Preclinical Comparison of Al18F- and 68Ga-Labeled Gastrin-Releasing Peptide Receptor Antagonists for PET Imaging of Prostate Cancer

@article{Chatalic2014PreclinicalCO,
  title={Preclinical Comparison of Al18F- and 68Ga-Labeled Gastrin-Releasing Peptide Receptor Antagonists for PET Imaging of Prostate Cancer},
  author={Kristell L.S. Chatalic and Gerben M. Franssen and W. M. van Weerden and William J. Mcbride and Peter Laverman and Erik de Blois and Bouchra Hajjaj and Luc Brunel and David M. Goldenberg and Jean-Alain Fehrentz and J. Martinez and Otto C Boerman and Marion de Jong},
  journal={The Journal of Nuclear Medicine},
  year={2014},
  volume={55},
  pages={2050 - 2056}
}
Gastrin-releasing peptide receptor (GRPR) is overexpressed in human prostate cancer and is being used as a target for molecular imaging. In this study, we report on the direct comparison of 3 novel GRPR-targeted radiolabeled tracers: Al18F-JMV5132, 68Ga-JMV5132, and 68Ga-JMV4168 (JMV5132 is NODA-MPAA-βAla-βAla-[H-d-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2], JMV4168 is DOTA-βAla-βAla-[H-d-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2], and NODA-MPAA is 2-[4-(carboxymethyl)-7-{[4-(carboxymethyl)phenyl… Expand
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References

SHOWING 1-10 OF 36 REFERENCES
Bombesin Antagonist–Based Radioligands for Translational Nuclear Imaging of Gastrin-Releasing Peptide Receptor–Positive Tumors
TLDR
The promising preclinical results warrant clinical translation of these probes for SPECT and PET of GRPr-positive tumors, and the chelators do influence the affinity, antagonistic potency, and pharmacokinetics of the conjugates. Expand
PET of Tumors Expressing Gastrin-Releasing Peptide Receptor with an 18F-Labeled Bombesin Analog
TLDR
A NotA-conjugated bombesin derivative, NOTA-8-Aoc-BBN(7-14)NH2, could be labeled rapidly and efficiently with 18F using a 1-pot, 1-step method and demonstrated GRPR-binding specificity, which was demonstrated by reduced tumor uptake of radiolabeled NOTA. Expand
In Vitro and In Vivo Evaluation of a 18F-Labeled High Affinity NOTA Conjugated Bombesin Antagonist as a PET Ligand for GRPR-Targeted Tumor Imaging
TLDR
The initial biological results suggest that [18F]AlF-NOTA-P2-RM26 is a promising candidate for PET imaging of GRPR in vivo. Expand
Synthesis and characterization of a high-affinity NOTA-conjugated bombesin antagonist for GRPR-targeted tumor imaging.
TLDR
The antagonistic bombesin analog NOTA-PEG2-d-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2 (NOTA- P2-RM26) is a promisindg candidate for prostate cancer imaging using PET and SPECT/CT. Expand
In Vivo Imaging of Prostate Cancer Using [68Ga]-Labeled Bombesin Analog BAY86-7548
TLDR
BAY86-7548 PET/CT is a promising molecular imaging technique for detecting intraprostatic prostate cancer and has a sensitivity, specificity, and accuracy of 88, 81, and 83%, respectively, for detection of primary PCa and sensitivity for metastatic lymph nodes using histology as gold standard. Expand
A Comparative Study of Radiolabeled Bombesin Analogs for the PET Imaging of Prostate Cancer
TLDR
The high-stability, efficient tumor uptake and optimal pharmacokinetic properties highlight 18F-AlF-NODAGA-RM1 as a probe with great potential and clinical application for the PET imaging of prostate cancer. Expand
Radiolabeled somatostatin receptor antagonists are preferable to agonists for in vivo peptide receptor targeting of tumors
TLDR
Somatostatin antagonist radiotracers are preferable over agonists for the in vivo targeting of sst3- or sst2-expressing tumors, and antagonists for other peptide receptors need to be evaluated in nuclear oncology as a result of this paradigm shift. Expand
Gastrin releasing peptide receptor-directed radioligands based on a bombesin antagonist: synthesis, (111)in-labeling, and preclinical profile.
Novel bombesin (BBN) antagonists were synthesized by coupling the chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) to H-d-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2 (JMV594)Expand
Development of a potent DOTA-conjugated bombesin antagonist for targeting GRPr-positive tumours
TLDR
A new conjugate, RM2, with the chelator DOTA coupled to D-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-Leu-NH2 via the cationic spacer 4-amino-1-carboxymethyl-piperidine is described for labelling with radiometals such as 111In and 68Ga. Expand
New lyophilized kit for rapid radiofluorination of peptides.
TLDR
It is indicated that (18)F-labeled peptides can be reproducibly prepared as stable Al-F complexes with good radiochemical yield and high specific activity using a simple, one-step, lyophilized kit followed by a rapid purification by SPE that provides the (18]F-peptide ready for patient injection within 30 min. Expand
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