PET imaging of prostate tumors with 18F‐Al‐NOTA‐MATBBN. (14th April 2014)

• Record Type: Journal Article
• Authors: Pan, Donghui; Yan, Yongjun; Yang, Ronghua; Xu, Yu Ping; Chen, Fei; Wang, Lizhen; Luo, Shineng; Yang, Min
• Is Part Of: Contrast media & molecular imaging. Volume 9:Number 5(2014:Sep./Oct.)
• Page Start: 342
• Page End: 348
• Publication Date: 2014-04-14
• Subjects: Diagnostic imaging -- Periodicals; Magnetic resonance imaging -- Periodicals; Contrast media (Diagnostic imaging) -- Periodicals; Contrast Media -- Periodicals; Diagnostic Imaging -- Periodicals; Substances de contraste -- Périodiques; Diagnostics moléculaires -- Périodiques; Imagerie médicale; Substance de contraste; Périodique électronique (Descripteur de forme); Ressource Internet (Descripteur de forme); 616.0754
• DOI: 10.1002/cmmi.1583
• Languages: English
• ISSNs: 1555-4309

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <p>Overexpression of the gastrin‐releasing peptide receptor (GRPR) in prostate cancer provides a promising target for detection the disease. MATBBN is a new bombesin analog originating from the GRPR antagonists with a hydrophilic linker. In this study NOTA‐conjugated MATBBN was labeled by the Al<sup>18</sup>F method and the potential of <sup>18</sup>F‐Al‐NOTA‐MATBBN for prostate tumor PET imaging was also evaluated. NOTA‐MATBBN was radiolabeled with <sup>18</sup>F using Al<sup>18</sup>F complexes. Partition coefficient, <italic>in vitro</italic> stability and GRPR binding affinity were also determined. PET studies were performed with <sup>18</sup>F‐Al‐NOTA‐MATBBN in PC‐3 tumor‐bearing mice. <sup>18</sup>F‐Al‐NOTA‐MATBBN can be produced within 30 min with a decay‐corrected yield of 62.5 ± 2.1% and a radiochemical purity of >98%. The log<italic>P</italic> octanol–water value for the Al<sup>18</sup>F‐labeled BBN analog was −2.40 ± 0.07 and the radiotracer was stable in phosphate‐buffered saline and human serum for 2 h. The IC<sub>50</sub> values of displacement for the <sup>18</sup>F‐Al‐NOTA‐MATBBN with MATBBN was 126.9 ± 2.75 n<sc>m</sc>. The PC‐3 tumors were clearly visible with high contrast after injection of the labeled peptide. At 60 min post‐injection, the tumor uptakes for <sup>18</sup>F‐Al‐NOTA‐MATBBN and <sup>18</sup>F‐FDG were 4.59 ± 0.43 and 1.98 ± 0.35% injected dose/g, and tumor to muscle uptake radios for two tracers were 6.77 ± 1.10 and 1.78 ± 0.32, respectively. Dynamic PET revealed that <sup>18</sup>F‐Al‐NOTA‐MATBBN was excreted mainly through the kidneys. GRPR‐binding specificity was also demonstrated by reduced tumor uptake of <sup>18</sup>F‐Al‐NOTA‐MATBBN after coinjection with excess unlabeled MATBBN peptide at 1 h post‐injection. NOTA‐ MATBBN could be labeled rapidly with <sup>18</sup>F using one step method. <sup>18</sup>F‐Al‐NOTA‐MATBBN may be a promising PET imaging agent for prostate cancer. Copyright © 2014 John Wiley & Sons, Ltd.</p> </abstract>