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. |
References |
1. Evans MJ, Matis L, Mueller EE, Nye SH, Rollins S, Rother RP, Springhorn JP, Squinto SP, Thomas TC, Wang Y et al.. (1995)
Methods and compositions for the treatment of glomerulonephritis and other inflammatory diseases. Patent number: WO1995029697A1. Assignee: Alexion Pharma Inc.. Priority date: 02/05/1994. Publication date: 09/11/1995. |
2. Horiuchi T, Tsukamoto H. (2016)
Complement-targeted therapy: development of C5- and C5a-targeted inhibition. Inflamm Regen, 36: 11. [PMID:29259684] |
3. Pittock SJ, Berthele A, Fujihara K, Kim HJ, Levy M, Palace J, Nakashima I, Terzi M, Totolyan N, Viswanathan S et al.. (2019)
Eculizumab in Aquaporin-4-Positive Neuromyelitis Optica Spectrum Disorder. N Engl J Med, 381 (7): 614-625. [PMID:31050279] |
4. Rother RP, Rollins SA, Mojcik CF, Brodsky RA, Bell L. (2007)
Discovery and development of the complement inhibitor eculizumab for the treatment of paroxysmal nocturnal hemoglobinuria. Nat Biotechnol, 25 (11): 1256-64. [PMID:17989688] |
5. Sheridan D, Yu ZX, Zhang Y, Patel R, Sun F, Lasaro MA, Bouchard K, Andrien B, Marozsan A, Wang Y et al.. (2018)
Design and preclinical characterization of ALXN1210: A novel anti-C5 antibody with extended duration of action. PLoS ONE, 13 (4): e0195909. [PMID:29649283] |