Method for purifying radionuclide-labeled drugs

The use of a strongly acidic cation exchange resin column with DOTA or NOTA and zirconium enables the separation of labeled and unlabeled peptides based on retention time differences, addressing the purification challenge and improving the efficacy of radionuclide-labeled peptides for medical applications.

JP7868523B2Active Publication Date: 2026-06-02JFE ENGINEERING CORP
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
JFE ENGINEERING CORP
Filing Date
2023-02-08
Publication Date
2026-06-02

AI Technical Summary

Technical Problem

Existing methods for purifying radionuclide-labeled peptides fail to distinguish between labeled and unlabeled peptides, leading to the adsorption of both on hydrophobic columns, which hinders the use of unlabeled peptides as radiodiagnostic or internal radiation therapy agents.

Method used

A method utilizing a strongly acidic cation exchange resin column to separate radionuclide-labeled peptides by exploiting the difference in retention times between labeled and unlabeled peptides, achieved through the use of a trivalent chelating agent like DOTA or NOTA and a tetravalent radionuclide such as zirconium, forming a +1-valent complex.

Benefits of technology

Effectively removes unlabeled peptides, allowing for the separation and purification of radionuclide-labeled peptides, enhancing their suitability for diagnostic and therapeutic applications.

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Abstract

To provide methods for separating peptides not labeled with a radionuclide from radionuclide-labeled agents.SOLUTION: Disclosed is a method for purifying an agent labeled with a radionuclide from a solution where the agent comprises a chelator that forms a complex with the radionuclide. The method comprises passing the solution through a column packed with a strongly acidic cation exchange resin to extract the radionuclide-labeled agent on the basis of a difference of the retention times to the column. The radionuclide is a tetravalent nuclide, i.e., zirconium. The chelator is a trivalent chelator including, DOTA or NOTA. The strongly acidic cation exchange resin comprises sulfonic acid groups as a functional group. The labeled agent is a prostate specific antigen binding agent, a somatostatin receptor binding agent, or a fibroblast activation protein binding agent.SELECTED DRAWING: Figure 1
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