Eribulin derivative and antibody-drug conjugate thereof, and medical use thereof
Eribulin derivatives with modified structures and targeted linkers in ADCs address toxicity issues, enhancing therapeutic efficacy and specificity for cancer treatment.
AU2025265434A1Pending Publication Date: 2026-07-23SHANGHAI PHRONTLINE BIOPHARMA CO LTD +1
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Patent Information
- Application Number
- AU2025265434
- Authority / Receiving Office
- AU · AU
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2024-04-28
- Filing Date
- 2025-04-21
- Publication Date
- 2026-07-23
AI Technical Summary
Technical Problem
Existing antibody-drug conjugates (ADCs) face issues of toxicity due to linker instability and non-specific endocytosis, leading to off-target toxicities and reduced therapeutic efficacy.
Method used
Development of eribulin derivatives with modified structures and an antibody-drug conjugate using appropriate linkers to enhance tumor targeting specificity and reduce toxicity, resulting in a larger therapeutic window.
Benefits of technology
The eribulin derivative-antibody conjugate achieves improved therapeutic efficiency with reduced toxicity and enhanced tumor targeting, expanding the therapeutic window for cancer treatment.
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Abstract
The present application relates to the technical field of medicines, and in particular to an eribulin derivative and an antibody-drug conjugate (ADC) thereof, and a medical use thereof. In the present application, a series of derivatives with good tumor suppression effects are synthesized by modifying eribulin, and have lower toxicity and a larger therapeutic window than that of eribulin; and then the the eribulin derivative and an antibody are made into an ADC by means of an appropriate linker, and the therapeutic efficiency of the eribulin derivative is improved using the targeting specificity of the antibody.
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