Lanthanide-based contrast agents having improved stability and methods for their production and purification

By formulating lanthanide metal complexes with macrocyclic chelators and employing specific purification and stabilization methods, the stability and toxicity issues of current MRI contrast agents are addressed, resulting in highly effective and safe imaging agents.

WO2025034668A9 Publication Date: 2025-04-03INVENTURE LLC
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Patent Information

Application Number
PCT/US2024/040973
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2023-08-04
Filing Date
2024-08-05
Publication Date
2025-04-03

AI Technical Summary

Technical Problem

Current MRI contrast agents based on lanthanide chelate complexes, such as gadolinium, face issues with stability and toxicity due to the release of free lanthanide ions, which can be toxic and require repeated administration.

Method used

The development of pharmaceutical formulations of lanthanide metal complexes with macrocyclic chelators that are free or substantially free of excess water molecules and metastable complexes, using methods that involve adding DOTA to purified water, stirring and heating, incremental addition of lanthanide oxide, and purification processes involving semipermeable membranes and meglumine addition to lock the TSA’ structure.

Benefits of technology

The resulting formulations achieve improved stability and reduced toxicity, with greater than 95% of gadolinium-DOTA complexes possessing a TSA’ structure and no coordinated water, leading to enhanced safety and efficacy as MRI contrast agents.

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Abstract

The present disclosure relates to pharmaceutical formulations of contrast agents used in magnetic resonance imaging (MRI) and methods of making and purifying the same. More specifically, disclosed are such pharmaceutical formulations of chelate complexes with lanthanide metal ions, such as gadolinium ions, as well as methods for obtaining and purifying the same. In particular, the pharmaceutical formulations are free or substantially free of water molecules coordinated with the lanthanide metal chelate complexes and provide pharmaceutical compositions that are more stable and release less lanthanide ion, specifically gadolinium ion, into the human body when injected as MRI contrast agents as compared to other typically used MRI contrast agents.
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