PNU anthracycline substance-derived linker-load, pharmaceutical composition and application of PNU anthracycline substance-derived linker-load

By developing PNU anthracycline-derived linker-load compounds, the problems of toxicity limitations and pharmacokinetic control of anthracyclines in cancer chemotherapy were solved, achieving more efficient cancer cell delivery and release, and enhancing the anti-cancer effect.

CN120615015APending Publication Date: 2025-09-09默沙东有限责任公司
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Patent Information

Application Number
CN202380093031.3
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2023-04-19
Filing Date
2023-12-18
Publication Date
2025-09-09

AI Technical Summary

Technical Problem

The effectiveness of existing anthracyclines in cancer chemotherapy is limited by their toxicity, and there is room for improvement in the pharmacokinetic control and cancer cell delivery and release of antibody-drug conjugates.

Method used

A class of PNU anthracycline-derived linker-payload compounds was developed, which were combined with PEG units through maleimide- or sulfone-substituted pyridyl peptide linkers for the preparation of antibody-drug conjugates to improve drug delivery and release in cancer cells.

Benefits of technology

The delivery efficiency and release control of anthracyclines in cancer cells are improved, thereby enhancing the anti-cancer effect while reducing toxicity.

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Abstract

The present disclosure relates to linker-loadings, and pharmaceutically acceptable salts, solvates or stereoisomers thereof, comprising the structure of Formula I: # imgabs0. The disclosure also relates to pharmaceutical compositions comprising these compounds and the use of these compounds, intermediates and compositions thereof in the prevention or treatment of cancer and / or tumors.
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