ABSTRACT

Certolizumab pegol (CZP) is a recombinant, polyethylene glycolylated, antigen-binding fragment of a humanized monoclonal antibody that selectively targets and neutralizes both soluble and transmembrane tumour necrosis factor (TNF)-a. In contrast to other anti-TNF agents, CZP does not contain Fc region; therefore it does not mediate complement-dependent or antibody-dependent cell-mediated cytotoxicity in vitro. Lack of Fc fragment also reduces placental transfer of CZP. On the other hand, pegylation not only increases the penetration and persistence of CZP in the inflamed tissues, but also reduces renal clearence of CZP. Moreover, pegylation of CZP appears to inhibit non-immune-stimulated degranulation of mast cells, which may explain low incidence of injection-site pain. Finally, monovalent binding of CZP to TNF molecule, prevents formation of immune complexes, thereby reducing neutrophil degranulation and superoxide production.Certolizumab, certolizumab pegol, pegylation, mode of action.