Chemical Linkers in Antibody–Drug Conjugates (ADCs)
Chapter 2: Antibody Conjugation Technologies
Published:15 Dec 2021
Special Collection: 2021 ebook collectionSeries: Drug Discovery
G. T. Hermanson, F. L. van Delft, 2021. "Antibody Conjugation Technologies", Chemical Linkers in Antibody–Drug Conjugates (ADCs), Floris van Delft, John M. Lambert
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A key quality attribute of any ADC is the mode of attachment of the linker-drug to the monoclonal antibody. Early generation technologies were based exclusively on one of two approaches, i.e. covalent bond formation with – abundantly available – lysine or cysteine sidechains. However, the need to develop ADCs with increased therapeutic index, and the insight that homogeneity, proper site selection, and stability all play a key role in this matter, has served as an inspiration for the development of a contemporary conjugation toolbox filled with alternative conjugation approaches. This chapter discusses in depth the state of the art in antibody conjugation, providing a comprehensive overview of technologies currently employed in clinical and late-stage preclinical ADC programs. The pros and cons of each technology are also discussed. Besides, a range of promising emerging technologies is highlighted, judged on their potential for application in next-generation ADCs.