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Issue 16, 2019
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Cleavable linkers in antibody–drug conjugates

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Antibody–Drug Conjugates (ADCs) are now established as a major class of therapeutics for the clinical treatment of cancer. The properties of the linker between the antibody and the payload are proven to be critical to the success of an ADC. Although ADC linkers can be ‘non-cleavable’, the vast majority of ADCs in clinical development have specific release mechanisms to allow controlled linker cleavage at the target site and are thus termed ‘cleavable’. In recent years, the development of new methods of drug release from ADCs has continued in parallel to the deepening understanding of the biological processes underlying the mechanisms of action of pre-existing technologies. This review summarises the advances in the field of cleavable linker technologies for ADCs.

Graphical abstract: Cleavable linkers in antibody–drug conjugates

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Article information

09 Apr 2019
First published
11 Jul 2019

Chem. Soc. Rev., 2019,48, 4361-4374
Article type
Tutorial Review

Cleavable linkers in antibody–drug conjugates

J. D. Bargh, A. Isidro-Llobet, J. S. Parker and D. R. Spring, Chem. Soc. Rev., 2019, 48, 4361
DOI: 10.1039/C8CS00676H

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