated Sclerosis3
3CompletedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)6
3RecruitingTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
3RecruitingTreatmentRespiratory Distress Syndrome, Adult1
3TerminatedNot AvailableRelapsing Remitting Multiple Sclerosis (RRMS)1
3TerminatedTreatmentDisseminated Sclerosis1
3WithdrawnTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
4CompletedNot AvailableDisseminated Sclerosis2
4CompletedNot AvailableRelapsing Remitting Multiple Sclerosis (RRMS)1
4CompletedBasic ScienceDisseminated Sclerosis1
4CompletedTreatmentClinically Isolated Syndrome (CIS) / Relapsing Multiple Sclerosis (RMS)1
4CompletedTreatmentDisseminated Sclerosis5
4CompletedTreatmentRelapsing Forms of Multiple Sclerosis1
4CompletedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)12
4RecruitingTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
4TerminatedNot AvailableRelapsing Remitting Multiple Sclerosis (RRMS)1
4TerminatedPreventionRelapsing Remitting Multiple Sclerosis (RRMS)1
4TerminatedTreatmentDisseminated Sclerosis1
4TerminatedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
4WithdrawnTreatmentDemyelinating Disorders / Disseminated Sclerosis / Myelitis NOS / Neuritis / Optic Neuritis1
4WithdrawnTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)2
Not AvailableActive Not RecruitingNot AvailableRelapsing Remitting Multiple Sclerosis (RRMS)1
Not AvailableCompletedNot AvailableDisseminated Sclerosis9
Not AvailableCompletedNot AvailableDisseminated Sclerosis / Low Bone Density1
Not AvailableCompletedNot AvailableDisseminated Sclerosis / Pregnancy / Prenatal Exposure Delayed Effects1
Not AvailableCompletedNot AvailableRelapsing Multiple Sclerosis (RMS)1
Not AvailableCompletedNot AvailableRelapsing Remitting Multiple Sclerosis (RRMS)5
Not AvailableCompletedTreatmentDisseminated Sclerosis1
Not AvailableRecruitingNot AvailableDisseminated Sclerosis1
Not AvailableRecruitingNot AvailableRelapsing Multiple Sclerosis (RMS)1
Not AvailableWithdrawnNot AvailableDisseminated Sclerosis1

Pharmacoeconomics

Manufacturers
  • Biogen Idec
Packagers
Dosage forms
FormRouteStrength
Injection, powder, lyophilized, for solutionIntramuscular30 ug/mL
Injection, solutionIntramuscular30 ug/.5mL
KitIntramuscular
Powder, for solutionIntramuscular
Powder, for solutionIntramuscular60 mcg
SolutionIntramuscular30 mcg
Injection, solutionSubcutaneous22 ug/.5mL
Injection, solutionSubcutaneous44 ug/.5mL
Kit; liquid; powderIntralesional; Subcutaneous
Kit; liquid; powder, for solutionSubcutaneous
SolutionSubcutaneous132 mcg
SolutionSubcutaneous22 mcg
SolutionSubcutaneous44 mcg
SolutionSubcutaneous66 mcg
SolutionSubcutaneous8.8 mcg
KitSubcutaneous
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)
CA1341604No2010-05-042027-05-04Canada

Properties

State
Liquid
Experimental Properties
PropertyValueSource
hydrophobicity-0.427Not Available
isoelectric point8.93Not 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
Human
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. [PubMed:10049744]
  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. [PubMed:16912135]
  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. [PubMed:12034032]
  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. [PubMed:11747625]
Kind
Protein
Organism
Human
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. [PubMed:16912135]
  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. [PubMed:11747625]

Drug created on June 13, 2005 07:24 / Updated on November 19, 2017 20:34