| Primary information |
|---|
| ThPP ID | Th1057 |
| Therapeutic Peptide/Protein Name | Interferon beta-1b |
| Sequence | MSYNLLGFLQRSSNFQSQKLLWQLNGRLEYCLKDRMNFDIPEEIKQLQQF view full sequnce in fasta |
| Functional Classification | Ib |
| Molecular Weight | 20011 |
| Chemical Formula | C908H1408N246O253S6 |
| Isoelectric Point | 9.02 |
| Hydrophobicity | -0.447 |
| Melting Point (℃) | N.A. |
| Half Life | 10-20 minutes |
| Description | Human interferon beta (165 residues), cysteine 17 is substituted with serine. Produced in E. coli, no carbohydrates, MW=18.5kD. |
| Indication/Disease | Interferon 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. |
| Pharmacodynamics | Interferon 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 Action | Interferon 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. |
| Toxicity | N.A. |
| Metabolism | N.A. |
| Absorption | N.A. |
| Volume of Distribution | 0.25 to 2,88 L/kg |
| Clearance | 9.4 - 28.9 mL/min/kg [patients with diseases other than MS receiving single intravenous doses up to 2.0 mg] |
| Categories | Adjuvants, Immunologic and Immunosuppressive Agents |
| Patents Number | CA1340861 |
| Date of Issue | 29/12/03 |
| Date of Expiry | 29/12/20 |
| Drug Interaction | N.A. |
| Target | N.A. |
| Information of corresponding available drug in the market |
|---|
| Brand Name | Betaseron |
| Company | Bayer |
| Brand Discription | Betaseron (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 for | Betaseron is used to treat relapsing multiple sclerosis (MS). Betaseron will not cure MS, it will only decrease the frequency of relapse symptoms. |
| Chemical Name | N.A. |
| Formulation | Each 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 Appearnce | Sterile, white to off-white powder |
| Route of Administration | Subcutaneous Injection |
| Recommended Dosage | The 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. |
| Contraindication | Betaseron is contraindicated in patients with a history of hypersensitivity to natural or recombinant interferon beta, Albumin (Human), |
| Side Effects | serious 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 Link | https://www.betaseron.com/home http://www.drugs.com/betaseron.html |
| PubMed ID | 26384035, 26039748, 24341722, 23962003, 22873735, 27730845, 26039748, 12224444, 12168506 |
| 3-D Structure | Th1057 (View) or (Download) |