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1376 details
Primary information
ThPP IDTh1057
Therapeutic Peptide/Protein NameInterferon beta-1b
SequenceMSYNLLGFLQRSSNFQSQKLLWQLNGRLEYCLKDRMNFDIPEEIKQLQQF view full sequnce in fasta
Functional ClassificationIb
Molecular Weight20011
Chemical FormulaC908H1408N246O253S6
Isoelectric Point9.02
Hydrophobicity-0.447
Melting Point (℃)N.A.
Half Life10-20 minutes
DescriptionHuman interferon beta (165 residues), cysteine 17 is substituted with serine. Produced in E. coli, no carbohydrates, MW=18.5kD.
Indication/DiseaseInterferon 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.
PharmacodynamicsInterferon 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 ActionInterferon 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.
ToxicityN.A.
MetabolismN.A.
AbsorptionN.A.
Volume of Distribution0.25 to 2,88 L/kg
Clearance9.4 - 28.9 mL/min/kg [patients with diseases other than MS receiving single intravenous doses up to 2.0 mg]
CategoriesAdjuvants, Immunologic and Immunosuppressive Agents
Patents NumberCA1340861
Date of Issue29/12/03
Date of Expiry29/12/20
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameBetaseron
CompanyBayer
Brand DiscriptionBetaseron (interferon beta-lb) is a purified, sterile, lyophilized protein product produced by recombinant DNA techniques. Interferon beta-1b is manufactured by bacterial fermentation of a strain of Escherichia coli that bears a genetically engineered plasmid containing the gene for human interferon betaser17 . The native gene was obtained from human fibroblasts and altered in a way that substitutes serine for the cysteine residue found at position 17. Interferon beta-1b has 165 amino acids and an approximate molecular weight of 18,500 daltons
Prescribed forBetaseron is used to treat relapsing multiple sclerosis (MS). Betaseron will not cure MS, it will only decrease the frequency of relapse symptoms.
Chemical NameN.A.
FormulationEach vial contains 0.3 mg of interferon beta-lb. The unit measurement is derived by comparing the antiviral activity of the product to the World Health Organization (WHO) reference standard of recombinant human interferon beta. Mannitol, USP and Albumin (Human), USP (15 mg each/vial) are added as stabilizers.
Physcial AppearnceSterile, white to off-white powder
Route of AdministrationSubcutaneous Injection
Recommended DosageThe recommended starting dose is 0.0625 mg (0.25 mL) subcutaneously every other day, with dose increases over a six week period to the recommended dose of 0.25 mg (1 mL) every other day.
ContraindicationBetaseron is contraindicated in patients with a history of hypersensitivity to natural or recombinant interferon beta, Albumin (Human),
Side Effectsserious side effects: depressed mood, anxiety, trouble sleeping, restlessness, or thoughts of suicide or hurting yourself; bruising, swelling, oozing, or skin changes where the injection was given; weight changes, pounding heartbeats, feeling too hot or cold; fever, chills, body aches, flu symptoms; or nausea, stomach pain, low fever, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).
Useful Linkhttps://www.betaseron.com/home http://www.drugs.com/betaseron.html
PubMed ID26384035, 26039748, 24341722, 23962003, 22873735, 27730845, 26039748, 12224444, 12168506
3-D StructureTh1057 (View) or (Download)