Tìm theo
Peginterferon alfa-2a
Thuốc giảm miễn dịch
Thuốc Gốc
Biotech
CAS: 198153-51-4
ATC: L03AB11
ĐG : F Hoffmann La Roche Ltd. , http://www.roche.com
PTK: 60000.0000
Human interferon 2a, is a covalent conjugate of recombinant alfa-2a interferon with a single branched bis-monomethoxy polyethylene glycol (PEG) chain. The PEG moiety is linked at a single site to the interferon alfa moiety via a stable amide bond to lysine. Peginterferon alfa-2a has an approximate molecular weight of 60,000 daltons. Interferon alfa-2a is produced using recombinant DNA technology in which a cloned human leukocyte interferon gene is inserted into and expressed in Escherichia coli. The resultant protein is 165 amino acids. 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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Phân tử khối
60000.0000
Độ tan chảy
61 °C
Điểm đẳng điện tích
5.99
Dược Lực Học : 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.
Cơ Chế Tác Dụng : Human interferon 2a, is a covalent conjugate of recombinant alfa-2a interferon with a single branched bis-monomethoxy polyethylene glycol (PEG) chain. The PEG moiety is linked at a single site to the interferon alfa moiety via a stable amide bond to lysine. Peginterferon alfa-2a has an approximate molecular weight of 60,000 daltons. Interferon alfa-2a is produced using recombinant DNA technology in which a cloned human leukocyte interferon gene is inserted into and expressed in Escherichia coli. The resultant protein is 165 amino acids. 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. 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.
Dược Động Học :

▧ Half Life :
Terminal half life is 80 hours (range 50 to 140 hours).
Chỉ Định : For treatment of hairy cell leukemia, malignant melanoma, and AIDS-related Kaposi's sarcoma.
Tương Tác Thuốc :
  • Aminophylline Interferon increases the effect and toxicity of theophylline
  • Dyphylline Interferon increases the effect and toxicity of theophylline
  • Etravirine Etravirine (a CYP2C9 substrate), when used concomitantly with peginterferon alfa-2a, may experience a decrease in serum concentration. It is recommended to monitor effectiveness of etravirine therapy.
  • Oxtriphylline Interferon increases the effect and toxicity of theophylline
  • Telbivudine Co-administration of Peginterferon alpha-2a and Telbivudine may increase the risk of serious peripheral neuropathy.
  • Theophylline Interferon increases the effect and toxicity of theophylline
Liều Lượng & Cách Dùng : Solution - Subcutaneous
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Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00008
GenBank
http://www.ncbi.nlm.nih.gov/nuccore/J00207
PharmGKB
http://www.pharmgkb.org/drug/PA164749390
Wikipedia
http://en.wikipedia.org/wiki/Peginterferon_alfa-2a
RxList
http://www.rxlist.com/cgi/generic3/pegasys.htm
Drugs.com
http://www.drugs.com/cdi/peginterferon-alfa-2a.html
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