Rowe, Steven P., Drzezga, Alexander, Neumaier, Bernd ORCID: 0000-0001-5425-3116, Dietlein, Markus, Gorin, Michael A., Zalutsky, Michael R. and Pomper, Martin G. (2016). Prostate-Specific Membrane Antigen-Targeted Radiohalogenated PET and Therapeutic Agents for Prostate Cancer. J. Nucl. Med., 57. S. 90S - 97. RESTON: SOC NUCLEAR MEDICINE INC. ISSN 1535-5667

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Abstract

Radiohalogenated agents are often the first line of pursuit in the development of new radiopharmaceuticals whether antibodies, peptides, or small molecules because of their ease of synthesis, lack of substantial steric perturbation of the original affinity agent (in some cases, providing enhanced affinity), and capacity to be transformed into therapeutics (in some cases, with a mere switch of an isotope). They often provide proof of a principle before optimization for pharmacokinetics or generation of radiometallated agents, when the latter are necessary. In particular, F-18 has been well integrated into normal clinical work flow in the form of F-18-FDG for oncologic imaging, with reliable daily production and distribution to sites for immediate use, without the need for on-site preparation. Here we discuss radiohalo-genated versions of imaging and therapeutic agents targeting the prostate-specific membrane antigen (PSMA); these were among the first such agents to be synthesized and used clinically. PSMA is highly expressed on prostate cancer epithelial cells and is currently being extensively investigated around the world as a target for imaging and therapy of prostate cancer. Additionally, the presence of PSMA on nonprostate tumor neovasculature has opened the possibility of PSMA-targeted molecules as generalizable cancer imaging and therapy agents. We focus on F-18-labeled agents for PET, as they begin to redefine-along with the corresponding Ga-68-labeled agents discussed elsewhere in this supplement to The Journal of Nuclear Medicine-the management of prostate cancer across a variety of clinical contexts.

Item Type: Journal Article
Creators:
CreatorsEmailORCIDORCID Put Code
Rowe, Steven P.UNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Drzezga, AlexanderUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Neumaier, BerndUNSPECIFIEDorcid.org/0000-0001-5425-3116UNSPECIFIED
Dietlein, MarkusUNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Gorin, Michael A.UNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Zalutsky, Michael R.UNSPECIFIEDUNSPECIFIEDUNSPECIFIED
Pomper, Martin G.UNSPECIFIEDUNSPECIFIEDUNSPECIFIED
URN: urn:nbn:de:hbz:38-261656
DOI: 10.2967/jnumed.115.170175
Journal or Publication Title: J. Nucl. Med.
Volume: 57
Page Range: S. 90S - 97
Date: 2016
Publisher: SOC NUCLEAR MEDICINE INC
Place of Publication: RESTON
ISSN: 1535-5667
Language: English
Faculty: Unspecified
Divisions: Unspecified
Subjects: no entry
Uncontrolled Keywords:
KeywordsLanguage
POSITRON-EMISSION-TOMOGRAPHY; BIOCHEMICAL RECURRENCE; PRECLINICAL EVALUATION; RADIATION-DOSIMETRY; GA-68-PSMA PET/CT; F-18-DCFBC PET/CT; BAY 1075553; PSMA; EXPRESSION; DIAGNOSISMultiple languages
Radiology, Nuclear Medicine & Medical ImagingMultiple languages
Refereed: Yes
URI: http://kups.ub.uni-koeln.de/id/eprint/26165

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