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 |
Immunopharmacology Comments |
By neutralising TNFα (soluble and membrane forms), certolizumab pegol disrupts production of pro-inflammatory cytokines such as IL-1β, and this action underlies its effectiveness in treating autoimmune diseases. |
Immunopharmacology Disease | |||
Disease | X-Refs | Comment | References |
Rheumatoid arthritis |
Disease Ontology:
DOID:7148 OMIM: 180300 |
An anti-TNFα therapy approved for RA. | |
Crohn's disease |
Disease Ontology:
DOID:8778 OMIM: 266600 Orphanet: ORPHA206 |
An anti-TNFα therapy approved for CD. | |
Axial spondyloarthritis | Approved drug for axial spondyloarthritis (EMA 2009) | ||
Psoriasis |
Disease Ontology:
DOID:8893 |
Approved drug for moderate-to-severe plaque psoriasis (FDA 2018) and psoriatic arthritis (EMA 2009). |