Labeling precursors with squaric acid coupling

By designing labeled precursors with chelating agents or fluorinated groups and connecting with target vectors through linker and spacer, the problem of low marker selectivity and accumulation efficiency in the prior art is solved, and efficient binding and low radiation exposure to tumor markers are achieved.

JP7653082B2Active Publication Date: 2025-03-28SCV SPEZIAL CHEMIKALIEN VERTRIEB GMBH
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Patent Information

Application Number
JP2021547891
Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Priority Date
2018-10-24
Filing Date
2019-10-21
Publication Date
2025-03-28
Estimated Expiration
2039-10-21

AI Technical Summary

Technical Problem

Existing tumor markers are difficult to achieve high selectivity and efficient accumulation in tumor cells during diagnosis and treatment, and there is also the problem of excessive radiation dose to healthy tissues.

Method used

A labeled precursor with chelating agents or fluorinated groups was designed to improve the biological and radioactive properties of the marker by linking the target vector to the chelating agents or fluorinated groups.

Benefits of technology

High selective binding of tumor markers such as PSMA, FAP and FPPS has been achieved, which improves tumor accumulation efficiency and reduces radiation exposure to healthy tissues.

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Abstract

The present invention provides 44 Sc, 47 Sc, 55 Co, 62 Cu, 64 Cu, 67 Cu, 66 Ga, 67 Ga, 68 Ga, 89 Zr, 86 Y, 90 Y, 90 Nb, 99 mTc, 111 ln, 135 Sm, 140 Pr, 159 Gd, 149 Tb, 160 Tb, 161 Tb, 165 Er, 166 Dy, 166 Ho, 175 Yb, 177 Lu, 186 Re, 188 Re, 213 Bi and 225 Ac, or 18 F, 131 I or 211 The present invention relates to a marking precursor comprising a chelating agent or fluorinated group for radiolabeling with At and one or two biological targeting vectors coupled to the chelating agent or fluorinated group via one or more squaric acid groups, as represented by formula (I): TIFF2022509385000043.tif49155
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