Eculizumab

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Eculizumab?
Therapeutic monoclonal antibody
Source	Humanized
Target	Complement protein C5
Identifiers
CAS number	219685-50-4
ATC code	L04AA25
PubChem	?
Chemical data
Formula	?
Mol. mass	148 kDa
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	8 to 15 days (mean 11 days)
Excretion	?
Therapeutic considerations
Licence data	EU, US
Pregnancy cat.	C(US)
Legal status	POM(UK) ℞-only(US)
Routes	Intravenous infusion

Eculizumab (INN and USAN, trade name Soliris) 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.^[1] Eculizumab was approved by the United States Food and Drug Administration (FDA) on March 16, 2007 and was later approved by the European Medicines Agency on June 20, 2007.

Ecuilzumab exibits its theraputic activity by binding to the 2b subunit of the C5 convertase enzyme. C5 convertase is produced by the binding of subunits C4b, C2a and C3b to the surface of the bacterium. Binding of Eculizumab to the 2b subunit results in a reduction of the esterase activity of this subunit, and therefore prevents C5 convertase from hydrolysizing C5 into the C5a and C5b subunits.

[edit] References

1. ^ Hillmen P, Young N, Schubert J, Brodsky R, Socié G, Muus P, Röth A, Szer J, Elebute M, Nakamura R, Browne P, Risitano A, Hill A, Schrezenmeier H, Fu C, Maciejewski J, Rollins S, Mojcik C, Rother R, Luzzatto L (2006). "The complement inhibitor eculizumab in paroxysmal nocturnal hemoglobinuria". N Engl J Med 355 (12): 1233–43. doi:10.1056/NEJMoa061648. PMID 16990386. 

[edit] External links

• Flash animation of eculizumab mechanism of action

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