Labeled fibroblast activation protein inhibitor and use thereof

By targeting fibroblast activating protein (FAP) with compounds that chelate with radionuclides, the limited therapeutic effects of FAP targeting in existing technologies have been addressed, enabling efficient diagnosis and treatment of diseases with upregulated FAP expression.

WO2026149382A1PCT designated stage Publication Date: 2026-07-16TIANJIN HENGRUI MEDICINE CO LTD +1

Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
TIANJIN HENGRUI MEDICINE CO LTD
Filing Date
2026-01-06
Publication Date
2026-07-16

AI Technical Summary

Technical Problem

Existing therapies targeting fibroblast activating protein (FAP) have limited effectiveness in cancer and other diseases, necessitating the development of more effective inhibitors and diagnostic tools.

Method used

A compound or a pharmaceutically acceptable salt thereof is provided for use in the preparation of medicaments for the diagnosis or treatment of diseases by complexation with a radionuclide, particularly by complexation with 161Tb or 212Pb for targeting diseases with upregulated expression of fibroblast activating protein (FAP).

Benefits of technology

It has achieved efficient diagnosis and treatment of diseases with upregulated FAP expression, especially imaging and treatment effects in tumors, inflammatory diseases, cardiovascular diseases and fibrotic diseases.

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Abstract

Provided are a labeled fibroblast activation protein inhibitor and a use thereof. Specifically, the present disclosure provides a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and the use thereof in diagnosing or treating diseases associated with fibroblast activation protein, such as tumors and cancers. Each substituent is respectively as defined in the description.
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