eculizumab

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Ligands
eculizumab

GtoPdb Ligand ID: 6884

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

eculizumab is an approved drug (FDA (2011), EMA (2007))

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]

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]