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). |