Peginterferon beta-1a
Identification
- Summary
Peginterferon beta-1a is an interferon beta used to treat relapsing forms of multiple sclerosis.
- Brand Names
- Plegridy
- Generic Name
- Peginterferon beta-1a
- DrugBank Accession Number
- DB09122
- Background
Multiple Sclerosis (MS) is a chronic and inflammatory autoimmune disease of the central nervous system, disrupting communication between the brain and other parts of the body. Most patients diagnosed with this illness experience their initial disease symptoms between the age of 20 to 40, often the most productive years of life. Symptoms may include but are not limited to fatigue, gait changes, bowel or bladder dysfunction, abnormal muscle twitching, vision disturbance, and depressing or mood swings.11 MS is one of the most common causes of neurological disability in young adults and is found to occur more frequently in women than in men.3,12
Peginterferon beta-1a is an interferon therapy used for the management of relapsing forms of MS. It was originally approved by the FDA in 2014 for subcutaneous use, and was approved for intramuscular use in January 2021.13 Currently, it is the only approved pegylated interferon for the management of MS with an proven ability to reduce relapses and delay the progression of disability resulting from MS.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Interferons - Protein Chemical Formula
- Not Available
- Protein Average Weight
- 22500.0 Da (predicted)
- Sequences
>Sequence MSYNLLGFLQRSSNFQCQKLLWQLNGRLEYCLKDRMNFDIPEEIKQLQQFQKEDAALTIY EMLQNIFAIFRQDSSSTGWNETIVENLLANVYHQINHLKTVLEEKLEKEDFTRGKLMSSL HLKRYYGRILHYLKAKEYSHCAWTIVRVEILRNFYFINRLTGYLRN
Download FASTA Format- Synonyms
- PEG IFN-beta-1a
- Peginterferon beta-1a
- Polyethylene glycol-interferon beta-1a
- External IDs
- BIIB-017
- BIIB017
Pharmacology
- Indication
Peginterferon beta-1a is indicated for the treatment of adult patients with relapsing forms of MS, including relapsing-remitting disease, clinically isolated syndrome, and active progressive secondary disease.13
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- Contraindications & Blackbox Warnings
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Peginterferon beta-1a likely reduces MS relapses and the progression of disability and brain lesions associated with MS by reducing inflammation.8,4 Specifically, IFN-beta decreases antigen presentation and T-cell proliferation. In addition, it modifies cytokine and matrix metalloproteinase (MMP) expression while restoring suppressor function.4
- Mechanism of action
The mechanism by which peginterferon beta-1a exerts its effects in patients with multiple sclerosis is unknown13, however, it likely exerts its therapeutic actions by reducing inflammation. Through the binding of IFN-beta to its receptor9, a cascade of transcriptional events occur, decreasing the inflammation that normally results in the progression of MS. Immune cells are the most likely target of therapeutic effects exerted by IFN-beta.4
Target Actions Organism UInterferon alpha/beta receptor 1 activatordownregulatorHumans - Absorption
Peginterferon beta-1a is almost completely absorbed after subcutaneous administration. After 125 microgram subcutaneous doses of peginterferon beta-1a to patient with MS, a Cmax of 280 pg/mL was reached between 1 and 1.5 days4, and the AUC over a 14 day dosing interval was 34.8 ng.hr/mL.13 The AUC ranges from 23.5-29.5 ng ml−1h, according to one pharmacokinetic study of patients with MS. Impairment of renal function may alter the Cmax and AUC of interferon beta-1a.4
- Volume of distribution
The volume of distribution of peginterferon beta-1a is about 481 L.13 One pharmacokinetic study of patients administered interferon beta-1a revealed a volume of distribution in the range of 248-726 L, depending on the week of treatment.4
- Protein binding
Protein binding information for peginterferon beta-1a is not readily available in the literature.
