Peginterferon beta-1a

Identification

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Name
Peginterferon beta-1a
Accession Number
DB09122
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Interferons
Description

Peginterferon beta-1a is an interferon beta-1a to which a single, linear 20,000 dalton (Da) methoxy poly(ethyleneglycol)-O-2-methylpropionaldehyde (PEG) molecule is covalently attached to the alpha amino group of the N-terminal amino acid residue. The amino acid sequence of the recombinant interferon beta-1a is identical to that of the human interferon beta counterpart. Although it's mechanism of action is unknown, peginterferon beta-1a is indicated for use in relapsing forms of Multiple Sclerosis (MS).

Interferon beta was the first drug to alter the course of MS, however multiple side effects and the need for weekly subcutaneous injection make it difficult to use. Interferon beta was subsequently PEGylated (covalently attached to polyethylene glycol) to extend its duration of action to every 14 days. It is currently available as peginterferon beta-1a as the FDA-approved product Plegridy.

Protein chemical formula
Not Available
Protein average weight
44000.0 Da
Sequences
>Sequence
MSYNLLGFLQRSSNFQCQKLLWQLNGRLEYCLKDRMNFDIPEEIKQLQQFQKEDAALTIY
EMLQNIFAIFRQDSSSTGWNETIVENLLANVYHQINHLKTVLEEKLEKEDFTRGKLMSSL
HLKRYYGRILHYLKAKEYSHCAWTIVRVEILRNFYFINRLTGYLRN
Download FASTA Format
Synonyms
Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
PlegridyInjection, solution125 ug/0.5mLSubcutaneousBiogen Inc.2014-08-15Not applicableUs
PlegridyInjection, solution125 mcgSubcutaneousBiogen Netherlands B.V.2014-07-16Not applicableEu
PlegridyLiquid63 mcgSubcutaneousBiogenNot applicableNot applicableCanada
PlegridyLiquid125 mcgSubcutaneousBiogen2015-09-29Not applicableCanada
PlegridyInjection, solution125 mcgSubcutaneousBiogen Netherlands B.V.2014-07-16Not applicableEu
PlegridyInjection, solution125 mcgSubcutaneousBiogen Netherlands B.V.2014-07-16Not applicableEu
PlegridyLiquid94 mcgSubcutaneousBiogenNot applicableNot applicableCanada
PlegridyInjection, solution125 mcgSubcutaneousBiogen Netherlands B.V.2014-07-16Not applicableEu
Plegridy PenInjection, solution125 ug/0.5mLSubcutaneousBiogen Inc.2014-08-15Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
PlegridyPeginterferon beta-1a (94 ug/0.5mL) + Peginterferon beta-1a (63 ug/0.5mL)KitBiogen Inc.2014-08-15Not applicableUs
PlegridyPeginterferon beta-1a (94 ug/0.5mL) + Peginterferon beta-1a (63 ug/0.5mL)KitBiogen Inc.2014-08-15Not applicableUs
PlegridyPeginterferon beta-1a (63 mcg) + Peginterferon beta-1a (94 mcg)Kit; LiquidSubcutaneousBiogen2015-09-25Not applicableCanada
PlegridyPeginterferon beta-1a (63 mcg) + Peginterferon beta-1a (94 mcg)Kit; LiquidSubcutaneousBiogen2015-09-25Not applicableCanada
Plegridy PenPeginterferon beta-1a (94 ug/0.5mL) + Peginterferon beta-1a (63 ug/0.5mL)KitBiogen Inc.2014-08-15Not applicableUs
Plegridy PenPeginterferon beta-1a (94 ug/0.5mL) + Peginterferon beta-1a (63 ug/0.5mL)KitBiogen Inc.2014-08-15Not applicableUs
Categories
UNII
I8309403R0
CAS number
1211327-92-2

Pharmacology

Indication

For the treatment of patients with relapsing forms of multiple sclerosis.

Associated Conditions
Pharmacodynamics
Not Available
Mechanism of action

The mechanism by which peginterferon beta-1a exerts its effects in patients with multiple sclerosis is unknown.

Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

After 125 microgram subcutaneous doses of peginterferon beta-1a in multiple sclerosis patients, the maximum concentration occurred between 1 and 1.5 days, the mean Cmax was 280 pg/mL, and the AUC over the 14 day dosing interval was 34.8 ng.hr/mL.

