Towards Optimal Automated 68 Ga-Radiolabeling Conditions of the DOTA-Bisphosphonate BPAMD Without Pre-Purification of the Generator Eluate.

Autor: Souche C; Nuclear Medicine Department, Institut Régional du Cancer de Montpellier (ICM), Université de Montpellier, Montpellier, France., Fouillet J; Nuclear Medicine Department, Institut Régional du Cancer de Montpellier (ICM), Université de Montpellier, Montpellier, France., Rubira L; Nuclear Medicine Department, Institut Régional du Cancer de Montpellier (ICM), Université de Montpellier, Montpellier, France., Donzé C; Nuclear Medicine Department, Institut Régional du Cancer de Montpellier (ICM), Université de Montpellier, Montpellier, France., Sallé A; Nuclear Medicine Department, Institut Régional du Cancer de Montpellier (ICM), Université de Montpellier, Montpellier, France., Dromard Y; Institut de Recherche en Cancérologie de Montpellier (IRCM), INSERM U1194, Institut Régional du Cancer de Montpellier (ICM), Université de Montpellier, Montpellier, France., Deshayes E; Nuclear Medicine Department, Institut Régional du Cancer de Montpellier (ICM), Université de Montpellier, Montpellier, France.; Institut de Recherche en Cancérologie de Montpellier (IRCM), INSERM U1194, Institut Régional du Cancer de Montpellier (ICM), Université de Montpellier, Montpellier, France., Fersing C; Nuclear Medicine Department, Institut Régional du Cancer de Montpellier (ICM), Université de Montpellier, Montpellier, France.; IBMM, Université de Montpellier, CNRS, ENSCM, Montpellier, France.
Jazyk: angličtina
Zdroj: Journal of labelled compounds & radiopharmaceuticals [J Labelled Comp Radiopharm] 2024 Nov 20. Date of Electronic Publication: 2024 Nov 20.
DOI: 10.1002/jlcr.4128
Abstrakt: DOTA-functionalized bisphosphonates can be useful tools for PET imaging of bone metastases when radiolabeled with 68 Ga. Moreover, the versatility of DOTA allows the complexation of radiometals with therapeutic applications (e.g., 177 Lu), positioning these bisphosphonates as attractive theranostic agents. Among these molecules, BPAMD is a compound whose radiolabeling with 68 Ga has already been described, but only through manual methods. Thus, a fully automated protocol for 68 Ga radiolabeling of BPAMD on the GAIA® ± LUNA® synthesis module was designed, and a thorough study of the radiolabeling conditions was undertaken. [ 68 Ga]Ga-BPAMD was produced in good radiochemical purity (> 93%) and high radiochemical yield (> 91%) using 0.3 M HEPES buffer. The nature of the reaction vessel showed no significant effect on the radiolabeling outcome. Similarly, addition of an antiradiolysis compound to the reaction medium did not significantly improve the already excellent stability of [ 68 Ga]Ga-BPAMD over time. The radiolabeled product obtained by automated synthesis was evaluated in vivo in healthy mice and confirmed high accumulation in the joints and along the backbone.
(© 2024 The Author(s). Journal of Labelled Compounds and Radiopharmaceuticals published by John Wiley & Sons Ltd.)
Databáze: MEDLINE
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