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  • ADC Payloads

    Antibody-drug conjugates (ADCs) are typically formed by an antibody specifically targeting an antigen and a cytotoxic payload through an appropriate linker. The activity, physicochemical properties, and mechanism of action of the payload are key factors that determine the efficacy of an ADC drug, and therefore the payload is an important component of ADC design. An ideal ADC payload should be characterized by sufficient cytotoxicity, low immunogenicity, high stability, and functional groups that can be modified. Common ADC payloads include tubulin inhibitors and DNA damaging agents. Other types of payloads such as transcription inhibitors, immuno-agonists, Bcl-xL inhibitors, and proteasome activity inhibitors are being developed.

    Microtubules are major components of the cytoskeleton in eukaryotic cells and play an important role in maintaining cell morphology, signal transduction, organelle transport, cell movement, cell division, mitosis, and other cellular functions. Tubulin is a component of microtubules. Tubulin inhibitors can interfere with the dynamic combination of microtubules by binding to tubulin. Because their anti-mitosis role, tubulin inhibitors are more toxic to rapidly dividing cells such as cancer cells than to most slow-growing normal cells, making them popular ADC payloads. Common tubulin inhibitors are the auristatins (MMAE and MMAF) and maytansinoids (DM1 and DM4).

    DNA inhibitors can damage DNA through double-strand breaks, alkylation, chimerism, cross-linking and other ways, acting on the whole cell cycle and playing a good therapeutic effect. Representative DNA inhibitors that are developed as ADC payloads include enediyne, pyrrolo[2,1-c][1,4] benzodiazepines (PBD), duocarmycins, and topoisomerase I (TOPO-I) inhibitors. To further expand the range of ADC payloads, RNA splicing inhibitors (Thailanstatin and its analogs) and RNA polymerase II inhibitors (Amatoxins) are two main types of RNA inhibitors developed as ADC payloads.

    Anti-payload Antibodies for ADC Quantitative Analysis

    Because ADCs are molecules composed of antibodies, payloads, and linkers, characterizing the ADC pharmacokinetic (PK) profiles requires measurements of total antibodies, conjugated antibodies, and free payloads. Amerigo Scientific provides high quality anti-payload antibodies for PK studies in the evaluation of ADCs.

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