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Synonyms: h5G1.1 | h5G1.1VHC | Soliris®
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]. Biosimilars: 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 | ||||||||||||||||||||||||||||||||||
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