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◆ ACS Omega2026-02-16· Chemistry

Site-Specific Glycan Conjugation Improves Stability and Efficacy of an Antibody–Drug Conjugates Bearing DXd as a Cytotoxic Payload

Shino Manabe, Shogo Senga, Shogo Iwamoto, Hikaru Yarita, Ryo Takahashi, Ai Mitani, Wataru Sumiyoshi, Asako Hoshinoo, Methanee Hiranyakorn, Takashi Kinoshita, Chihoko Yoshimura

原始摘要(英文原文)· Original abstract
High Resolution Image Download MS PowerPoint Slide This study developed a homogeneous ADC via site-specific conjugation of a potent antitumor agent, a camptothecin derivative, to the N -glycan in the Fc domain of an antibody, achieving a drug-to-antibody ratio (DAR) of 4. The resulting glycan-conjugated ADC exhibited improved thermal stability, reduced aggregation, and reduced premature payload release in human plasma. Despite utilizing the same antibody and payload, this glycan-linked ADC outperformed a clinically approved cysteine-conjugated homogeneous ADC (DAR 8) in vivo .
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Site-Specific Glycan Conjugation Improves Stability and Efficacy of an Antibody–Drug Conjugates Bearing DXd as a Cytotoxic Payload — 科研速览 Science Skim