- Metabolism
Peginterferon beta-1a is not extensively metabolized in the liver.13
- Route of elimination
Peginterferon beta-1a is mainly cleared through the kidneys.4,13
- Half-life
The mean half life of peginterferon beta-1a is approximately 78 h in patients with MS15, however, the half-life is highly variable and depends on duration of treatment and other factors.4
- Clearance
The average steady state clearance of peginterferon beta-1a is about 4.1 L/h.13 One pharmacokinetic study revealed a clearance within the range of 3.68-7.89 L/h, depending on the week of treatment.4
- Adverse Effects
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LD50 information for peginterferon beta-1a is not readily available in the literature. In clinical trials, no cases of overdoses occurred with the administration of interferon beta-1a at a dose of 75 μg administered subcutaneously 3 times a week.13 In a case report, a 38-year-old patient attempted suicide with about 6 or 7 pre-filled syringes containing 44 mug (12 MIU) of subcutaneous interferon beta-1a; symptoms were limited to malaise and skin erythema, which resolved within 24 hours with no intervention. Laboratory test results were unremarkable.10 In the case of an overdose with interferon-beta 1a, prescribing information suggests to contact the local poison control centre.15
- 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 Integrate drug-drug
interactions in your softwareAbatacept 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 risk or severity of bleeding can be increased when Acenocoumarol is 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. 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. Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Peginterferon beta-1a. Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Peginterferon beta-1a. Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Peginterferon beta-1a. Allopurinol The risk or severity of adverse effects can be increased when Allopurinol is combined with Peginterferon beta-1a. 
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- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- International/Other Brands
- Plegridy (Biogen)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Plegridy Liquid 63 mcg / 0.5 mL Subcutaneous Biogen Not applicable Not applicable Canada 
Plegridy Injection, solution 125 mcg Subcutaneous Biogen Netherlands B.V. 2016-09-08 Not applicable EU 
Plegridy Injection, solution 125 mcg Intramuscular Biogen Netherlands B.V. 2020-12-28 Not applicable EU Plegridy Injection, solution 125 mcg Subcutaneous Biogen Netherlands B.V. 2016-09-08 Not applicable EU Plegridy Injection, solution 125 ug/0.5mL Subcutaneous Biogen Inc. 2014-08-15 Not applicable US 
Plegridy Liquid 125 mcg / 0.5 mL Subcutaneous Biogen 2015-09-29 Not applicable Canada Plegridy Injection, solution 125 mcg Intramuscular Biogen Netherlands B.V. 2020-12-28 Not applicable EU Plegridy Injection, solution 125 ug/0.5mL Intramuscular Biogen Inc. 2021-01-29 Not applicable US Plegridy Injection, solution 125 mcg Subcutaneous Biogen Netherlands B.V. 2016-09-08 Not applicable EU Plegridy Liquid 94 mcg / 0.5 mL Subcutaneous Biogen Not applicable Not applicable Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Plegridy Peginterferon beta-1a (94 ug/0.5mL) + Peginterferon beta-1a (63 ug/0.5mL) Kit; Liquid Subcutaneous Biogen Inc. 2014-08-15 Not applicable US Plegridy Peginterferon beta-1a (63 mcg / 0.5 mL) + Peginterferon beta-1a (94 mcg / 0.5 mL) 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) Kit; Liquid Subcutaneous Biogen Inc. 2014-08-15 Not applicable US Plegridy Peginterferon beta-1a (63 mcg / 0.5 mL) + Peginterferon beta-1a (94 mcg / 0.5 mL) Kit; Liquid Subcutaneous Biogen 2015-09-25 Not applicable Canada PLEGRİDY 63 MCG/0.5 ML+94 MCG/0.5 ML SC ENJEKSİYONLUK ÇÖZELTİ İÇEREN KULLANIMA HAZIR KALEM TEDAVİYE BAŞLAMA PAKETİ , 1 ADET 63 MGC/0.5 ML+1 ADET 94 MCG/0.5 ML Peginterferon beta-1a (63 mcg/0.5mL) + Peginterferon beta-1a (94 mcg/0.5mL) Injection; Kit Subcutaneous GEN İLAÇ VE SAĞLIK ÜRÜNLERİ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey 
