| Title |
Synthesis and preclinical evaluation of an Al18F radiofluorinated GLU-UREA-LYS(AHX)-HBED-CC PSMA ligand
|
|---|---|
| Published in |
European Journal of Nuclear Medicine and Molecular Imaging, June 2016
|
| DOI | 10.1007/s00259-016-3437-y |
| Pubmed ID | |
| Authors |
Stefano Boschi, Jason T. Lee, Seval Beykan, Roger Slavik, Liu Wei, Claudio Spick, Uta Eberlein, Andreas K. Buck, Filippo Lodi, Gianfranco Cicoria, Johannes Czernin, Michael Lassmann, Stefano Fanti, Ken Herrmann |
| Abstract |
The aim of this study was to synthesize and preclinically evaluate an (18)F-PSMA positron emission tomography (PET) tracer. Prostate-specific membrane antigen (PSMA) specificity, biodistribution, and dosimetry in healthy and tumor-bearing mice were determined. Several conditions for the labeling of (18)F-PSMA-11 via (18)F-AlF-complexation were screened to study the influence of reaction temperature, peptide amount, ethanol volume, and reaction time. After synthesis optimization, biodistribution and dosimetry studies were performed in C57BL6 mice. For proof of PSMA-specificity, mice were implanted with PSMA-negative (PC3) and PSMA-positive (LNCaP) tumors in contralateral flanks. Static and dynamic microPET/computed tomography (CT) imaging was performed. Quantitative labeling yields could be achieved with >97 % radiochemical purity. The (18)F-PSMA-11 uptake was more than 24-fold higher in PSMA-high LNCaP than in PSMA-low PC3 tumors (18.4 ± 3.3 %ID/g and 0.795 ± 0.260 %ID/g, respectively; p < 4.2e-5). Results were confirmed by ex vivo gamma counter analysis of tissues after the last imaging time point. The highest absorbed dose was reported for the kidneys. The maximum effective dose for an administered activity of 200 MBq was 1.72 mSv. (18)F-PSMA-11 using direct labeling of chelate-attached peptide with aluminum-fluoride detected PSMA-expressing tumors with high tumor-to-liver ratios. The kidneys were the dose-limiting organs. Even by applying the most stringent dosimetric calculations, injected activities of up to 0.56 GBq are feasible. |
X Demographics
The data shown below were collected from the profile of 1 X user who shared this research output. Click here to find out more about how the information was compiled.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Practitioners (doctors, other healthcare professionals) | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 78 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 78 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 13 | 17% |
| Researcher | 13 | 17% |
| Student > Master | 10 | 13% |
| Student > Bachelor | 5 | 6% |
| Other | 4 | 5% |
| Other | 9 | 12% |
| Unknown | 24 | 31% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 21 | 27% |
| Medicine and Dentistry | 10 | 13% |
| Pharmacology, Toxicology and Pharmaceutical Science | 5 | 6% |
| Biochemistry, Genetics and Molecular Biology | 3 | 4% |
| Engineering | 3 | 4% |
| Other | 10 | 13% |
| Unknown | 26 | 33% |
Attention Score in Context
This research output has an Altmetric Attention Score of 4. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 03 June 2021.
All research outputs
#7,320,351
of 23,806,312 outputs
Outputs from European Journal of Nuclear Medicine and Molecular Imaging
#883
of 3,083 outputs
Outputs of similar age
#117,162
of 356,080 outputs
Outputs of similar age from European Journal of Nuclear Medicine and Molecular Imaging
#17
of 52 outputs
Altmetric has tracked 23,806,312 research outputs across all sources so far. This one has received more attention than most of these and is in the 68th percentile.
So far Altmetric has tracked 3,083 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 6.1. This one has gotten more attention than average, scoring higher than 70% of its peers.
Older research outputs will score higher simply because they've had more time to accumulate mentions. To account for age we can compare this Altmetric Attention Score to the 356,080 tracked outputs that were published within six weeks on either side of this one in any source. This one has gotten more attention than average, scoring higher than 66% of its contemporaries.
We're also able to compare this research output to 52 others from the same source and published within six weeks on either side of this one. This one has gotten more attention than average, scoring higher than 63% of its contemporaries.