Fibroblast activation protein targeted compounds and use thereof

Radiopharmaceuticals targeting FAP, designed as Y-L-X conjugates, address the need for effective cancer and disease treatment by providing both imaging and therapeutic capabilities through targeted radionuclide delivery.

WO2026127965A1 Publication Date: 2026-06-18PERSPECTIVE THERAPEUTICS INC

Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
PERSPECTIVE THERAPEUTICS INC
Filing Date
2024-12-12
Publication Date
2026-06-18

AI Technical Summary

Technical Problem

There is a need for alternative radiopharmaceuticals that can be safely and effectively used for the imaging and/or treating of cancer and other disease states, particularly targeting fibroblast activation protein (FAP) which is highly upregulated in various cancers and disease conditions.

Method used

Development of radiopharmaceuticals designed as Y-L-X conjugates, where Y is a radionuclide, L is a molecular linker, and X is a targeting molecular structure that binds to FAP, enabling imaging and therapeutic applications by utilizing radionuclides that emit gamma rays, beta particles, or alpha particles.

🎯Benefits of technology

The developed radiopharmaceuticals provide effective imaging and treatment options for cancer and other diseases by targeting FAP, with specific examples demonstrating high binding affinity, metabolic stability, and tumor uptake.

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Abstract

The present invention relates to a composition comprising fibroblast activation protein alpha (FAP)-targeting conjugate comprising Formula (I): Y-L-X, wherein Y is a chelator or cytotoxic drug, L is a linker, and X comprises a binding peptide sequence of AA1-AA2-AA3-AA4-AA5-AA6-AA7 which may be in the form of a cyclic peptide, wherein the composition further contains a radioprotectant and / or is in a lyophilized form.
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