| Title |
44Sc-PSMA-617 for radiotheragnostics in tandem with 177Lu-PSMA-617—preclinical investigations in comparison with 68Ga-PSMA-11 and 68Ga-PSMA-617
|
|---|---|
| Published in |
EJNMMI Research, January 2017
|
| DOI | 10.1186/s13550-017-0257-4 |
| Pubmed ID | |
| Authors |
Christoph A. Umbricht, Martina Benešová, Raffaella M. Schmid, Andreas Türler, Roger Schibli, Nicholas P. van der Meulen, Cristina Müller |
| Abstract |
The targeting of the prostate-specific membrane antigen (PSMA) is of particular interest for radiotheragnostic purposes of prostate cancer. Radiolabeled PSMA-617, a 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid (DOTA)-functionalized PSMA ligand, revealed favorable kinetics with high tumor uptake, enabling its successful application for PET imaging ((68)Ga) and radionuclide therapy ((177)Lu) in the clinics. In this study, PSMA-617 was labeled with cyclotron-produced (44)Sc (T 1/2 = 4.04 h) and investigated preclinically for its use as a diagnostic match to (177)Lu-PSMA-617. (44)Sc was produced at the research cyclotron at PSI by irradiation of enriched (44)Ca targets, followed by chromatographic separation. (44)Sc-PSMA-617 was prepared under standard labeling conditions at elevated temperature resulting in a radiochemical purity of >97% at a specific activity of up to 10 MBq/nmol. (44)Sc-PSMA-617 was evaluated in vitro and compared to the (177)Lu- and (68)Ga-labeled match, as well as (68)Ga-PSMA-11 using PSMA-positive PC-3 PIP and PSMA-negative PC-3 flu prostate cancer cells. In these experiments it revealed similar in vitro properties to that of (177)Lu- and (68)Ga-labeled PSMA-617. Moreover, (44)Sc-PSMA-617 bound specifically to PSMA-expressing PC-3 PIP tumor cells, while unspecific binding to PC-3 flu cells was not observed. The radioligands were investigated with regard to their in vivo properties in PC-3 PIP/flu tumor-bearing mice. (44)Sc-PSMA-617 showed high tumor uptake and a fast renal excretion. The overall tissue distribution of (44)Sc-PSMA-617 resembled that of (177)Lu-PSMA-617 most closely, while the (68)Ga-labeled ligands, in particular (68)Ga-PSMA-11, showed different distribution kinetics. (44)Sc-PSMA-617 enabled distinct visualization of PC-3 PIP tumor xenografts shortly after injection, with increasing tumor-to-background contrast over time while unspecific uptake in the PC-3 flu tumors was not observed. The in vitro characteristics and in vivo kinetics of (44)Sc-PSMA-617 were more similar to (177)Lu-PSMA-617 than to (68)Ga-PSMA-617 and 68Ga-PSMA-11. Due to the almost four-fold longer half-life of (44)Sc as compared to (68)Ga, a centralized production of (44)Sc-PSMA-617 and transport to satellite PET centers would be feasible. These features make (44)Sc-PSMA-617 particularly appealing for clinical application. |
Mendeley readers
The data shown below were compiled from readership statistics for 157 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| United States | 1 | <1% |
| Unknown | 156 | 99% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 30 | 19% |
| Researcher | 30 | 19% |
| Student > Master | 13 | 8% |
| Student > Bachelor | 10 | 6% |
| Other | 9 | 6% |
| Other | 22 | 14% |
| Unknown | 43 | 27% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 34 | 22% |
| Medicine and Dentistry | 16 | 10% |
| Pharmacology, Toxicology and Pharmaceutical Science | 14 | 9% |
| Physics and Astronomy | 11 | 7% |
| Biochemistry, Genetics and Molecular Biology | 8 | 5% |
| Other | 26 | 17% |
| Unknown | 48 | 31% |
Attention Score in Context
This research output has an Altmetric Attention Score of 3. 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 26 December 2019.
All research outputs
#7,657,585
of 23,312,088 outputs
Outputs from EJNMMI Research
#150
of 572 outputs
Outputs of similar age
#142,812
of 419,455 outputs
Outputs of similar age from EJNMMI Research
#3
of 11 outputs
Altmetric has tracked 23,312,088 research outputs across all sources so far. This one is in the 44th percentile – i.e., 44% of other outputs scored the same or lower than it.
So far Altmetric has tracked 572 research outputs from this source. They receive a mean Attention Score of 2.6. This one has gotten more attention than average, scoring higher than 68% 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 419,455 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 53% of its contemporaries.
We're also able to compare this research output to 11 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 72% of its contemporaries.