certolizumab pegol   Click here for help

GtoPdb Ligand ID: 6774

Synonyms: CDP870 | Cimzia® | PHA 738144
Approved drug Immunopharmacology Ligand
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.
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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
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
tumour necrosis factor shed form Primary target of this compound Hs Antibody Binding - - - 2
Description: Note IC90 value of 3ng/ml is provided