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Antibody–Drug Conjugates for Cancer Therapy

by Umbreen Hafeez 1,2,3, Sagun Parakh 1,2,3, Hui K. Gan 1,2,3,4 and Andrew M. Scott 1,3,4,5,*
Tumour Targeting Laboratory, Olivia Newton-John Cancer Research Institute, Melbourne, VIC 3084, Australia
Department of Medical Oncology, Olivia Newton-John Cancer and Wellness Centre, Austin Health, Melbourne, VIC 3084, Australia
School of Cancer Medicine, La Trobe University, Melbourne, VIC 3084, Australia
Department of Medicine, University of Melbourne, Melbourne, VIC 3084, Australia
Department of Molecular Imaging and Therapy, Austin Health, Melbourne, VIC 3084, Australia
Author to whom correspondence should be addressed.
Academic Editor: João Paulo C. Tomé
Molecules 2020, 25(20), 4764;
Received: 14 August 2020 / Revised: 10 October 2020 / Accepted: 13 October 2020 / Published: 16 October 2020
(This article belongs to the Special Issue Immunoconjugates for Cancer Imaging and Therapy)
Antibody–drug conjugates (ADCs) are novel drugs that exploit the specificity of a monoclonal antibody (mAb) to reach target antigens expressed on cancer cells for the delivery of a potent cytotoxic payload. ADCs provide a unique opportunity to deliver drugs to tumor cells while minimizing toxicity to normal tissue, achieving wider therapeutic windows and enhanced pharmacokinetic/pharmacodynamic properties. To date, nine ADCs have been approved by the FDA and more than 80 ADCs are under clinical development worldwide. In this paper, we provide an overview of the biology and chemistry of each component of ADC design. We briefly discuss the clinical experience with approved ADCs and the various pathways involved in ADC resistance. We conclude with perspectives about the future development of the next generations of ADCs, including the role of molecular imaging in drug development. View Full-Text
Keywords: antibody–drug conjugate; ADC; monoclonal antibody; cytotoxic payload; linkers; cancer; molecular imaging antibody–drug conjugate; ADC; monoclonal antibody; cytotoxic payload; linkers; cancer; molecular imaging
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MDPI and ACS Style

Hafeez, U.; Parakh, S.; Gan, H.K.; Scott, A.M. Antibody–Drug Conjugates for Cancer Therapy. Molecules 2020, 25, 4764.

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