FAPI theranostic compounds assembled with tetrazine ligation

FAP inhibitor ligands assembled via tetrazine ligation address the challenge of short tumor retention by enhancing tumor accumulation and therapeutic efficacy, offering improved radiopharmaceuticals for targeted cancer therapy.

WO2026037958A1 Publication Date: 2026-02-19TETRAKIT TECHNOLOGIES APS
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Patent Information

Application Number
PCT/EP2025/073476
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-08-15
Filing Date
2025-08-15
Publication Date
2026-02-19

AI Technical Summary

Technical Problem

Existing FAP-based radiopharmaceuticals face challenges in achieving prolonged tumor residence time and effective therapeutic efficacy due to short tumor retention times, especially when labeled with therapeutic radiometals, and radiohalogens like iodine-131 exhibit suboptimal properties with high liver and gastrointestinal tract excretion.

Method used

Development of FAP inhibitor ligands assembled through tetrazine ligation, incorporating a linker and IsoF-TCO, allowing for quick and efficient radiolabeling with radiohalogens or radiometals, enabling higher tumor accumulation and modularity for optimizing pharmacokinetic properties.

Benefits of technology

The FAP inhibitor ligands demonstrate improved tumor accumulation and therapeutic efficacy, surpassing previous compounds like [111In]In-DOTAGA.Glu.(FAPi)2, with enhanced tumor retention and reduced off-target accumulation.

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Abstract

The present invention relates to fibroblast activation protein (FAP) - based ligands assembled through tetrazine ligation and their use in radiotherapy and imaging. The FAP inhibitor (FAPi) ligand compounds provided herein comprises a FAP targeting moiety, a linker, an IsoF-TCO and a radiolabeled tetrazine. The FAPi targeting compounds are possessing advantageous pharmacokinetic properties and enable quick and efficient modifications of the radiopharmaceuticals allowing a fast renal excretion and reduced liver accumulation.
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