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.
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
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.
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.
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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