Combination of carbonic anhydrase ix ligands

A dual-agent approach with a first agent having a larger KD than the radiolabeled second agent competes for CA IX binding, reducing healthy tissue accumulation and maintaining therapeutic efficacy in CA IX-positive diseases.

WO2026125277A1 Publication Date: 2026-06-18DEBIOPHARM INTERNATIONAL SA

Patent Information

Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
DEBIOPHARM INTERNATIONAL SA
Filing Date
2025-12-08
Publication Date
2026-06-18

AI Technical Summary

Technical Problem

Existing radiolabeled carbonic anhydrase IX (CA IX) ligands accumulate in healthy tissues, leading to adverse side effects such as hemorrhagic gastritis and inflammation, limiting their therapeutic efficacy in cancer treatment.

Method used

A combination of a first agent and a second agent, both capable of binding to CA IX, where the second agent is radiolabeled, is administered to reduce accumulation in healthy tissues by competitive binding, using a first agent with a larger equilibrium dissociation constant (KD) to minimize healthy tissue uptake.

🎯Benefits of technology

The combination reduces adverse side effects in healthy tissues while maintaining therapeutic efficacy in CA IX-positive diseases by minimizing radiolabeled agent accumulation, enhancing tumor uptake and diagnostic imaging.

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Abstract

The present invention relates to a combination of agents and its use in targeted radionuclide therapy. The present invention also relates to the use of the combination in methods of diagnosing, imaging and / or treating CA IX-positive diseases, e.g., tumors or cancers.
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