Synonyms: CDP870 | Cimzia® | PHA 738144
certolizumab pegol is an approved drug (FDA (2008), EMA (2009))
Compound class:
Antibody
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 |
Bioactivity Comments |
Certolizumab pegol neutralises soluble TNFα in vitro, with an IC90 of 3ng/ml [2], neutralises the effects mediated by membrane bound TNFα, and inhibits production of IL-1β in monocytes stimulated with LPS. |
Selectivity at ligand targets | ||||||||||||||||||||||||||||||||||
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