Antibody-drug conjugates containing trabectedin and lurubinectedin derivatives

Novel trabectedin and lurubinectedin derivatives, used in antibody-drug conjugates, address the limitations of existing ADCs by enhancing cytotoxicity against ovarian, gastric, and breast cancer cells, offering improved therapeutic efficacy.

JP2026510365APending Publication Date: 2026-04-02AXCYNSIS THERAPEUTICS PTE LTD
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Filing Date
2023-10-24
Publication Date
2026-04-02

AI Technical Summary

Technical Problem

There is a need for alternative or improved cytotoxic compounds that can be used both as direct anticancer drugs and as payloads in antibody-drug conjugates, as existing ADCs face challenges in development due to the complexity of payloads and linkers, and there has been limited progress in enhancing the medical applications of trabectedin and lurubinectedin derivatives.

Method used

Development of novel trabectedin and lurubinectedin derivatives, including specific compounds represented by formulas (I), (VII), and (XIII), which are used as payloads in antibody-drug conjugates, specifically with antibodies like sirumutuzumab, sacituzumab, and trastuzumab, to target cancer cells effectively.

Benefits of technology

The novel derivatives exhibit improved in vitro potency against tumor cell lines, including ovarian, gastric, and breast cancer cells, with enhanced cytotoxicity when used alone and in antibody-drug conjugates, demonstrating potential as potent therapeutic agents for these cancers.

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Abstract

The present invention relates to novel trabectedin and lurubinectedin derivatives, corresponding antibody-drug conjugates, and methods for preparing antibody-drug conjugates. The present invention further relates to pharmaceutical dosage forms comprising novel trabectedin or lurubinectedin derivatives or corresponding antibody-drug conjugates. Furthermore, the present invention relates to novel trabectedin and lurubinectedin derivatives, corresponding antibody-drug conjugates, and corresponding pharmaceutical dosage forms for use as pharmaceuticals or in the treatment of specific types of cancer.
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Citation Information

Patent Citations

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    WO2011147828A1

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