certolizumab pegol

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Ligands
certolizumab pegol

GtoPdb Ligand ID: 6774

Synonyms: CDP870 | Cimzia® | PHA 738144

certolizumab pegol is an approved drug (FDA (2008), EMA (2009))

Comment: This therapeutic is a TNFα neutralising agent. Structurally it is a Fab' fragment of a TNFα-binding monoclonal antibody, which has polyethylene glycol (PEG) conjugated to a free cysteine residue in its hinge region (Cys227 of the heavy chain). Removing the Fc portion minimizes complement-dependent cytotoxicity (CDC) and antibody-dependent cell-mediated cytotoxicity (ADCC), two reactions known to cause unwanted side-effects in mAb therapies. PEGylation is used to increase the drug's half life, as Fab' fragments are normally rapidly degraded in vivo.

View more information in the IUPHAR Pharmacology Education Project: certolizumab pegol

References
1. Choy EH, Hazleman B, Smith M, Moss K, Lisi L, Scott DG, Patel J, Sopwith M, Isenberg DA. (2002) Efficacy of a novel PEGylated humanized anti-TNF fragment (CDP870) in patients with rheumatoid arthritis: a phase II double-blinded, randomized, dose-escalating trial. Rheumatology (Oxford), 41 (10): 1133-7. [PMID:12364632]
2. Nesbitt A, Fossati G, Bergin M, Stephens P, Stephens S, Foulkes R, Brown D, Robinson M, Bourne T. (2007) Mechanism of action of certolizumab pegol (CDP870): in vitro comparison with other anti-tumor necrosis factor alpha agents. Inflamm Bowel Dis, 13 (11): 1323-32. [PMID:17636564]
3. Song IH, Rudwaleit M. (2013) Certolizumab pegol in axial spondyloarthritis. Expert Rev Clin Immunol, 9 (12): 1161-72. [PMID:24215406]

References

1. Choy EH, Hazleman B, Smith M, Moss K, Lisi L, Scott DG, Patel J, Sopwith M, Isenberg DA. (2002)
Efficacy of a novel PEGylated humanized anti-TNF fragment (CDP870) in patients with rheumatoid arthritis: a phase II double-blinded, randomized, dose-escalating trial.
Rheumatology (Oxford), 41 (10): 1133-7. [PMID:12364632]

2. Nesbitt A, Fossati G, Bergin M, Stephens P, Stephens S, Foulkes R, Brown D, Robinson M, Bourne T. (2007)
Mechanism of action of certolizumab pegol (CDP870): in vitro comparison with other anti-tumor necrosis factor alpha agents.
Inflamm Bowel Dis, 13 (11): 1323-32. [PMID:17636564]

3. Song IH, Rudwaleit M. (2013)
Certolizumab pegol in axial spondyloarthritis.
Expert Rev Clin Immunol, 9 (12): 1161-72. [PMID:24215406]