Peginterferon beta-1a

Identification

Accession Number

DB09122

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.

Type

Biotech

Groups

Approved

Biologic Classification

Protein Based Therapies
Interferons

Protein Chemical Formula

Not Available

Protein Average Weight

44000.0 Da

Sequences

>Sequence
MSYNLLGFLQRSSNFQCQKLLWQLNGRLEYCLKDRMNFDIPEEIKQLQQFQKEDAALTIY
EMLQNIFAIFRQDSSSTGWNETIVENLLANVYHQINHLKTVLEEKLEKEDFTRGKLMSSL
HLKRYYGRILHYLKAKEYSHCAWTIVRVEILRNFYFINRLTGYLRN

Download FASTA Format

Synonyms

Not Available

Pharmacology

Indication

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

Associated Conditions

Disseminated Sclerosis

Contraindications & Blackbox Warnings

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Pharmacodynamics

Not Available

Mechanism of action

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

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

Adverse Effects

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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

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.

Drug	Interaction
Unlock Additional Data
Abatacept	The risk or severity of adverse effects can be increased when Abatacept is combined with Peginterferon beta-1a.
Abciximab	The risk or severity of bleeding can be increased when Abciximab is combined with Peginterferon beta-1a.
Acenocoumarol	The metabolism of Acenocoumarol can be decreased when combined with Peginterferon beta-1a.
Acetaminophen	The metabolism of Acetaminophen can be decreased when combined with Peginterferon beta-1a.
Acetylsalicylic acid	The risk or severity of bleeding can be increased when Acetylsalicylic acid is combined with Peginterferon beta-1a.
Acyclovir	The metabolism of Acyclovir can be decreased when combined with Peginterferon beta-1a.
Adalimumab	The risk or severity of adverse effects can be increased when Adalimumab is combined with Peginterferon beta-1a.
Adenovirus type 7 vaccine live	The risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Peginterferon beta-1a.
Agomelatine	The metabolism of Agomelatine can be decreased when combined with Peginterferon beta-1a.
Albendazole	The metabolism of Albendazole can be decreased when combined with Peginterferon beta-1a.

Additional Data Available

Extended Description

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Extended description of the mechanism of action and particular properties of each drug interaction.

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Severity

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A severity rating for each drug interaction, from minor to major.

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Evidence Level

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A rating for the strength of the evidence supporting each drug interaction.

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Action

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An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions

Not Available

Products

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Unlock Additional Data
Plegridy	Liquid	125 mcg	Subcutaneous	Biogen	2015-09-29	Not applicable
Plegridy	Injection, solution		Intramuscular	Biogen Netherlands B.V.	2014-07-17	Not applicable
Plegridy	Injection, solution	125 mcg	Subcutaneous	Biogen Netherlands B.V.	2014-07-16	Not applicable
Plegridy	Injection, solution	125 mcg	Subcutaneous	Biogen Netherlands B.V.	2014-07-16	Not applicable
Plegridy	Liquid	94 mcg	Subcutaneous	Biogen	Not applicable	Not applicable
Plegridy	Injection, solution	125 mcg	Subcutaneous	Biogen Netherlands B.V.	2014-07-16	Not applicable
Plegridy	Liquid	63 mcg	Subcutaneous	Biogen	Not applicable	Not applicable
Plegridy	Injection, solution		Intramuscular	Biogen Netherlands B.V.	2014-07-17	Not applicable
Plegridy	Injection, solution	125 ug/0.5mL	Subcutaneous	Biogen Inc.	2014-08-15	Not applicable
Plegridy	Injection, solution	125 mcg	Subcutaneous	Biogen Netherlands B.V.	2014-07-16	Not applicable

Additional Data Available

Application Number

Available for Purchase

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

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Product Code

Available for Purchase

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

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Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
Plegridy	Peginterferon beta-1a (94 ug/0.5mL) + Peginterferon beta-1a (63 ug/0.5mL)		Subcutaneous	Biogen Inc.	2014-08-15	Not applicable
Plegridy	Peginterferon beta-1a (63 mcg) + Peginterferon beta-1a (94 mcg)	Kit; Liquid	Subcutaneous	Biogen	2015-09-25	Not applicable
Plegridy	Peginterferon beta-1a (63 mcg) + Peginterferon beta-1a (94 mcg)	Kit; Liquid	Subcutaneous	Biogen	2015-09-25	Not applicable
Plegridy	Peginterferon beta-1a (94 ug/0.5mL) + Peginterferon beta-1a (63 ug/0.5mL)		Subcutaneous	Biogen Inc.	2014-08-15	Not applicable
Plegridy Pen	Peginterferon beta-1a (94 ug/0.5mL) + Peginterferon beta-1a (63 ug/0.5mL)		Subcutaneous	Biogen Inc.	2014-08-15	Not applicable
Plegridy Pen	Peginterferon beta-1a (94 ug/0.5mL) + Peginterferon beta-1a (63 ug/0.5mL)		Subcutaneous	Biogen Inc.	2014-08-15	Not applicable

Chemical Identifiers

UNII: I8309403R0
CAS number: 1211327-92-2

References

General References

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]
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
RxNav: 1546168
RxList: RxList Drug Page

AHFS Codes

08:18.20 — Interferons

FDA label

Download (12.6 MB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Completed	Treatment	Relapsing Remitting Multiple Sclerosis (RRMS)	2
4	Recruiting	Prevention	Disseminated Sclerosis	1
4	Recruiting	Treatment	Relapsing Remitting Multiple Sclerosis (RRMS)	1
4	Withdrawn	Supportive Care	Relapsing Remitting Multiple Sclerosis (RRMS)	1
4	Withdrawn	Treatment	Relapsing Multiple Sclerosis (RMS)	1
3	Completed	Treatment	Relapsing Multiple Sclerosis (RMS)	3
3	Recruiting	Treatment	Coronavirus (SARS-CoV) / Coronavirus Disease 2019 (COVID‑19) / INTERFERON	1
3	Recruiting	Treatment	Relapsing Remitting Multiple Sclerosis (RRMS)	2
2	Not Yet Recruiting	Treatment	Relapsing Multiple Sclerosis (RMS)	1
1	Completed	Basic Science	Healthy Volunteers / Impaired kidney function	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Injection	Intramuscular	30 MCG/0.5ML
Solution	Subcutaneous	88 mcg
Injection, solution	Intramuscular
Injection, solution	Parenteral; Subcutaneous	63 MCG
Injection, solution	Subcutaneous	125 ug/0.5mL
Injection, solution	Subcutaneous	125 mcg
Kit; liquid	Subcutaneous
Liquid	Subcutaneous	125 mcg
Liquid	Subcutaneous	63 mcg
Liquid	Subcutaneous	94 mcg
Injection	Subcutaneous	125 mcg/0.5ml
Injection; kit	Subcutaneous	63 mcg/0.5mL
Solution	Subcutaneous	125 mcg
Solution	Subcutaneous	63 mcg
Solution	Subcutaneous	94 mcg

Prices

Not Available

Patents

Not Available

Properties

State: Solid
Experimental Properties: Not Available

Enzymes

Details1. Cytochrome P450 1A2

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

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. [PubMed:9064483]