Eculizumab

drugbox
type = mab


source = Humanized
target = Complement protein C5
CAS_number = 219685-50-4
ATC_prefix = L04
ATC_suffix = AA25
PubChem =
DrugBank =
chemical_formula =
molecular_weight = 148 kDa
bioavailability =
protein_bound =
metabolism =
elimination_half-life = 8 to 15 days (mean 11 days)
excretion =
pregnancy_AU =
pregnancy_US = C
pregnancy_category=
legal_AU =
legal_CA =
legal_UK = POM
legal_US = Rx-only
legal_status =
routes_of_administration = Intravenous infusion
licence_EU = Soliris
licence_US = Eculizumab

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. [cite journal | author = 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 | title = The complement inhibitor eculizumab in paroxysmal nocturnal hemoglobinuria | journal = N Engl J Med | volume = 355 | issue = 12 | pages = 1233–43 | year = 2006 | pmid = 16990386 | doi = 10.1056/NEJMoa061648] 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 exhibits 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.

References

External links

* [http://www.healthvalue.net/globulerougeexplose.html Flash animation of eculizumab mechanism of action]