RT Journal Article
SR Electronic
T1 Prostate-Specific Membrane Antigen–Targeted Radiohalogenated PET and Therapeutic Agents for Prostate Cancer
JF Journal of Nuclear Medicine
JO J Nucl Med
FD Society of Nuclear Medicine
SP 90S
OP 96S
DO 10.2967/jnumed.115.170175
VO 57
IS Supplement 3
A1 Steven P. Rowe
A1 Alexander Drzezga
A1 Bernd Neumaier
A1 Markus Dietlein
A1 Michael A. Gorin
A1 Michael R. Zalutsky
A1 Martin G. Pomper
YR 2016
UL http://jnm.snmjournals.org/content/57/Supplement_3/90S.abstract
AB 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 of 18F-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 on 18F-labeled agents for PET, as they begin to redefine—along with the corresponding 68Ga-labeled agents discussed elsewhere in this supplement to The Journal of Nuclear Medicine—the management of prostate cancer across a variety of clinical contexts.