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Antibody-drug conjugates (ADCs) combine the advantages of the precise targeting of monoclonal antibodies with the high killing efficiency of payloads. ADCs have become one of the fastest developing drug categories in recent years due to their low side effects, wide therapeutic applications, and high therapeutic index. The cytotoxic payload is an important component of ADC design, and the other components are an antibody and a linker. The activity and physicochemical properties of payloads directly affect the efficacy of ADCs. An ideal cytotoxic payload should have sufficient toxicity, low immunogenicity, high stability, and functional groups that can be modified. In addition, the water solubility of the payload and its stability during ADC preparation and cycling are also important.

The mechanism of action of the payload is a critical determinant of ADC performance and common mechanisms include tubulin inhibition and DNA-damaging. Tubulin inhibitors can kill target cells by disrupting their cytoskeleton structures and interfering with mitosis. In particular, tumor cells are more sensitive to tubulin inhibitors because they divide faster than normal cells. DNA-damaging agents kill tumor cells by disrupting the DNA structure through double-strand breaks, alkylation, chimerism, and cross-linking. Representative DNA-damaging payloads include enediyne, topoisomerase I inhibitors, and pyrrolobenzodiazepines. In addition, RNA polymerase inhibitors, B‐cell lymphoma‐extra‐large (Bcl‐xL) inhibitors, and immunostimulants are being developed as novel ADC payloads.

Amerigo Scientific offers DNA damaging agents, tubulin inhibitors, and other cytotoxic agents as payloads for the preparation of ADCs.