PLEGRİDY 63 MCG/0.5 ML+94 MCG/0.5 ML SC ENJEKSİYONLUK ÇÖZELTİ İÇEREN KULLANIMA HAZIR KALEM TEDAVİYE BAŞLAMA PAKETİ , 1 ADET 63 MGC/0.5 ML+1 ADET 94 MCG/0.5 ML Peginterferon beta-1a (63 mcg/0.5mL) + Peginterferon beta-1a (94 mcg/0.5mL) Injection; Kit Subcutaneous GEN İLAÇ VE SAĞLIK ÜRÜNLERİ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey 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
- Amino Acids, Peptides, and Proteins
- Antineoplastic and Immunomodulating Agents
- Biological Factors
- Compounds used in a research, industrial, or household setting
- Immunosuppressive Agents
- Intercellular Signaling Peptides and Proteins
- Interferon Type I
- Interferon-beta
- 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
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- I8309403R0
- CAS number
- 1211327-92-2
References
- Synthesis Reference
Alessandra Del RioJoel Richard ; PEG-interferon-beta formulations. United States Patent US9138403B2. 2015-Sep-22
- 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. [Article]
- 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. [Article]
- Ghasemi N, Razavi S, Nikzad E: Multiple Sclerosis: Pathogenesis, Symptoms, Diagnoses and Cell-Based Therapy. Cell J. 2017 Apr-Jun;19(1):1-10. Epub 2016 Dec 21. [Article]
- Hu X, Cui Y, White J, Zhu Y, Deykin A, Nestorov I, Hung S: Pharmacokinetics and pharmacodynamics of peginterferon beta-1a in patients with relapsing-remitting multiple sclerosis in the randomized ADVANCE study. Br J Clin Pharmacol. 2015 Mar;79(3):514-22. doi: 10.1111/bcp.12521. [Article]
- Hoy SM: Peginterferon beta-1a: a review of its use in patients with relapsing-remitting multiple sclerosis. CNS Drugs. 2015 Feb;29(2):171-9. doi: 10.1007/s40263-015-0227-1. [Article]
- Madsen C: The innovative development in interferon beta treatments of relapsing-remitting multiple sclerosis. Brain Behav. 2017 May 8;7(6):e00696. doi: 10.1002/brb3.696. eCollection 2017 Jun. [Article]
- Pestka S, Langer JA, Zoon KC, Samuel CE: Interferons and their actions. Annu Rev Biochem. 1987;56:727-77. doi: 10.1146/annurev.bi.56.070187.003455. [Article]
- Markowitz CE: Interferon-beta: mechanism of action and dosing issues. Neurology. 2007 Jun 12;68(24 Suppl 4):S8-11. doi: 10.1212/01.wnl.0000277703.74115.d2. [Article]
- Mastrangeli R, Iozzino L, Lanzoni L, Angiuoni G, Ferrao C, Izzo A, Fiumi S, Camerini F, Mascia M, Palinsky W, Bierau H: Biological Functions of Interferon beta-1a Are Enhanced By Deamidation. J Interferon Cytokine Res. 2016 Sep;36(9):534-41. doi: 10.1089/jir.2016.0025. Epub 2016 Jun 27. [Article]
- Falcone NP, Nappo A, Neuteboom B: Interferon beta-1a overdose in a multiple sclerosis patient. Ann Pharmacother. 2005 Nov;39(11):1950-2. doi: 10.1345/aph.1E416. Epub 2005 Oct 4. [Article]
- MS Society Document, Canada [Link]
- FDA approves new oral drug to treat multiple sclerosis [Link]
- FDA Approved Drug Products: PLEGRIDY (peginterferon beta-1a) injection, for subcutaneous or intramuscular use [Link]
- EMD Serono MSDS: Interferon beta 1a [Link]
- Product monograph: Avonex (interferon beta-1a) injection [Link]
- EMA Assessment Report: Plegridy (peginterferon beta-1a) for injection [Link]
- External Links
- KEGG Drug
