Certolizumab Pegol Therapy of Rheumatoid Arthritis: Overview

First-line treatment for moderate to severe rheumatoid arthritis (RA) has been the use of disease-modifying anti-rheumatic drugs (DMARDs), e.g., methotrexate. Because of the cases of failure reported to respond to available treatments, newer RA drugs including tumor necrosis factor (TNF-a) blockers have emerged. Certolizumab pegol (CZP) is a unique polyethylene glycolated (PEG) humanized monoclonal antibody designed specifically to target TNF-a pro-inflammatory cytokine. Given that its properties closely reflect its PEG fragment, CZP has demonstrated a clear efficiency. Pharmacokinetics and pharmacodynamics of CZP are described together with Phase II and III CZP clinical studies focused on CZP efficiency and safety. We also discuss the future of CZP and new clinical studies that might help physicians in their choice of CZP among available TNF-a blockers. Drug Dev Res 72:603-614, 2011. r 2011 Wiley Periodicals, Inc.