Antibody-Drug Conjugates (ADCs) are a class of targeted therapies in which a monoclonal antibody is connected to a biologically active, small molecule cytotoxic drug cargo using a linker [1-2]. Upon docking a targeted tumor antigen at the surface of cancer cells, the ADC is internalized, and the cytotoxic cargo is released through the enzymatic cleavage of the linker. Release of the cytotoxic cargo in cancer cells will induce cell death. An essential component of the ADC is the linker, which should be stable when the antibody is circulating in the vascular system but should be labile when the ADC is internalized into cancer cells. Such features allow for improved safety and efficacy.
1. Hamilton GS.2015 2. Pettinato MC.2021