Automated synthesis of [89Zr]ZrCl(4), [89Zr]ZrDFOSquaramide-bisPh(PSMA) and [89Zr]ZrDFOSquaramide-TATE

Noor, A; Roselt, PD; McGowan, ER; Poniger, S; Wheatcroft, MP; Donnelly, PS

Author(s): Noor, A; Roselt, PD; McGowan, ER; Poniger, S; Wheatcroft, MP; Donnelly, PS;
Details: Publication Year 2024-05-08,Volume 9,Issue #1,Page 39
Journal Title: EJNMMI Radiopharmacy and Chemistry
Publication Type: Research article
Abstract: BACKGROUND: Automated [(89)Zr]Zr-radiolabeling processes have the potential to streamline the production of [(89)Zr]Zr-labelled PET imaging agents. Most radiolabeling protocols use [(89)Zr][Zr(ox)(4)](4-) as the starting material and oxalate is removed after radiolabeling. In some instances, radiolabeling with [(89)Zr]ZrCl(4) as starting material gives better radiochemical yields at lower reaction temperatures. In this work, a fully-automated process for production of [(89)Zr]ZrCl(4) is reported and its use for the synthesis of [(89)Zr]ZrDFOSq-bisPhPSMA and [(89)Zr]ZrDFOSq-TATE. RESULTS: A simple automated process for the isolation of [(89)Zr]ZrCl(4) by trapping [(89)Zr][Zr(ox)(4)](4-) on a bicarbonate-activated strong anion exchange cartridge followed by elution with 0.1 M HCl in 1 M NaCl was developed. [(89)Zr]ZrCl(4) was routinely recovered from [(89)Zr][Zr(ox)(4)](4-) in > 95% yield in mildly acidic solution of 0.1 M HCl in 1 M NaCl using a fully-automated process. The [(89)Zr]ZrCl(4) was neutralized with sodium acetate buffer (0.25 M) removing the requirement for cumbersome manual neutralization with strong base. The mixture of [(89)Zr]ZrCl(4) was used for direct automated radiolabeling reactions to produce [(89)Zr]Zr-DFOSquaramide-bisPhPSMA and [(89)Zr]ZrDFOSquaramide-TATE in 80-90% over all RCY in > 95% RCP. CONCLUSIONS: This method for the production of [(89)Zr]ZrCl(4) does not require removal of HCl by evaporation making this process relatively fast and efficient. The fully automated procedures for the production of [(89)Zr]ZrCl(4) and its use in radiolabeling are well suited to support the centralized and standardized manufacture of multiple dose preparations of zirconium-89 based radiopharmaceuticals.
Publisher: Springer Nature
Keywords: Automated synthesis; Radiopharmaceuticals; Zirconium-89; [89Zr]ZrCl4
Department(s): Cancer Imaging
Publisher's Version: https://doi.org/10.1186/s41181-024-00270-2
Open Access at Publisher's Site: https://doi.org/10.1186/s41181-024-00270-2
Terms of Use/Rights Notice: Refer to copyright notice on published article.

Creation Date: 2024-07-17 03:02:37

Last Modified: 2024-07-17 03:11:20