eculizumab   Click here for help

GtoPdb Ligand ID: 6884

Synonyms: h5G1.1 | h5G1.1VHC | Soliris®
Approved drug Immunopharmacology Ligand
eculizumab is an approved drug (FDA (2011), EMA (2007))
Compound class: Antibody
Comment: Eculizumab is a humanized monoclonal antibody targeting terminal complement activation, by binding to complement component C5 and inhibiting the production of C5a [4]. It is the first approved therapy for paroxysmal nocturnal hemoglobinuria.
Eculizumab's developers, Alexion Pharmaceuticals have developed a next-generation version of eculizumab called ravulizumab (ALXN1210; FDA approved in December 2018), that has a longer circulating half-life than the originator, which allows for monthly dosing.
The evidence confirming C5, C5a and the C5a receptor as anti-inflammatory and anti-cancer drug targets is reviewed by Horiuchi and Tsukamoto (2016) [2].

Amgen's biosimilar ABP 959 (Bekemv®) was approved by the EMA in April 2023.
Samsung Bioepis' biosimilar (SB12; Epysqli®) was approved by the EMA in May 2023.
BOW080 (Polpharma Biologics, formerly Epirus Biopharmaceuticals) was in development, but this project appears to have been discontinued.
Bioactivity Comments
Eculizumab binds to and blocks the cleavage of the complement protein C5, thereby preventing the formation of C5a. The terminal half-life of eculizumab is 11.3 ± 3.4 days [4].
Selectivity at ligand targets
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
complement C5 Primary target of this compound Hs Antibody Binding 9.2 – 10.5 pKd - 1,5
pKd 10.5 (Kd 3x10-11 M) [5]
Description: At pH7.4 in a SPR assay.
pKd 10.5 (Kd 3x10-11 M) [1]
pKd 9.2 (Kd 6x10-10 M) [5]
Description: At pH6.0 in a SPR assay.