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

Abstract

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.

Keywords:

• certolizumab pegol
• cimzia
• Crohn’s disease
• pharmacodynamics
• pharmacokinetics
• remission rate
• response rate
• TNF-α antagonists

Declaration of interest

Alan Lobo is on the advisory board for Takeda Pharmaceuticals (UK) and Inflectra UK. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

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