1. Peginterferon alfa-2b Drugbank ID : DB00022
Protein average weight :
Half life : The mean elimination half-life is approximately 40 hours (range 22 to 60 hours) in patients with HCV infection.

2. Description : Indication : Pharmacodynamics :
Peginterferon alfa-2b is a covalent conjugate of recombinant alfa-2b interferon with monomethoxy polyethylene glycol (PEG). The average molecular weight of the PEG portion of the molecule is 12,000 daltons. The average molecular weight of the PEG-Intron molecule is approximately 31,000 daltons. The specific activity of peginterferon alfa-2b is approximately 0.7 x 108 IU/mg protein. Interferon alfa-2b is a water-soluble protein with a molecular weight of 19,271 daltons produced by recombinant DNA techniques. It is obtained from the bacterial fermentation of a strain of <i>Escherichia coli</i> bearing a genetically engineered plasmid containing an interferon gene from human leukocytes. The PEG strand protects the molecule in vivo from proteolytic breakdown, substantially increases its in vivo half-life, and reduces immunogenicity by wrapping around and physically hindering access to the protein portion of the molecule.
Indication :
For the treatment of chronic hepatitis C in patients not previously treated with interferon alpha who have compensated liver disease and are at least 18 years of age.
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 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.

3. Mechanism of action :Interferon 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.
Absorption : Following a single subcutaneous dose of peginterferon alfa-2b, the mean absorption half-life (t&frac12; k_a) was 4.6 hours.
Route of Elimination : Renal elimination accounts for 30% of the clearance.
Clearance : * Oral cl=22 mL/hr∙kg [patients with HCV infection]

4. Drug Interaction: Targets : Affected organisms :
Aminophylline : Interferon increases the effect and toxicity of theophylline
Dyphylline : Interferon increases the effect and toxicity of theophylline
Oxtriphylline : Interferon increases the effect and toxicity of theophylline
Theophylline : Interferon increases the effect and toxicity of theophylline
Targets :
Interferon alpha/beta receptor 1,Interferon alpha/beta receptor 2
Affected organisms :
Humans and other mammals .

5. Categories : Patents : Sequence : Immunosuppressive Agents
Country Patent Number Approved Expires
Canada
Canada
Sequence :
CDLPQTHSLGSRRTLMLLAQMRRISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMIQQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMKEDSILAVRKYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE

6. Brands : PEG-Intron
Company : Schering Corp
Description : PegIntron, peginterferon alfa-2b, is a covalent conjugate of recombinant alfa-2b interferon with monomethoxy polyethylene glycol (PEG). The average molecular weight of the PEG portion of the molecule is 12,000 daltons. The average molecular weight of the PegIntron molecule is approximately 31,000 daltons. The specific activity of peginterferon alfa-2b is approximately 0.7 x 108 IU/mg protein.
Used for/Prescribed for : used to treat chronic hepatitis C in adults. Peginterferon alfa-2b is often used in combination with another medication called ribavirin (Rebetol, Ribasphere) to treat hepatitis C in adults and children who are at least 3 years old.
Formulation : white tablet-like solid that is whole/in pieces or as a loose powder, and 1.11 mg dibasic sodium phosphate anhydrous, 1.11 mg monobasic sodium phosphate dihydrate, 59.2 mg sucrose, and mg polysorbate 80.
Form : poowder
Route of administration : subcutaneous injection

7. Dosage : The recommended dose of PegIntron is 1. 5 mcg/kg/week
Dosage : The recommended dose of PegIntron is 1.5 mcg/kg/week. The volume of PegIntron to be injected depends on the strength of PegIntron and patient's body weight Contraindication : allergic or in case of having autoimmune hepatitis, liver failure, severe kidney disease, a hemoglobin blood cell disorder, Side effects : vision problems; fast heart rate, feeling like you might pass out Drug interaction : A total of 179 drugs (577 brand and generic names) are known to interact with PegIntron (peginterferon alfa-2b) among which 22 major (88 brand and generic names), 152 moderate (471 brand and generic names) and 5 minor drug interactions (18 brand and generic names).

8. References : http://www. pegintron. com/peg/pegintron/consumer/index