==== Reference: Usmani SS, Bedi G, Samuel JS, Singh S, Kalra S, Kumar P, et al. (2017) THPdb: Database of FDA-approved peptide and protein therapeutics. PLoS ONE 12(7) e0181748.====

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1379 details
Primary information
ThPP IDTh1058
Therapeutic Peptide/Protein NameInterferon alfacon-1
SequenceCDLPQTHSLGSRRTLMLLAQMRRISLFSCLKDRHDFGFPQEEFGNQFQKA view full sequnce in fasta
Functional ClassificationIb
Molecular Weight19271
Chemical FormulaC860H1353N229O255S9
Isoelectric Point5.99
Hydrophobicity0.339
Melting Point (℃)61
Half LifeThe elimination half-life following both intramuscular and subcutaneous injections was approximately
DescriptionRecombinant type-I Interferon alpha 2b (human leukocyte clone hif-sn 206 protein moiety reduced), composed of 165 amino acid residues with R at position 23. It resembles leukocyte secreted interferon. Widely used as an antiviral or antineoplastic agent.
Indication/DiseaseFor the treatment of hairy cell leukemia, malignant melanoma, and AIDS-related Kaposi's sarcoma.
PharmacodynamicsUpregulates 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. 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 ActionInterferon alpha binds to type I interferon receptors (IFNAR1 and IFNAR2c) which upon dimerization 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 alpha binds less stably to type I interferon receptors than interferon beta.
ToxicityThere is limited experience with overdosage. Postmarketing surveillance includes reports of patients receiving a single dose as great as 10 times the recommended dose. In general, the primary effects of an overdose are consistent with the effects seen with therapeutic doses of interferon alfa-2b. Hepatic enzyme abnormalities, renal failure, hemorrhage, and myocardial infarction have been reported with single administration overdoses and/or with longer durations of treatment than prescribed. Toxic effects after ingestion of interferon alfa-2b are not expected because interferons are poorly absorbed orally.
MetabolismN.A.
AbsorptionAbsorption is high (greater than 80%) when administered intramuscularly or subcutaneously.
Volume of DistributionN.A.
ClearanceN.A.
CategoriesAntiviral Agents and Immunosuppressive Agents
Patents NumberCA1341567
Date of Issue20/02/12
Date of Expiry20/02/29
Drug InteractionZidovudine, The interferon increases the effect and toxicity of zidovudine
TargetInterferon alpha/beta receptor 1,Interferon alpha/beta receptor 2
Information of corresponding available drug in the market
Brand NameINFERGEN
CompanyKadmon Pharmaceuticals, LLC.
Brand DiscriptionInterferon alfacon-1 is a wholly synthetic type-I interferon. The 166-amino acid sequence of interferon alfacon-1 was derived by scanning the sequences of several natural interferon alpha subtypes and assigning the most frequently observed amino acid in each corresponding position resulting in a consensus sequence.
Prescribed forINFERGEN (interferon alfacon-1) is indicated for treatment of chronic hepatitis C in patients 18 years of age or older with compensated liver disease.
Chemical NameN.A.
Formulationsingle-use vials containing 9 mcg and 15 mcg interferon alfacon-1 at a fill volume of 0.3 mL and 0.5 mL, respectively. INFERGEN vials contain 0.03 mg/mL interferon alfacon-1, sodium chloride (5.9 mg/mL), and sodium phosphate (3.8 mg/mL) in Water for Injection, USP.
Physcial AppearnceINFERGEN is a Sterile, clear, colorless, preservative-free liquid
Route of AdministrationSubcutaneous Injection
Recommended DosageThe recommended dose of INFERGEN monotherapy for the initial treatment of chronic HCV infection is 9 mcg administered three times a week as a single subcutaneous injection for 24 weeks.
Contraindicationcontraindicated in patients with hepatic decompensation; autoimmune hepatitis; known hypersensitivity reactions such as urticaria, angioedema, bronchoconstriction, anaphylaxis to interferon alphas or to any component of the product.
Side EffectsINFERGEN alone or in combination with ribavirin causes a broad range of serious adverse reactions;
Useful Linkhttp://www.rxlist.com/infergen-drug.htm http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=29ad47ed-cb94-470b-b3ab-9281abf414d5
PubMed ID19714721, 19291790, 17235418, 16758306, 16179960, 16179960, 16179960, 19714721, 19291790
3-D StructureTh1058 (View) or (Download)