Antibody conjugate drugs based on fluorinated diphenylethane payload and hydrophilic linker and preparation and application thereof
By designing antibody-drug conjugates with fluorodiphenyl ethane payloads and hydrophilic linkers, and utilizing linkers of polyethylene glycol and β-glucuronic acid units as well as secondary cyclized spacers, the problems of water solubility and release efficiency of fluorodiphenyl ethane toxins were solved, achieving stability and high-efficiency killing activity of the highly loaded drug.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- SHANGHAI INST OF TECH
- Filing Date
- 2026-05-12
- Publication Date
- 2026-07-17
AI Technical Summary
Fluorodiphenyl ethane cytotoxins are highly active but have extremely poor water solubility. Traditional linkers are difficult to use to prepare high-load drugs and have low release efficiency, leading to aggregation and precipitation problems.
Antibody-drug conjugates based on fluorodiphenyl ethane payloads and hydrophilic linkers are used. By introducing linkers containing polyethylene glycol and β-glucuronic acid units and combining them with secondary cyclized spacers, water solubility is improved and rapid release is achieved.
It significantly improved the water solubility and stability of the drug, solved the aggregation problem under high load, and ensured the efficient release of phenolic hydroxytoxin, exhibiting excellent cytotoxic activity and plasma stability.
Smart Images
Figure CN122399050A_ABST