Copyright WuXi AppTec
Antibody-drug conjugates (ADCs) represent a significant paradigm shift in cancer treatment, marrying the precise target recognition of monoclonal antibodies with the potent cell-killing capabilities of cytotoxic agents. In contrast to traditional small-molecule therapies, ADCs are multifaceted structures with three distinct components — i.e., antibody, cytotoxic payload and a linker — each playing a crucial role in the drug’s operation and effectiveness.
Following administration, the antibody guides the payload to the tumor site, relying on the antibody’s ability to recognize and bind to cancer cell antigens. Once at the tumor site, the linker undergoes cleavage — through enzymatic action, changes in pH, exposure to light, iron or glutathione (GSH) or breakdown in lysosome — releasing the cytotoxic payload or payload-related metabolites to exert its lethal effect on the canc…