Medicinal Chemistry Reviews

Volume 52, Chapter 19

Thinking Small and Dreaming Big:  Medicinal Chemistry Strategies for Designing Optimal Antibody-Drug Conjugates (ADCs)

L. Nathan Tumey

1.          Introduction                                                                                                               363

2.         Thinking Small: Optimization of the Linker-Payload                                            364

            2.1        Advancing New Linker-Cleavage Mechanisms                                           364

            2.2       Understanding the Released Species                                                          367

            2.3       Optimizing the Linker Stability                                                                    370

3.         Dreaming Big: Optimization of the Bioconjugate                                                  373

            3.1        The Impact of the Linker-Payload on the Biophysical Properties 

                        of the ADC                                                                                                     373

            3.2       The Impact of Conjugation Site on the Stability of the Linker Payload  375

4.         Conclusions and Future Outlook                                                                             379

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