Evaluation of pharmacokinetics and pharmacodynamics and clinical efficacy of certolizumab pegol for Crohn's disease.

INTRODUCTION: TNF-α antagonists have transformed the treatment of patients with Crohn's disease (CD). Certolizumab pegol (CZP) is the third TNF-α antagonist to be approved for use in the United States but is not currently approved in Europe. AREAS COVERED: This review evaluates the pharmacokinetics, pharmacodynamics and efficacy of CZP in CD. Safety, immunogenicity and its use in pregnancy have also been assessed. A literature search was conducted using Pub Med (2004 - 2014) for the terms 'Crohn's disease' and 'certolizumab pegol' or 'certolizumab' or 'cimzia'. Additional studies were identified from other sources including citation. EXPERT OPINION: As a Fab' fragment, CZP is effective in binding TNF-α, but does not cause Fc-mediated effects. PEGylation has improved its pharmacokinetic profile and allowed for an increased half-life of 2 weeks. Benefit for inducing response (an improvement in symptoms) and maintenance of remission has been shown. However, the benefit is less clear for the more stringent end-points of inducing remission and mucosal healing. There may be an advantage from the PEGylated formulation of CZP in terms of reduced injection-site reactions, reduced placental transfer in pregnancy and as a treatment option in patients who are unable to tolerate infliximab.