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Certolizumab pegol: a PEGylated anti-tumour necrosis factor alpha biological agent

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Book cover PEGylated Protein Drugs: Basic Science and Clinical Applications

Part of the book series: Milestones in Drug Therapy ((MDT))

Abstract

Tumour necrosis factor (TNF)α is a proinflammatory cytokine involved in systemic inflammation that mediates chronic inflammatory diseases such as rheumatoid arthritis (RA), Crohn’s disease (CD) and psoriasis. Recognition of TNFα as a primary mediator of inflammatory disease has driven the development of monoclonal antibodies (mAbs) against TNFα as potential novel therapies for these disorders. Certolizumab pegol is a novel, polyethylene glycol (PEG)-conjugated, humanised, antigen-binding fragment (Fab’) of an anti-TNFα mAb that does not mediate apoptosis or neutrophil degranula- tion. Preclinical studies have shown excellent bioavailability, with preferential distribution and retention in inflamed tissue, which could be due to the low diffusion rate of PEGylated molecules and/or the lack of an Fc, which prevents FcRn-mediated transport. Pharmacokinetics are linear and predictable. Certolizumab pegol is a potentially valuable new treatment option for several inflammatory diseases. It has shown promising efficacy and tolerability results in Phase II and III trials for RA, CD and psoriasis.

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Nesbitt, A.M., Stephens, S., Chartash, E.K. (2009). Certolizumab pegol: a PEGylated anti-tumour necrosis factor alpha biological agent. In: Veronese, F.M. (eds) PEGylated Protein Drugs: Basic Science and Clinical Applications. Milestones in Drug Therapy. Birkhäuser Basel. https://doi.org/10.1007/978-3-7643-8679-5_14

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