Fibroblast activation protein inhibitor

By designing the compound XmYnZp to bind to radionuclides, the enrichment and retention of tumor sites is enhanced, and the problem of short retention time of existing FAPI small molecule drugs in tumor tissues is solved, achieving more efficient tumor treatment effects.

WO2025167951A1 Publication Date: 2025-08-14BOOMRAY PHARMACEUTICALS CO LTD
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Patent Information

Application Number
PCT/CN2025/075914
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-08-09
Filing Date
2025-02-06
Publication Date
2025-08-14

AI Technical Summary

Technical Problem

The existing FAPI small molecule radioactive drugs have a short retention time in tumor tissue, resulting in low tumor absorption rate, limiting their application in tumor treatment.

Method used

A compound XmYnZp is designed with a specific chemical structure for binding to radionuclides, enhancing enrichment and retention at tumor sites, and achieving targeted treatment by specific binding to tumor cells with high expression of fibroblast activation protein (FAP).

Benefits of technology

It improves the drug retention time in tumor tissue, enhances the tumor treatment effect, improves the tumor absorption rate, and improves the treatment effect.

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Abstract

The present invention relates to a fibroblast activation protein inhibitor, a pharmaceutical composition comprising the compound, and a use thereof in the diagnosis or treatment of fibroblast activation protein overexpression diseases.
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