Linker, antibody-drug conjugate, and preparation method therefor

Through the design of new linker-antibody conjugates, the problems of insufficient stability and pharmacokinetic properties of ADC were solved, and efficient delivery and drug release of antibody drugs at the tumor site were achieved, thereby enhancing the therapeutic effect.

WO2025209482A1 Publication Date: 2025-10-09FUDAN UNIVERSITY
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Patent Information

Application Number
PCT/CN2025/086645
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-09-27
Filing Date
2025-04-01
Publication Date
2025-10-09

AI Technical Summary

Technical Problem

Existing antibody-drug conjugates (ADCs) have deficiencies in stability and pharmacokinetic properties, resulting in uneven distribution in the body and poor efficacy, especially aggregation and sedimentation caused by traditional linkers and rapid liver metabolism.

Method used

A new type of linker, containing a linker group with a specific structure and a glucose group, is used to form an antibody-drug conjugate (ADC) by coupling with an antibody to increase the drug loading capacity and optimize the physicochemical and pharmacokinetic properties of the ADC.

Benefits of technology

It achieves efficient delivery and drug release of antibody-drug conjugates in tumor target cells, increases drug accumulation at the tumor site, enhances the therapeutic effect, and controls the drug exposure and half-life in plasma.

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Abstract

The present invention provides a linker, an antibody-drug conjugate, and a preparation method therefor. The drug linker of the present invention has good solubility, and can greatly improve the water solubility of existing small molecule compounds and improve the stability and uniformity of the conjugate after being conjugated to an antibody.
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