Prostate-Specific Membrane Antigen-Targeted Radiohalogenated PET and Therapeutic Agents for Prostate Cancer.
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,18F has been well integrated into normal clinical work flow in the form of18F-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 radiohalogenated 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 on18F-labeled agents for PET, as they begin to redefine-along with the corresponding68Ga-labeled agents discussed elsewhere in this supplement to The Journal of Nuclear Medicine-the management of prostate cancer across a variety of clinical contexts.
The Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins University School of Medicine, Baltimore, Maryland.
Steven P
SP
Rowe
Department of Nuclear Medicine, University Hospital of Cologne, Cologne, Germany.
Alexander
A
Drzezga
Institute of Radiochemistry and Experimental Molecular Imaging, University Hospital of Cologne, Cologne, Germany.
Bernd
B
Neumaier
Department of Nuclear Medicine, University Hospital of Cologne, Cologne, Germany.
Markus
M
Dietlein
The James Buchanan Brady Urological Institute and Department of Urology, Johns Hopkins University School of Medicine, Baltimore, Maryland; and.
Michael A
MA
Gorin
Department of Radiology, Duke University Medical Center, Durham, North Carolina.
Michael R
MR
Zalutsky
The Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins University School of Medicine, Baltimore, Maryland mpomper@jhmi.edu.
Martin G
MG
Pomper
D019317:Evidence-Based Medicine; D006219:Halogens / Q000493:pharmacokinetics / Q000627:therapeutic use*; D006801:Humans; D007089:Image Enhancement; D008297:Male; D015336:Molecular Probe Techniques; D058990:Molecular Targeted Therapy; D049268:Positron-Emission Tomography; D017430:Prostate-Specific Antigen / Q000037:antagonists & inhibitors*; D011471:Prostatic Neoplasms / Q000000981:diagnostic imaging* / Q000378:metabolism / Q000532:radiotherapy*; D011868:Radioisotopes / Q000627:therapeutic use*; D019275:Radiopharmaceuticals / Q000627:therapeutic use; D016896:Treatment Outcome
D006219:Halogens; D011868:Radioisotopes; D019275:Radiopharmaceuticals; D017430:Prostate-Specific Antigen
18F; 211At; PET; biochemical recurrence; prostate-specific membrane antigen
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