TY - JOUR
T1 - Imaging of prostate-specific membrane antigen with small-molecule PET radiotracers
T2 - From the bench to advanced clinical applications
AU - Rowe, Steven P.
AU - Gorin, Michael A.
AU - Pomper, Martin G.
N1 - Publisher Copyright:
© 2019 by Annual Reviews.
PY - 2019/1/27
Y1 - 2019/1/27
N2 - In recent years, small-molecule inhibitors of prostate-specific membrane antigen (PSMA) labeled with radionuclides that allow for positron emission tomography (PET) imaging have been extensively studied in many clinical contexts in men with prostate cancer (PCa). The high sensitivity and specificity of these agents for identifying sites of PCa has quickly led to their widespread adoption as a de facto clinical standard of care throughout much of the world. PSMA-targeted PET radiotracers have been particularly well-studied in preoperatively staging men with high-risk PCa, evaluating biochemical recurrence following definitive therapy, and guiding metastasis-directed therapy in patients suspected of having oligorecurrent/oligometastatic disease. Furthermore, the expression of PSMA on the tumor neovasculature of many nonprostate malignancies has enabled a burgeoning subfield concentrated on delineating the potential utility of PSMA-targeted PET agents for imaging other cancers. In this review, we highlight the preclinical development of key small molecules that are now being clinically utilized for PCa imaging, discuss the roles of PSMA-targeted agents in guiding patient management, and consider the role these compounds may play in imaging nonprostate cancers.
AB - In recent years, small-molecule inhibitors of prostate-specific membrane antigen (PSMA) labeled with radionuclides that allow for positron emission tomography (PET) imaging have been extensively studied in many clinical contexts in men with prostate cancer (PCa). The high sensitivity and specificity of these agents for identifying sites of PCa has quickly led to their widespread adoption as a de facto clinical standard of care throughout much of the world. PSMA-targeted PET radiotracers have been particularly well-studied in preoperatively staging men with high-risk PCa, evaluating biochemical recurrence following definitive therapy, and guiding metastasis-directed therapy in patients suspected of having oligorecurrent/oligometastatic disease. Furthermore, the expression of PSMA on the tumor neovasculature of many nonprostate malignancies has enabled a burgeoning subfield concentrated on delineating the potential utility of PSMA-targeted PET agents for imaging other cancers. In this review, we highlight the preclinical development of key small molecules that are now being clinically utilized for PCa imaging, discuss the roles of PSMA-targeted agents in guiding patient management, and consider the role these compounds may play in imaging nonprostate cancers.
KW - glutamate carboxypeptidase II NAALADase
KW - prostate cancer
KW - renal cell carcinoma
KW - tumor neovasculature
UR - http://www.scopus.com/inward/record.url?scp=85060621050&partnerID=8YFLogxK
U2 - 10.1146/annurev-med-062117-073027
DO - 10.1146/annurev-med-062117-073027
M3 - Review article
C2 - 30691373
AN - SCOPUS:85060621050
SN - 0066-4219
VL - 70
SP - 461
EP - 477
JO - Annual Review of Medicine
JF - Annual Review of Medicine
ER -