title: Evaluation of pharmacokinetics and pharmacodynamics and clinical efficacy of certolizumab pegol for Crohn's disease.
abstract: BACKGROUND
  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.
  
  
  METHODS
  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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Gastroenterology Unit, Royal Hallamshire Hospital , P Floor, Glossop Road, Sheffield S10 2JF , UK.
authors.forename: Gloria S Z
authors.initials: GS
authors.lastname: Tun
authors.forename: Alan J
authors.initials: AJ
authors.lastname: Lobo
mesh_terms: D000818:Animals; D061067:Antibodies, Monoclonal, Humanized / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D000068582:Certolizumab Pegol; D003424:Crohn Disease / Q000188:drug therapy* / Q000503:physiopathology; D005260:Female; D006207:Half-Life; D006801:Humans; D007140:Immunoglobulin Fab Fragments / Q000494:pharmacology / Q000627:therapeutic use*; D007166:Immunosuppressive Agents / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D011092:Polyethylene Glycols / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D011247:Pregnancy; D012074:Remission Induction; D016896:Treatment Outcome; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors
chemical_list: D061067:Antibodies, Monoclonal, Humanized; D007140:Immunoglobulin Fab Fragments; D007166:Immunosuppressive Agents; D014409:Tumor Necrosis Factor-alpha; D011092:Polyethylene Glycols; D000068582:Certolizumab Pegol
keywords: Crohn’s disease; TNF-α antagonists; certolizumab pegol; cimzia; pharmacodynamics; pharmacokinetics; remission rate; response rate