Volume of distribution

481 L

Protein binding
Not Available
Metabolism

Peginterferon beta-1a is not extensively metabolized in the liver.

Route of elimination

The major pathway of elimination is renal.

Half life

78 hr

Clearance

4.1 L/hr

Toxicity

The most commonly reported adverse reactions were injection site erythema, influenza-like illness, pyrexia, headache, myalgia, chills, injection site pain, asthenia, injection site pruritus, and arthralgia.

Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe risk or severity of bleeding can be increased when (R)-warfarin is combined with Peginterferon beta-1a.
(S)-WarfarinThe risk or severity of bleeding can be increased when (S)-Warfarin is combined with Peginterferon beta-1a.
2-MethoxyethanolThe risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Peginterferon beta-1a.
3-isobutyl-1-methyl-7H-xanthineThe metabolism of 3-isobutyl-1-methyl-7H-xanthine can be decreased when combined with Peginterferon beta-1a.
4-hydroxycoumarinThe risk or severity of bleeding can be increased when 4-hydroxycoumarin is combined with Peginterferon beta-1a.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Peginterferon beta-1a.
7-DeazaguanineThe metabolism of 7-Deazaguanine can be decreased when combined with Peginterferon beta-1a.
7,9-DimethylguanineThe metabolism of 7,9-Dimethylguanine can be decreased when combined with Peginterferon beta-1a.
8-azaguanineThe metabolism of 8-azaguanine can be decreased when combined with Peginterferon beta-1a.
8-chlorotheophyllineThe metabolism of 8-chlorotheophylline can be decreased when combined with Peginterferon beta-1a.
Additional Data Available
  • Extended Description
    Extended Description

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  • Severity
    Severity

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  • Evidence Level
    Evidence Level

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  • Action
    Action

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Food Interactions
Not Available

References

General References
  1. Newsome SD, Guo S, Altincatal A, Proskorovsky I, Kinter E, Phillips G, You X, Sabatella G: Impact of peginterferon beta-1a and disease factors on quality of life in multiple sclerosis. Mult Scler Relat Disord. 2015 Jul;4(4):350-7. doi: 10.1016/j.msard.2015.06.004. Epub 2015 Jun 14. [PubMed:26195056]
  2. Khan UT, Tanasescu R, Constantinescu CS: PEGylated IFNbeta-1a in the treatment of multiple sclerosis. Expert Opin Biol Ther. 2015 Jul;15(7):1077-84. doi: 10.1517/14712598.2015.1053206. Epub 2015 Jun 3. [PubMed:26036950]
External Links
KEGG Drug
D10483
PubChem Substance
347910413
ATC Codes
L03AB13 — Peginterferon beta-1a
AHFS Codes
  • 08:18.20 — Interferons
FDA label
Download (12.6 MB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedBasic ScienceHealthy Volunteers / Impaired Renal Function1
1CompletedTreatmentDisseminated Sclerosis1
1CompletedTreatmentHealthy Volunteers1
3CompletedTreatmentRelapsing Multiple Sclerosis (RMS)2
3CompletedTreatmentRelapsing Multiple Sclerosis (RMS) / Relapsing Remitting Multiple Sclerosis (RRMS)1
3Not Yet RecruitingTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
3RecruitingTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
4CompletedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
4RecruitingPreventionDisseminated Sclerosis1
4RecruitingTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)2
4WithdrawnSupportive CareRelapsing Remitting Multiple Sclerosis (RRMS)1
4WithdrawnTreatmentRelapsing Multiple Sclerosis (RMS)1
Not AvailableActive Not RecruitingNot AvailableRelapsing Forms of Multiple Sclerosis1
Not AvailableRecruitingNot AvailableDisseminated Sclerosis / Exposure During Pregnancy1
Not AvailableRecruitingNot AvailableRelapsing Remitting Multiple Sclerosis (RRMS)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Injection, solutionSubcutaneous125 ug/0.5mL
Injection, solutionSubcutaneous125 mcg
Kit
Kit; liquidSubcutaneous
LiquidSubcutaneous125 mcg
LiquidSubcutaneous63 mcg
LiquidSubcutaneous94 mcg
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not 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

Drug created on September 23, 2015 09:59 / Updated on June 18, 2019 01:48