Heterodimeric compounds targeting fap and mitochondria and uses thereof

CN122255179APending Publication Date: 2026-06-23BEIJING NORMAL UNIVERSITY
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
BEIJING NORMAL UNIVERSITY
Filing Date
2025-12-31
Publication Date
2026-06-23

AI Technical Summary

Technical Problem

Existing tumor molecular probes targeting FAP have insufficient uptake and retention in tumors, making it difficult to meet the needs of early tumor diagnosis and treatment. Furthermore, the application of mitochondrial-targeting compounds in tumors has not been fully developed.

Method used

A heterodimeric compound targeting FAPI and mitochondria was designed. By introducing a hydrazine nicotinamide (HYNIC) group into the FAPI and TPP+ pharmacophore groups and using a 99mTc labeling strategy, a highly stable and targeted radioactive molecular probe was prepared for the diagnosis and efficacy evaluation of various tumors.

Benefits of technology

It achieves high uptake and good retention in tumors, significantly improves the tumor/non-target ratio, and demonstrates excellent tumor imaging performance, making it suitable for early diagnosis and efficacy evaluation of various tumors.

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Abstract

The present application relates to the field of radiopharmaceutical chemistry and clinical nuclear medicine technology, and particularly relates to a kind of FAP and mitochondrion targeted heterodimer compound and application thereof.The radioactive preparation obtained by labeling the FAP and mitochondrion targeted heterodimer compound with radionuclide is simple to prepare, has high radiochemical purity, good stability, has very high uptake and high target-to-non-target ratio in the tumor site of tumor-bearing mice, has good tumor retention, and specifically binds to FAP in tumor, so it is a new type of tumor radioactive drug with popularization and application value.
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