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Cytotoxic Payloads for Antibody–Drug Conjugates Editors: David E Thurston, Paul J M Jackson


About this book

Antibody–drug conjugates (ADCs) represent one of the most promising and exciting areas of anticancer drug discovery. Five ADCs are now approved in the US and EU [i.e., ado-trastuzumab emtansine (Kadcyla™), brentuximab vedotin (Adcetris™), inotuzumab ozogamicin (Besponsa™), gemtuzumab ozogamicin (Mylotarg™) and moxetumomab pasudotox-tdfk (Lumoxiti®)] and over 70 others are in various stages of clinical development, with impressive interim results being reported for many.

The technology is based on the concept of delivering a cytotoxic payload selectively to cancer cells by attaching it to an antibody targeted to antigens on the cell surfaces. This approach has several advantages including the ability to select patients as likely responders based on the presence of antigen on the surface of their cancer cells and a wider therapeutic index, given that ADC targeting enables a more efficient delivery of cytotoxic agents to cancer cells than can be achieved by conventional chemotherapy, thus minimising systemic toxicity.

Although there are many examples of antibodies that have been developed for this purpose, along with numerous linker technologies used to attach the cytotoxic agent to the antibody, there is presently a relatively small number of payload molecules in clinical use. The purpose of this book is to describe the variety of payloads used to date, along with a discussion of their advantages and disadvantages and to provide information on novel payloads at the research stage that may be used clinically in the future.

From the book series:
Drug Discovery

Book content

  • 1. Introduction to ADCs and their Components
  • 2. Design Factors Important for ADC Payloads
  • 3. The Use of Molecular Modelling Techniques in ADC Payload Discovery and Development
  • 4. Auristatin Payloads for Antibody-Drug Conjugates
  • 5. Maytansinoid Payloads
  • 6. Colchicine, Vinblastine and Taxol-Based Payloads
  • 7. Traditional Cytotoxic Agents as ADC Payloads
  • 8. Topoisomerase Inhibitors as ADC Payloads
  • 9. Duocarmycins
  • 10. CXI Dimers as ADC Payloads
  • 11. Duocarmycin-PBD Dimers
  • 12. Calicheamicins
  • 13. Pro-Pyrrolobenzodiazepines and Conjugates as ADC Payloads
  • 14. Pyrrolobenzodiazepine Dimers
  • 15. Indolinobenzodiazepine Dimers (IGNs) as ADC Payloads
  • 16. Pyridinobenzodiazepines (PDDs): Development of Sequence-Selective DNA Mono-Alkylating Agents as ADC Payloads
  • 17. Splicing Inhibitors as ADC Payloads
  • 18. Tubulysins as Novel ADC Payloads
  • 19. RNA Polymerase II 
  • Inhibitors
  • 20. Protein Toxin Payloads for ADCs
  • 21. Health and Safety Aspects of Ultratoxic Payloads
  • 22. The Future of ADC Payloads

The print version of this book is planned for release on 15 July 2019. Information about this book is subject to change without notice.

Pre-order hardback £179.00 *
* Exclusive of taxes
This book contains 500 pages.

Publication details

Copyright year: 2019
Print ISBN: 978-1-78801-077-1
ePub eISBN: 978-1-78801-845-6
Citation: