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Innovations in linker design are focused on multiple issues ranging from serum stability to mechanism of release to drug to antibody ratio (dar) To date, 17 adcs have received regulatory approval for treating both hematologic and solid tumors As linkers become increasingly sophisticated, more emphasis is being placed on the methods of bioconjugation between linker and antibody, with the goal of producing homogeneous adc populations.
An antibody is linked to a small molecule via a covalent tether An ideal linker should be stable in the circulatory system and release the cytotoxic payload specifically in the tumor Linker tethering payload to antibody is vital for adc
This review provides an overview of linkers of 17 approved adcs and recent innovations in linker design, focusing on drug release triggers, bioconjugation strategies, the impact of spacers on hydrophilicity, traceless drug release, and linker architecture, as well as a discussion of the bystander effect, offering insights for the rational.
Target, antibody, linker, payload, and conjugation method.
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