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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Summary of Clinical Use Click here for help
Used to treat rheumatoid arthritis (RA) and Crohn's disease [1]. May also have some effect in related conditions such as axial spondyloarthritis [3]. The EMA granted Europe-wide approval for the use of this drug in patients with RA (moderate to severe, active disease and severe, active and progressive disease), axial spondyloarthritis and psoriatic arthritis in 2009. FDA approval was expanded to include treatment of moderate-to-severe plaque psoriasis, in June 2018.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
A recombinant Fab' antibody fragment/40kDa polyethylene glycol (PEG2MAL40K) conjugate against TNFα. By neutralising TNFα (soluble and membrane forms), certolizumab pegol disrupts production of pro-inflammatory cytokines such as IL-1β, and this may account for its effectiveness in treating autoimmune conditions such as Crohn's disease [2] and rheumatoid arthritis.
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