Exo-Cleavable Linkers: Enhancing Stability and Therapeutic Efficacy in Antibody-Drug Conjugates

Exo-Cleavable Linkers: Enhancing Stability and Therapeutic Efficacy in Antibody-Drug Conjugates

Customized drug delivery systems are essential for precision medicine, with antibody-drug conjugates (ADCs) representing a pivotal approach that integrates cytotoxic payloads with monoclonal antibodies (mAbs) through sophisticated chemical linkers. However, optimizing ADC stability while achieving c...

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Veröffentlicht in:Journal of Synthetic Organic Chemistry, Japan Japan, 2024/11/01, Vol.82(11), pp.1117-1124
Hauptverfasser: Watanabe, Tomohiro, Fujii, Tomohiro, Matsuda, Yutaka
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container_title Journal of Synthetic Organic Chemistry, Japan
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creator Watanabe, Tomohiro
Fujii, Tomohiro
Matsuda, Yutaka
description Customized drug delivery systems are essential for precision medicine, with antibody-drug conjugates (ADCs) representing a pivotal approach that integrates cytotoxic payloads with monoclonal antibodies (mAbs) through sophisticated chemical linkers. However, optimizing ADC stability while achieving controlled payload release remains challenging. The FDA-approved valine-citrulline (Val-Cit) linker commonly used in ADCs, suffers from issues such as hydrophobicity-induced aggregation, limited drug-antibody ratio (DAR), and premature payload release.
doi_str_mv 10.5059/yukigoseikyokaishi.82.1117
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title Exo-Cleavable Linkers: Enhancing Stability and Therapeutic Efficacy in Antibody-Drug Conjugates
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