Interferon beta-1b

Identification

Summary

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

Brand Names
Betaferon, Betaseron, Extavia
Generic Name
Interferon beta-1b
DrugBank Accession Number
DB00068
Background

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

Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Interferons
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
  • Interferon beta-1b,recombinant
  • Interferon-beta-1b
  • Recombinant interferon beta-1b

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.

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, 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
Humans
AInterferon alpha/beta receptor 2
agonist
Humans
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]
Adverse Effects
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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
AbataceptThe risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Abatacept.
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Interferon beta-1b.
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Interferon beta-1b.
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Interferon beta-1b.
Acetylsalicylic acidThe risk or severity of bleeding can be increased when Acetylsalicylic acid is combined with Interferon beta-1b.
AcyclovirThe metabolism of Acyclovir can be decreased when combined with Interferon beta-1b.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Interferon beta-1b.
Adenovirus type 7 vaccine liveThe risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Interferon beta-1b.
AgomelatineThe metabolism of Agomelatine can be decreased when combined with Interferon beta-1b.
AlbendazoleThe metabolism of Albendazole can be decreased when combined with Interferon beta-1b.
Interactions
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Food Interactions
  • Avoid excessive or chronic alcohol consumption. Alcohol and Interferon beta-1 can both cause hepatoxicity, therefore if they are used together they may have additive hepatoxic effects.

Products

Products
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Ag2016-09-08Not applicableEU flag
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Ag2016-09-08Not applicableEU flag
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Ag2016-09-08Not applicableEU flag
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Ag2016-09-08Not applicableEU flag
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Ag2016-09-08Not applicableEU flag
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Ag2016-09-08Not applicableEU flag
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Ag2016-09-08Not applicableEU flag
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Ag2016-09-08Not applicableEU flag
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Ag2016-09-08Not applicableEU flag
BetaferonInjection, powder, for solution0.25 mg/mlSubcutaneousBayer Ag2016-09-08Not applicableEU flag

Categories

ATC Codes
L03AB08 — Interferon beta-1b
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
  • Humans and other mammals

Chemical Identifiers

UNII
TTD90R31WZ
CAS number
145155-23-3

References

Synthesis Reference

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

US4289689
General References
  1. Lin L: Betaseron. Dev Biol Stand. 1998;96:97-104. [Article]
  2. Link [Link]
UniProt
P01574
Genbank
V00534
KEGG Drug
D00746
KEGG Compound
C07901
PubChem Substance
46504458
RxNav
72258
ChEMBL
CHEMBL1201563
Therapeutic Targets Database
DAP001283
PharmGKB
PA450039
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Interferon_beta-1b
FDA label
Download (1.38 MB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentMultiple Sclerosis, Relapsing Forms of Multiple Sclerosis1
4CompletedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)5
4RecruitingTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
4TerminatedPreventionRelapsing Remitting Multiple Sclerosis (RRMS)1
4TerminatedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)2
4Unknown StatusTreatmentDisseminated Sclerosis1
4WithdrawnTreatmentRelapsing Multiple Sclerosis (RMS)1
3CompletedTreatmentDisseminated Sclerosis2
3CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections1
3CompletedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Bayer Healthcare
  • Berlex Labs
  • Chiron Corp.
  • InterMune Inc.
  • Novartis AG
Dosage Forms
FormRouteStrength
Injection, powder, for solutionSubcutaneous
Injection, powder, for solutionSubcutaneous0.25 mg/ml
SolutionParenteral; Subcutaneous
Injection, powder, lyophilized, for solutionSubcutaneous0.25 mg
KitSubcutaneous0.25 mg/1mL
Powder, for solutionSubcutaneous0.3 mg / vial
InjectionSubcutaneous0.25 mg/1.0mL
Injection, powder, for solutionSubcutaneous250 μg/ml
PowderSubcutaneous
PowderSubcutaneous8 MIU/1vial
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)Region
CA1340861No1999-12-282016-12-28Canada flag
CA1339707No1998-03-102015-03-10Canada flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource
hydrophobicity-0.447Not Available
isoelectric point9.02Not Available

Targets

Drugtargets
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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. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Kind
Protein
Organism
Humans
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. [Article]
  2. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [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 July 29, 2021 06:27