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Synthesis and preclinical evaluation of an Al18F radiofluorinated GLU-UREA-LYS(AHX)-HBED-CC PSMA ligand.


ABSTRACT: The aim of this study was to synthesize and preclinically evaluate an 18F-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 18F-PSMA-11 via 18F-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 18F-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?

SUBMITTER: Boschi S 

PROVIDER: S-EPMC5050145 | biostudies-literature | 2016 Nov

REPOSITORIES: biostudies-literature

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Synthesis and preclinical evaluation of an Al<sup>18</sup>F radiofluorinated GLU-UREA-LYS(AHX)-HBED-CC PSMA ligand.

Boschi Stefano S   Lee Jason T JT   Beykan Seval S   Slavik Roger R   Wei Liu L   Spick Claudio C   Eberlein Uta U   Buck Andreas K AK   Lodi Filippo F   Cicoria Gianfranco G   Czernin Johannes J   Lassmann Michael M   Fanti Stefano S   Herrmann Ken K  

European journal of nuclear medicine and molecular imaging 20160622 12


<h4>Purpose</h4>The aim of this study was to synthesize and preclinically evaluate an <sup>18</sup>F-PSMA positron emission tomography (PET) tracer. Prostate-specific membrane antigen (PSMA) specificity, biodistribution, and dosimetry in healthy and tumor-bearing mice were determined.<h4>Methods</h4>Several conditions for the labeling of <sup>18</sup>F-PSMA-11 via <sup>18</sup>F-AlF-complexation were screened to study the influence of reaction temperature, peptide amount, ethanol volume, and rea  ...[more]

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