Primary information |
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ThPP ID | Th1031 |
Therapeutic Peptide/Protein Name | Interferon Alfa-2a, Recombinant |
Sequence | CDLPQTHSLGSRRTLMLLAQMRKISLFSCLKDRHDFGFPQEEFGNQFQKA view full sequnce in fasta |
Functional Classification | Ib |
Molecular Weight | 19241.1 |
Chemical Formula | C860H1353N227O255S9 |
Isoelectric Point | 5.99 |
Hydrophobicity | -0.336 |
Melting Point (℃) | N.A. |
Half Life | IM half-life of interferon alfa-2a is 6 hours to 8 hours |
Description | Its a type I interferon consisting of 165 amino acid residues with lysine in position 23. This protein is produced by recombinant DNA technology and resembles interferon secreted by leukocytes. It is used extensively as an antiviral or antineoplastic agent. An oral form is being developed by Amarillo Biosciences. |
Indication/Disease | For the treatment of chronic hepatitis C, hairy cell leukemia, AIDS-related Kaposi's sarcoma, and chronic myelogenous leukemia. Also for the treatment of oral warts arising from HIV infection. |
Pharmacodynamics | 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 bbetter target for CTL-mediated killing. Interferon alpha also induce the synthesis of several key antiviral mediators, including 2-5 oligoadenylate synthetase (2-5 A synthetase) and protein kinase R. |
Mechanism of Action | It binds directly to the type II interferon gamma receptor IFNGR1, leading to a complex of IFNGR1 and IFNGR2. This activates JAK1 and JAK2 kinases which form a STAT1 docking site. This leads to STAT1 phosphorylation, nuclear translocation and initiation of gene transcription of multiple immune-related genes. |
Toxicity | Interferon alfa-2 may cause serious adverse effects such as anemia; autoimmune diseases, including vasculitis, arthritis, hemolytic anemia, and erythematosus syndrome; cardiotoxicity; hepatotoxicity; hyperthyroidism or hypothyroidism; transient ischemic a |
Metabolism | N.A. |
Absorption | Absorption is high (greater than 80%) when administered intramuscularly or subcutaneously. |
Volume of Distribution | 0.223 to 0.748 L/kg [healthy people] |
Clearance | 2.14 - 3.62 mL/min/kg [healthy] |
Categories | N.A. |
Patents Number | CA2172664 |
Date of Issue | 03/10/00 |
Date of Expiry | 26/03/16 |
Drug Interaction | Interferon increases the effect and toxicity of theophylline |
Target | Interferon alpha/beta receptor 1,Interferon alpha/beta receptor 2 |
Information of corresponding available drug in the market |
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Brand Name | Roferon A |
Company | Hoffmann-La Roche Inc |
Brand Discription | Roferon-A is manufactured by recombinant DNA technology that employs a genetically engineered Escherichia coli bacterium containing DNA that codes for the human protein. Interferon alfa-2a, recombinant is a highly purified protein containing 165 amino aci |
Prescribed for | To treat chronic hepatitis C and hairy cell leukemia in patients 18 years of age or older. In addition, it is indicated for chronic phase, Philadelphia chromosome (Ph) positive chronic myelogenous leukemia (CML) patients who are minimally pretreated (with |
Chemical Name | N.A. |
Formulation | 3 million IU (11.1 mcg/0.5 mL) Roferon-A (interferon alfa-2a, recombinant) per syringe — The solution is colorless and each 0.5 mL contains 3 MIU of Interferon alfa-2a, recombinant, 3.605 mg sodium chloride, 0.1 mg polysorbate 80, 5 mg benzyl alcohol as a |
Physcial Appearnce | Solution |
Route of Administration | Subcutaneous Injection |
Recommended Dosage | Dosage for the treatment of chronic hepatitis C is 3 MIU three times a week (tiw) administered subcutaneously for 12 months (48-52 weeks). As an alternative, patients may be treated with an induction dose of 6 MIU tiw for the first 3 months (12 weeks) followed by 3 MIU tiw for 9 months (36 weeks). |
Contraindication | Hypersensitivity to Roferon-A (interferon alfa-2a, recombinant) or any of its components |
Side Effects | Injection site reactions (pain/swelling/redness), headache, tiredness, diarrhea, upset stomach, loss of appetite, back pain, dizziness, dry mouth, taste changes, nausea, or vomiting may occur. Tooth and gum problems may sometimes occur during treatment. |
Useful Link | http://www.fda.gov/downloads/Drugs/DrugSafety/ucm111340.pdf |
PubMed ID | 3598612 |
3-D Structure | Th1031 (View) or (Download) |