Antibody drug conjugates (ADCs) have staged a comeback in the past 7 years. They demonstrate a synergistic advantage of increased specificity, affinity, and circulatory half-life offered by the antibody as well as cytotoxicity afforded by the small molecule. While the beneficial properties of ADCs are obvious, the scarcity of approved ADCs highlights the need to further develop strategies for development of ADCs. Traditional ADC development uses lysine or cysteine residues for conjugation. This results in varying antibody/drug ratios. Furthermore, traditional ADCs have floppy linkers between the drug and the antibody, which may affect drug release if the conjugate is tightly bound to the antibody. The goal of this study is to design, synthesize, and evaluate ADCs that have site-specific conjugation, conformationally defined linkers, and enhanced antibody/drug ratios.

Synthesis and evaluation of site-specific antibody-drug conjugates using conformationally restricted linkers

245th National Meeting (2013)

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