Antibody-drug Conjugates with Novel Kinesin Spindle Protein Inhibitor Payloads and a Tailor-made Linker Chemistry

With the approval of meanwhile five ADCs and more than 80 ADCs in clinical trials, the ADC landscape has developed rapidly during the last decade. However, as indicated also by the large number of ADCs which failed in the clinic, it remains challenging to achieve a sufficiently large therapeutic window in cancer patients.

Pharmacokinetic Considerations to Maximize an ADC’s Therapeutic Index

The Antibody-drug Conjugate (ADC) field is poised for several significant advances in solid tumors as the industry has built upon knowledge gained over the past several years. The biggest challenge facing clinical translation of these drugs is improving the therapeutic index (TI). With the use of proven targeting agents (monoclonal antibodies) and proven cancer cytotoxins (e.g. microtubule inhibitors and DNA alkylating agents), increasing delivery to cancer cells while avoiding healthy tissue is the key issue in improving the TI.