Identification

Name
Interferon beta-1b
Accession Number
DB00068  (BTD00078, BIOD00078)
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Interferons
Description

Human interferon beta (165 residues), cysteine 17 is substituted with serine. Produced in E. coli, no carbohydrates, MW=18.5kD

Protein structure
Db00068
Protein chemical formula
C908H1408N246O253S6
Protein average weight
20011.0 Da
Sequences
>DB00068 sequence
SYNLLGFLQRSSNFQSQKLLWQLNGRLEYCLKDRMNFDIPEEIKQLQQFQKEDAALTIYE
MLQNIFAIFRQDSSSTGWNETIVENLLANVYHQINHLKTVLEEKLEKEDFTRGKLMSSLH
LKRYYGRILHYLKAKEYSHCAWTIVRVEILRNFYFINRLTGYLRN
Download FASTA Format
Synonyms
  • Interferon beta 1b (recombinant)
  • Interferon beta-1b,recombinant
  • Interferon-beta-1b
  • Recombinant interferon beta-1b
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Pharma Ag1995-11-30Not applicableEu
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Pharma Ag1995-11-30Not applicableEu
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Pharma Ag1995-11-30Not applicableEu
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Pharma Ag1995-11-30Not applicableEu
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Pharma Ag1995-11-30Not applicableEu
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Pharma Ag1995-11-30Not applicableEu
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Pharma Ag1995-11-30Not applicableEu
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Pharma Ag1995-11-30Not applicableEu
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Pharma Ag1995-11-30Not applicableEu
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Pharma Ag1995-11-30Not applicableEu
Categories
UNII
TTD90R31WZ
CAS number
145155-23-3

Pharmacology

Indication

Interferon beta-1b is a drug used for the treatment of relapsing/remitting multiple sclerosis. It has been shown to slow the advance of the disease as well as to decrease the frequency of attacks.

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, neopterin and protein kinase R.

Mechanism of action

Interferon beta binds to type I interferon receptors (IFNAR1 and IFNAR2c) which 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 2
agonist
Human
Absorption
Not Available
Volume of distribution
  • 0.25 to 2,88 L/kg
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
  • 9.4 – 28.9 mL/min•kg-1 [patients with diseases other than MS receiving single intravenous doses up to 2.0 mg]
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
Ambroxol acefyllinateThe metabolism of Ambroxol acefyllinate can be decreased when combined with Interferon beta-1b.Experimental
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Interferon beta-1b.Approved
DyphyllineThe metabolism of Dyphylline can be decreased when combined with Interferon beta-1b.Approved
TheophyllineThe metabolism of Theophylline can be decreased when combined with Interferon beta-1b.Approved
ZidovudineThe risk or severity of adverse effects can be increased when Interferon beta-1b 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
  1. Lin L: Betaseron. Dev Biol Stand. 1998;96:97-104. [PubMed:9890522]
  2. Link [Link]
External Links
UniProt
P01574
Genbank
V00534
KEGG Drug
D00746
KEGG Compound
C07901
ChEMBL
CHEMBL1201563
Therapeutic Targets Database
DAP001283
PharmGKB
PA450039
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Interferon_beta-1b
ATC Codes
L03AB08 — Interferon beta-1b
AHFS Codes
  • 92:20.00 — Immunomodulatory Agents
FDA label
Download (1.38 MB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentDisseminated Sclerosis1
1CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Kaposi s Sarcoma (KS)1
1, 2CompletedTreatmentAcute Lung Injury (ALI) / Acute Respiratory Distress Syndrome (ARDS)1
2CompletedNot AvailableDisseminated Sclerosis1
2CompletedTreatmentDisseminated Sclerosis3
2CompletedTreatmentDisseminated Sclerosis / Relapsing-Remitting1
2CompletedTreatmentHeart Diseases / Prophylaxis of cardiomyopathy1
2CompletedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
2Unknown StatusTreatmentDisseminated Sclerosis1
2, 3RecruitingTreatmentDisseminated Sclerosis / Relapsing Remitting Multiple Sclerosis (RRMS)1
2, 3RecruitingTreatmentMiddle East Respiratory Syndrome Coronavirus (MERS-CoV)1
2, 3TerminatedTreatmentDisseminated Sclerosis1
3CompletedTreatmentDisseminated Sclerosis2
3CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections1
3CompletedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)2
3TerminatedTreatmentRelapsing Multiple Sclerosis (RMS)1
3WithdrawnTreatmentDisseminated Sclerosis1
4CompletedNot AvailableDisseminated Sclerosis1
4CompletedTreatmentRelapsing Forms of Multiple Sclerosis1
4CompletedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)4
4TerminatedPreventionRelapsing Remitting Multiple Sclerosis (RRMS)1
4TerminatedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
4Unknown StatusTreatmentDisseminated Sclerosis1
Not AvailableCompletedNot AvailableClinically Isolated System / Disseminated Sclerosis1
Not AvailableCompletedNot AvailableDisseminated Sclerosis15
Not AvailableCompletedNot AvailableDisseminated Sclerosis / Low Bone Density1
Not AvailableCompletedNot AvailableDisseminated Sclerosis / Relapsing Remitting Multiple Sclerosis (RRMS)1
Not AvailableCompletedNot AvailableMultiple Sclerosis, Chronic Progressive1
Not AvailableCompletedNot AvailableRelapsing Remitting Multiple Sclerosis (RRMS)4
Not AvailableCompletedNot AvailableRelapsing Remitting Multiple Sclerosis (RRMS) / Secondary Progressive Multiple Sclerosis (SPMS)2
Not AvailableCompletedTreatmentCytomegalovirus Retinitis / Human Immunodeficiency Virus (HIV) Infections1
Not AvailableRecruitingNot AvailableDisseminated Sclerosis3
Not AvailableWithdrawnNot AvailableRelapsing Remitting Multiple Sclerosis (RRMS)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Dosage forms
FormRouteStrength
Injection, powder, for solutionSubcutaneous0.25 mg/ml
Kit
Kit
Powder, for solutionSubcutaneous0.3 mg
Injection, powder, for solutionSubcutaneous250 μg/ml
Prices
Unit descriptionCostUnit
Betaseron 14 0.3 mg Solution 1 Box Contains Fourteen .3 mg Vials.3315.06USD box
Betaseron 0.3 mg kit227.69USD kit
Extavia 0.3 mg kit196.76USD kit
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1340861No1999-12-282016-12-28Canada
CA1339707No1998-03-102015-03-10Canada

Properties

State
Liquid
Experimental Properties
PropertyValueSource
hydrophobicity-0.447Not Available
isoelectric point9.02Not 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. 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
Human
Pharmacological action
Yes
Actions
Agonist
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. 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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Drug created on June 13, 2005 07:24 / Updated on October 23, 2017 14:13