Antibody-multidrug conjugate precursor and synthetic intermediate thereof

JPWO2023234427A5Pending Publication Date: 2026-06-12
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Applications
Filing Date
2023-06-02
Publication Date
2026-06-12

AI Technical Summary

Technical Problem

Current antibody-drug conjugates (ADCs) often face challenges in delivering multiple antitumor drugs effectively to cancer cells, with existing linkers lacking stability and hydrophilicity, which affects their pharmacokinetics and antitumor activity.

Method used

Development of an antibody-multi-drug conjugate (AMDC) with a branched linker modified with lactonyl and phosphoryl groups, enhancing stability and hydrophilicity, and the synthesis of conjugate precursors to facilitate the formation of stable Y-shaped AMDCs that exhibit improved pharmacokinetics and antitumor activity.

Benefits of technology

The modified linker and conjugate precursors enable the creation of AMDCs that demonstrate enhanced blood stability, high hydrophilicity, and effective antitumor activity in both in vitro and in vivo tests, showcasing improved drug delivery and efficacy.

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Abstract

Provided is a conjugate precursor for obtaining a more useful antitumor agent by further developing a conventional antibody-drug conjugate. Provided are: an antibody-multidrug conjugate precursor represented by general formula (I) (in the formula, the symbols have the meanings as defined in the specification) or a salt thereof; and a synthetic intermediate thereof or a salt thereof.
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