Chemical Linkers in Antibody–Drug Conjugates (ADCs)
Chapter 9: The Use of Uniform PEG Compounds in the Design of ADCs
Published:15 Dec 2021
M. W. Giese, R. H. Woodman, G. T. Hermanson, and P. D. Davis, in Chemical Linkers in Antibody–Drug Conjugates (ADCs), ed. F. van Delft and J. M. Lambert, The Royal Society of Chemistry, 2021, ch. 9, pp. 286-376.
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Uniform polyethylene glycol (PEG) linkers and spacers have proven to be critical components for modifying and mediating the properties of antibody–drug conjugates (ADCs). These short, flexible, amphiphilic compounds lack polymeric dispersity and can be used and analyzed like highly pure small molecules. This chapter closely examines how these linkers and spacers are used in the construction of antibody–drug conjugates and how they affect their physicochemical, pharmacodynamic, and pharmacokinetic properties. Hypotheses are offered to explain how PEG linkers affect these properties. Suggestions for future ADC applications are extrapolated from current applications and other available evidence.