Side-by-side comparison of the two widely studied GRPR radiotracers, radiolabeled NeoB and RM2, in a preclinical setting.
GRPR
NeoB
Peptide receptor radionuclide therapy
Prostate cancer
RM2
Journal
European journal of nuclear medicine and molecular imaging
ISSN: 1619-7089
Titre abrégé: Eur J Nucl Med Mol Imaging
Pays: Germany
ID NLM: 101140988
Informations de publication
Date de publication:
Nov 2023
Nov 2023
Historique:
received:
28
04
2023
accepted:
24
07
2023
medline:
30
10
2023
pubmed:
16
8
2023
entrez:
16
8
2023
Statut:
ppublish
Résumé
NeoB and RM2 are the most investigated gastrin-releasing peptide receptor (GRPR)-targeting radiotracers in preclinical and clinical studies. Therefore, an extensive side-by-side comparison of the two radiotracers is valuable to demonstrate whether one has advantages over the other. Accordingly, this study aims to compare the in vitro and in vivo characteristics of radiolabeled NeoB and RM2 to guide future clinical studies. The stability of the radiolabeled GRPR analogs was determined in phosphate buffered saline (PBS), and commercially available mouse and human serum. Target affinity was determined by incubating human prostate cancer PC-3 cells with [ Both radiotracers demonstrated high stability in PBS and human serum, but stability in mouse serum decreased substantially over time. Moreover, both radiotracers demonstrated high GRPR affinity and specificity, but a higher uptake of [ Based on these findings, we conclude that the in vivo tumor-targeting capability of radiolabeled NeoB and RM2 is similar. Additional studies are needed to determine whether the differences observed in physiological organ uptakes, i.e., the pancreas, kidneys, and blood, result in relevant differences in organ absorbed doses when the radiotracers are applied for therapeutic purposes.
Identifiants
pubmed: 37584725
doi: 10.1007/s00259-023-06364-4
pii: 10.1007/s00259-023-06364-4
pmc: PMC10611828
doi:
Substances chimiques
Bombesin
PX9AZU7QPK
Receptors, Bombesin
0
Types de publication
Comparative Study
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
3851-3861Subventions
Organisme : NWO ZonMw Veni
ID : 09150161810061
Informations de copyright
© 2023. The Author(s).
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