Universität zu Köln

Zlatopolskiy, Boris D., Endepols, Heike ORCID: 0000-0002-6166-4818, Krapf, Philipp ORCID: 0000-0003-1671-2443, Guliyev, Mehrab, Urusova, Elizaveta A., Richarz, Raphael, Hohberg, Melanie, Dietlein, Markus, Drzezga, Alexander and Neumaier, Bernd (2019). Discovery of F-18-JK-PSMA-7, a PET Probe for the Detection of Small PSMA-Positive Lesions. J. Nucl. Med., 60 (6). S. 817 - 824. RESTON: SOC NUCLEAR MEDICINE INC. ISSN 1535-5667

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Abstract

Prostate-specific membrane antigen (PSMA), expressed by most prostate carcinomas (PCa), is a promising target for PCa imaging. The application of PSMA-specific F-18-labeled PET probes such as F-18-DCFPyL and F-18-PSMA-1007 considerably improved the accuracy of PCa tumor detection. However, there remains a need for further improvements in sensitivity and specificity. The aim of this study was the development of highly selective and specific PSMA probes with enhanced imaging properties, in comparison with F-18-DCFPyL, F-18-PSMA-1007, and Ga-68-PSMA-11. Methods: Eight novel F-18-labeled PSMA ligands were prepared. Their cellular uptake in PSMA-positive LNCaP C4-2 and PSMA-negative PC-3 cells was compared with that of F-18-DCFPyL. The most promising candidates were additionally evaluated by small-animal PET in healthy rats using PSMA-positive peripheral ganglia as a model for small PCa lesions. PET images of the ligand with the best outcome, F-18-JK-PSMA-7, were compared with those of F-18-DCFPyL, F-18-PSMA-1007, and Ga-68-PSMA-11 with respect to key image-quality parameters for the time frame 60-120 min. Results: Compared with F-18-DCFPyL, F-18-JK-PSMA-7 demonstrated increased PSMA-specific cellular uptake. Although target-to-background ratios of F-18-DCFPyL and F-18-PSMA-1007 were comparable, this parameter was higher for F-18-JK-PSMA-7 and lower for Ga-68-PSMA-11. Image acutance was significantly higher for F-18-JK-PSMA-7 and F-18-PSMA-1007 than for F-18-DCFPyL and Ga-68-PSMA-11. Image resolution was similar for all 4 tracers. F-18-PSMA-1007 demonstrated significantly higher blood protein binding and bone uptake than the other tracers. Conclusion: F-18-JK-PSMA-7 is a promising candidate for high-quality visualization of small PSMA-positive lesions. Excellent preclinical imaging properties justify further preclinical and clinical studies of this tracer.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Zlatopolskiy, Boris D. UNSPECIFIED UNSPECIFIED UNSPECIFIED Endepols, Heike UNSPECIFIED orcid.org/0000-0002-6166-4818 UNSPECIFIED Krapf, Philipp UNSPECIFIED orcid.org/0000-0003-1671-2443 UNSPECIFIED Guliyev, Mehrab UNSPECIFIED UNSPECIFIED UNSPECIFIED Urusova, Elizaveta A. UNSPECIFIED UNSPECIFIED UNSPECIFIED Richarz, Raphael UNSPECIFIED UNSPECIFIED UNSPECIFIED Hohberg, Melanie UNSPECIFIED UNSPECIFIED UNSPECIFIED Dietlein, Markus UNSPECIFIED UNSPECIFIED UNSPECIFIED Drzezga, Alexander UNSPECIFIED UNSPECIFIED UNSPECIFIED Neumaier, Bernd UNSPECIFIED UNSPECIFIED UNSPECIFIED
URN:	urn:nbn:de:hbz:38-146819
DOI:	10.2967/jnumed.118.218495
Journal or Publication Title:	J. Nucl. Med.
Volume:	60
Number:	6
Page Range:	S. 817 - 824
Date:	2019
Publisher:	SOC NUCLEAR MEDICINE INC
Place of Publication:	RESTON
ISSN:	1535-5667
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language ANTIGEN-LIGAND PSMA-7; PROSTATE-CANCER; F-18-DCFPYL PET/CT; DESIGN Multiple languages Radiology, Nuclear Medicine & Medical Imaging Multiple languages
Refereed:	Yes
URI:	http://kups.ub.uni-koeln.de/id/eprint/14681