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Product Details:

  • CAS No: 219685-50-4
  • AHFC code:
  • Synonyms: Alexion, Eculizumab, Eculizumab (genetical recombination, h5G1.1, h5G1.1VHC h5G1.1VLC, h5G1.1VHC(+)h5G1.1VLC, h5G1.1VHC+h5G1.1VLC, Immunoglobulin, anti-(human complement C5 alpha-chain) (human-mouse monoclonal 5G1.1 heavy chain), disulfide with human-mouse monoclonal 5G.1.1 light chain, dimer. Molecular weight is approximately 150,000 daltons, Soliris, UNII-A3ULP0F556
  • ATC Code: L04AA25
  • Chemical Formula:
  • Molecular Weight: 148000.0 Da
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB01257
  • SMILES:
  • InChl:
  • PubChem:
  • IUPAC: Immunoglobulin, anti-(human complement C5 a-chain) (human-mouse monoclonal 5G1.1 heavy chain), disulfide with human-mouse monoclonal 5G.1.1 light chain, dimer

Additional Details

Indication:
For the treatment of patients with paroxysmal nocturnal hemoglobinuria (PNH) to reduce hemolysis.
Pharmacodynamics:
Eculizumab is a monoclonal antibody directed against the complement protein C5. This antibody blocks the cleavage of C5 and halts the process of complement-mediated cell destruction. Eculizumab is a product of Alexion Pharmaceuticals and has been shown to be effective in treating paroxysmal nocturnal hemoglobinuria. Eculizumab was approved by the FDA in March, 2007.
Mode of Action:
A genetic mutation in PNH patients leads to the generation of populations of abnormal RBCs (known as PNH cells) that are deficient in terminal complement inhibitors (CD-59), rendering PNH RBCs sensitive to persistent terminal complement-mediated destruction. The destruction and loss of these PNH cells (intravascular hemolysis) results in low RBC counts (anemia) and also fatigue, difficulty in functioning, pain, dark urine, shortness of breath, and blood clots. Eculizumab, the active ingredient in Soliris, is a monoclonal antibody that binds to the complement protein C5 specifically and with high affinity, thereby inhibiting its cleavage to C5a and C5b and subsequent generation of the terminal complement complex C5b-9. Soliris inhibits terminal complement mediated intravascular hemolysis in PNH patients and therefore the destruction of PNH erythrocytes that lack complement protection with CD-59.
Metabolism:
Toxicity:
General Reference:
Hillmen P, Young NS, Schubert J, Brodsky RA, Socie G, Muus P, Roth A, Szer J, Elebute MO, Nakamura R, Browne P, Risitano AM, Hill A, Schrezenmeier H, Fu CL, Maciejewski J, Rollins SA, Mojcik CF, Rother RP, Luzzatto L: The complement inhibitor eculizumab in paroxysmal nocturnal hemoglobinuria. N Engl J Med. 2006 Sep 21;355(12):1233-43. PubmedThomas TC, Rollins SA, Rother RP, Giannoni MA, Hartman SL, Elliott EA, Nye SH, Matis LA, Squinto SP, Evans MJ: Inhibition of complement activity by humanized anti-C5 antibody and single-chain Fv. Mol Immunol. 1996 Dec;33(17-18):1389-401. PubmedDmytrijuk A, Robie-Suh K, Cohen MH, Rieves D, Weiss K, Pazdur R: FDA report: eculizumab (Soliris) for the treatment of patients with paroxysmal nocturnal hemoglobinuria. Oncologist. 2008 Sep;13(9):993-1000. Epub 2008 Sep 10. PubmedRother RP, Rollins SA, Mojcik CF, Brodsky RA, Bell L: Discovery and development of the complement inhibitor eculizumab for the treatment of paroxysmal nocturnal hemoglobinuria. Nat Biotechnol. 2007 Nov;25(11):1256-64. Pubmed
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