Peginterferon beta-1a
Identification
- Name
- Peginterferon beta-1a
- 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
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- 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
Learn about our commercial Adverse Effects data.
Learn More- 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 DataAbatacept 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 DescriptionExtended DescriptionAvailable for Purchase
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - SeveritySeverityAvailable for Purchase
A severity rating for each drug interaction, from minor to major.
Learn more - Evidence LevelEvidence LevelAvailable for Purchase
A rating for the strength of the evidence supporting each drug interaction.
Learn more - ActionActionAvailable for Purchase
An effect category for each drug interaction. Know how this interaction affects the subject drug.
Learn more
- Food Interactions
- Not Available
Products
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataPlegridy Injection, solution Intramuscular Biogen Netherlands B.V. 2014-07-17 Not applicable EU Plegridy Injection, solution 125 ug/0.5mL Subcutaneous Biogen Inc. 2014-08-15 Not applicable US Plegridy Injection, solution 125 mcg Subcutaneous Biogen Netherlands B.V. 2014-07-16 Not applicable EU Plegridy Liquid 94 mcg Subcutaneous Biogen Not applicable Not applicable Canada Plegridy Injection, solution Intramuscular Biogen Netherlands B.V. 2014-07-17 Not applicable EU Plegridy Injection, solution 125 mcg Subcutaneous Biogen Netherlands B.V. 2014-07-16 Not applicable EU Plegridy Liquid 63 mcg Subcutaneous Biogen Not applicable Not applicable Canada Plegridy Injection, solution 125 mcg Subcutaneous Biogen Netherlands B.V. 2014-07-16 Not applicable EU Plegridy Injection, solution 125 mcg Subcutaneous Biogen Netherlands B.V. 2014-07-16 Not applicable EU Plegridy Liquid 125 mcg Subcutaneous Biogen 2015-09-29 Not applicable Canada Additional Data Available- Application NumberApplication NumberAvailable for Purchase
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct CodeAvailable for Purchase
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Plegridy Peginterferon beta-1a (63 mcg) + Peginterferon beta-1a (94 mcg) Kit; Liquid Subcutaneous Biogen 2015-09-25 Not applicable Canada Plegridy Peginterferon beta-1a (94 ug/0.5mL) + Peginterferon beta-1a (63 ug/0.5mL) Subcutaneous Biogen Inc. 2014-08-15 Not applicable US Plegridy Peginterferon beta-1a (94 ug/0.5mL) + Peginterferon beta-1a (63 ug/0.5mL) Subcutaneous Biogen Inc. 2014-08-15 Not applicable US Plegridy Peginterferon beta-1a (63 mcg) + Peginterferon beta-1a (94 mcg) Kit; Liquid Subcutaneous Biogen 2015-09-25 Not applicable Canada Plegridy Pen Peginterferon beta-1a (94 ug/0.5mL) + Peginterferon beta-1a (63 ug/0.5mL) Subcutaneous Biogen Inc. 2014-08-15 Not applicable US Plegridy Pen Peginterferon beta-1a (94 ug/0.5mL) + Peginterferon beta-1a (63 ug/0.5mL) Subcutaneous Biogen Inc. 2014-08-15 Not applicable US
Categories
- ATC Codes
- L03AB13 — Peginterferon beta-1a
- Drug Categories
- Adjuvants, Immunologic
- Alcohols
- Amino Acids, Peptides, and Proteins
- Antineoplastic and Immunomodulating Agents
- Biological Factors
- Compounds used in a research, industrial, or household setting
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
- Cytochrome P-450 Enzyme Inhibitors
- Cytokines
- Ethylene Glycols
- Glycols
- Immunosuppressive Agents
- Intercellular Signaling Peptides and Proteins
- Interferon Type I
- Interferons
- Macromolecular Substances
- Myelosuppressive Agents
- Pegylated agents
- Peptides
- Polymers
- Proteins
- 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
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
- 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
- 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]
Drug created on September 23, 2015 09:59 / Updated on January 23, 2021 21:03