Antibody-drug conjugate and use thereof

By designing antibody-drug conjugates targeting CEACAM5 and linking them to topoisomerase I inhibitors or camptothecin derivatives using specific linkers, the cytotoxicity and stability issues of existing CEACAM5-targeting drugs have been resolved, resulting in more efficient and safer tumor treatment.

WO2026158363A1PCT designated stage Publication Date: 2026-07-30CSPC MEGALITH BIOPHARMACEUTICAL CO LTD
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Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
CSPC MEGALITH BIOPHARMACEUTICAL CO LTD
Filing Date
2026-01-21
Publication Date
2026-07-30

AI Technical Summary

Technical Problem

Existing CEACAM5-targeting antibody-drug conjugates have issues with cytotoxicity, stability, and safety, resulting in less than expected efficacy and a narrow therapeutic window, making them difficult to effectively treat tumors that overexpress CEACAM5.

Method used

An antibody-drug conjugate was designed, the structure of which consists of an antibody targeting CEACAM5 or its antigen-binding fragment linked to a topoisomerase I inhibitor or camptothecin derivative through a specific linker. The drug-antibody conjugate ratio (DAR) is controlled between 1 and 12. The antibody-drug conjugate with higher stability and safety is prepared by using inter-light and heavy chain reducing disulfide bonds or enzymatic conjugation techniques.

Benefits of technology

It improved the stability and safety of antibody-drug conjugates, expanded the therapeutic window, reduced toxicity, and significantly enhanced the tumor-suppressive effect against CEACAM5-overexpressing tumors.

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Abstract

Provided are an antibody-drug conjugate and use thereof, in particular an antibody-drug conjugate targeting CEACAM5.
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