Biologics are drugs made from complex molecules manufactured using living microorganisms, plant or animal cells. Many biologics are produced using recombinant DNA technology. Glycoproteins represent a major portion of biologics, including monoclonal antibodies, Fc-fusion proteins and other therapeutic proteins or enzymes. A thorough understanding of the nature and function of the carbohydrate moiety and its impact on pharmacology properties is essential in discovering, developing and manufacturing safe and efficacious glycoprotein biopharmaceuticals. This review summarizes the recent development in glycosylation engineering and characterization methodology. Examples of N-linked and/or O-linked glycosylation impacting drug pharmacology properties (including activity, pharmacokinetics, clearance, and immunogenicity) of marketed and developing therapeutic proteins are presented.
Keywords: ADCC, CHO, Fc-fusion, Fluorescence, Fucose, Glycan release, Glycoengineering, Glycoprotein, Glycosylation, Half-life, HILIC, HPLC, IgG, mAbs, Mass spectrometry, PAD, Pharmacodynamics, Pharmacokinetics, Recombinant human erythropoietin, Sialic acids.