- D10483
- PubChem Substance
- 347910413
- 1546168
- RxList
- RxList Drug Page
- Wikipedia
- Peginterferon_beta-1a
- 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 Multiple 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 Coronavirus Disease 2019 (COVID‑19) / SARS-Associated Coronavirus 1 3 Recruiting Treatment Relapsing Remitting Multiple Sclerosis (RRMS) 2 3 Withdrawn Treatment Relapsing Remitting Multiple Sclerosis (RRMS) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Intramuscular 30 MCG/0.5ML Solution Subcutaneous Injection, solution Intramuscular 125 mcg Injection, solution Intramuscular 125 ug/0.5mL Injection, solution Intramuscular; Parenteral 125 MCG Injection, solution Parenteral; Subcutaneous 63 MCG Injection, solution Subcutaneous 125 MCG Injection, solution Subcutaneous 125 ug/0.5mL Kit; liquid Subcutaneous Liquid Subcutaneous 125 mcg / 0.5 mL Liquid Subcutaneous 63 mcg / 0.5 mL Liquid Subcutaneous 94 mcg / 0.5 mL Injection Subcutaneous Injection; kit Subcutaneous Solution Subcutaneous 125 mcg Solution Subcutaneous 63 mcg Solution Subcutaneous 94 mcg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
Property Value Source boiling point (°C) 100 https://imgcdn.mckesson.com/CumulusWeb/Click_and_learn/SDS_9BIOGN_AVONEX_KIT_30MCG_5ML_4BX.pdf isoelectric point 9.02 https://collab.its.virginia.edu/access/content/group/f85bed6c-45d2-4b18-b868-6a2353586804/2/Ch32_Lee_S_Human_Interferon-Beta_--Homo_sapiens-_-/Ch32_Lee_S_Human_Interferon-Beta_--Homo_sapiens_Human_Interferon_beta.html
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- ActivatorDownregulator
- Curator comments
- Interferon 1 receptor is the target of beta interferon 1-a, however, the mechanism of action of this drug is not fully understood; some sources suggest down regulation of interferon 1 receptors, while others suggest activation of interferon 1 receptors.
- 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
- Hu X, Cui Y, White J, Zhu Y, Deykin A, Nestorov I, Hung S: Pharmacokinetics and pharmacodynamics of peginterferon beta-1a in patients with relapsing-remitting multiple sclerosis in the randomized ADVANCE study. Br J Clin Pharmacol. 2015 Mar;79(3):514-22. doi: 10.1111/bcp.12521. [Article]
- Pestka S, Langer JA, Zoon KC, Samuel CE: Interferons and their actions. Annu Rev Biochem. 1987;56:727-77. doi: 10.1146/annurev.bi.56.070187.003455. [Article]
- Mastrangeli R, Iozzino L, Lanzoni L, Angiuoni G, Ferrao C, Izzo A, Fiumi S, Camerini F, Mascia M, Palinsky W, Bierau H: Biological Functions of Interferon beta-1a Are Enhanced By Deamidation. J Interferon Cytokine Res. 2016 Sep;36(9):534-41. doi: 10.1089/jir.2016.0025. Epub 2016 Jun 27. [Article]
- Hu X, Seddighzadeh A, Stecher S, Zhu Y, Goyal J, Matson M, Marbury T, Smith W, Nestorov I, Hung S: Pharmacokinetics, pharmacodynamics, and safety of peginterferon beta-1a in subjects with normal or impaired renal function. J Clin Pharmacol. 2015 Feb;55(2):179-88. doi: 10.1002/jcph.390. Epub 2014 Sep 23. [Article]
- Liberati AM, Fizzotti M, Proietti MG, Di Marzio R, Schippa M, Biscottini B, Senatore M, Berruto P, Canali S, Peretti G, et al.: Biochemical host response to interferon-beta. J Interferon Res. 1988 Dec;8(6):765-77. doi: 10.1089/jir.1988.8.765. [Article]
- EMA Assessment Report: Plegridy (peginterferon beta-1a) for injection [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Downregulator
- Curator comments
- A study in rats demonstrated that interferon beta-1a down regulated CYP1A2 in rats. Clinical relevance is unknown.
- 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. [Article]
Drug created on September 23, 2015 15:59 / Updated on September 19, 2021 19:53