title: PEGylated drugs in rheumatology--why develop them and do they work?
abstract: Lack of efficacy and drug-related adverse effects are important reasons for the discontinuation of treatment in patients with rheumatic diseases. The development of new biologic therapies seeks to address these problems by specifically targeting the pathogenic mechanisms of disease. Most current biologics are proteins (particularly antibodies and enzymes) administered parenterally. It is important to optimize properties such as serum half-life, immunogenicity and solubility. Companies have thus begun to modify the drugs by conjugate chemistry, binding inert molecules such as polyethylene glycol (PEG) to biologic molecules to improve their pharmacodynamic properties. The use of PEG to alter these properties has to be weighed against the negative aspects of PEGylation, such as decreased activity and heterogeneity. This review focuses on the currently available PEGylated drugs used in rheumatological diseases, their efficacy, drawbacks and the current clinical trial evidence supporting their use.
authors: Centre for Rheumatology Research, Division of Medicine, University College London, Room 412 Rayne Institute, 5 University Street, London WC1E 6JF, UK. anisur.rahman@ucl.ac.uk.
authors: Thomas
authors: T
authors: McDonnell
authors: Yiannis
authors: Y
authors: Ioannou
authors: Anisur
authors: A
authors: Rahman
mesh_terms: D018501:Antirheumatic Agents / Q000493:pharmacokinetics / Q000627:therapeutic use*; D001688:Biological Products / Q000493:pharmacokinetics / Q000627:therapeutic use*; D006207:Half-Life; D006801:Humans; D007125:Immunogenetics; D011092:Polyethylene Glycols; D012216:Rheumatic Diseases / Q000188:drug therapy*; D016896:Treatment Outcome
chemical_list: D018501:Antirheumatic Agents; D001688:Biological Products; D011092:Polyethylene Glycols
keywords: PEGylation; clinical trials; gout; rheumatoid arthritis
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