The goal of this research was to investigate the feasibility of Cu labeling in prostate-specific membrane antigen imaging and therapy (PSMA I&T) for PSMA positron emission tomography (PET) imaging and biodistribution evaluation. PSMA I&T was labeled with Cu, and stability in human and mouse sera was evaluated. Prostate cancer cell lines were used for specific uptake assays (22RV1 for PSMA-positive, PC-3 for -negative). Both PC-3 and 22RV1 cells were transplanted into the left and right thighs in a mouse for PET/computed tomography (CT) imaging. Biodistribution was performed using 22RV1 tumor models. Labeling yield (decay corrected) of Cu-PSMA I&T was more than 95% compared to the free Cu peak. The serum stability of Cu-PSMA I&T was maintained at more than 90% until 60 h. Regarding the specific binding of Cu-PSMA I&T was 7.5-fold higher to 22RV1 cells than PC-3 cells ( < 0.001). On PET/CT imaging, more specific Cu-PSMA I&T uptake was observed to 22RV1 tumors than to PC-3 tumors. In the PSMA blocking study using 2-phosphonomethoxypropyl adenine (2-PMPA), the Cu-PSMA I&T signal significantly decreased in the 22RV1 tumor region. In the biodistribution study, the kidney uptake was the highest among all organs at 2 h (52.6 ± 20.8%ID/g) but sharply decreased at 24 and 48 h. Also, the liver showed similar uptake over time (range, 10-12%ID/g). On the contrary, Cu-PSMA I&T uptake of the tumors increased with time and peaked at 48 h (5.6 ± 0.1%ID/g). PSMA I&T labeled with Cu showed the feasibility of the PSMA specific PET imaging through and studies. Furthermore, Cu-PSMA I&T might be considered as the candidate of future clinical trial.
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http://dx.doi.org/10.1089/cbr.2020.4189 | DOI Listing |
J Nucl Med
September 2024
Division of Radiopharmaceutical Chemistry, University Hospital Basel, Basel, Switzerland;
The demand for PET tracers that target prostate-specific membrane antigen (PSMA) continues to increase. Meeting this demand with approved Ga- and F-labeled PSMA tracers is challenging outside of major urban centers. This is because the short physical half-life of these radionuclides makes it necessary to produce them near their sites of usage.
View Article and Find Full Text PDFNucl Med Biol
February 2024
Department of Oncology, Cross Cancer Institute, University of Alberta, Edmonton, Alberta T6G 1Z2, Canada; Cancer Research Institute of Northern Alberta, University of Alberta, Edmonton, Alberta T6G 2E1, Canada. Electronic address:
Introduction: Copper-64 (Cu, t = 12.7 h) is a positron emitter well suited for theranostic applications with beta-emitting Cu for targeted molecular imaging and radionuclide therapy. The present work aims to evaluate the radionuclidic purity and radiochemistry of Cu produced via the Zn(p,nα)Cu nuclear reaction.
View Article and Find Full Text PDFPharmaceuticals (Basel)
April 2022
Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), Key Laboratory for Research and Evaluation of Radiopharmaceuticals (National Medical Products Administration), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing 100142, China.
Prostate-specific membrane antigen (PSMA) is an ideal target for the diagnosis and treatment of prostate cancer. Due to the short half-life in blood, small molecules/peptides are rapidly cleared by the circulatory system. Prolonging the half-life of PSMA probes has been considered as an effective strategy to improve the tumor detection.
View Article and Find Full Text PDFCancers (Basel)
November 2021
Department of Radiation Oncology, IRCCS Regina Elena National Cancer Institute, 00144 Rome, Italy.
Background: We aimed assess the detection rate (DR) of positron emission tomography/computed tomography with two novel tracers in patients referred for salvage radiotherapy (sRT) with a presumed local recurrence at multiparametric magnetic resonance (mpMR) after radical prostatectomy (RP).
Methods: The present prospective study was conducted at a single institution between August 2017 and June 2020. Eligibility criteria were undetectable PSA after RP; subsequent biochemical recurrence (two consecutive PSA rises to 0.
Asia Ocean J Nucl Med Biol
January 2021
Institute of Nuclear Medicine with PET-Center, Klinik Ottakring, Vienna, Austria.
Prostate cancer is considered to be the most common solid cancer affecting men worldwide and leading to a significant morbidity and mortality. Metastases are usually seen in bone or lymph nodes. For recurrent disease, PET imaging with Ga-PSMA-11 (also known as HBED-CC, Glu-urea-Lys(Ahx)-HBED-CC, and PSMA-HBED-CC) is widely used.
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