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.
