PSMA ligands in prostate cancer – Probe optimization and theranostic applications

•PSMA ligands allow highly specific diagnostic imaging and radioligand therapy of PCa.•Structural changes may affect the pharmacokinetics of the PSMA ligands.•Structural changes resulted in the development of novel theranostic applications. Due to its selective overexpression in prostate cancer (PCa...

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Bibliographic Details
Published in:Methods (San Diego, Calif.) Calif.), 2017-11, Vol.130, p.42-50
Main Authors: Lütje, Susanne, Slavik, Roger, Fendler, Wolfgang, Herrmann, Ken, Eiber, Matthias
Format: Article
Language:English
Subjects:
Animals
Antigens, Surface
Binding Sites - physiology
Fluorodeoxyglucose F18 - administration & dosage
Fluorodeoxyglucose F18 - metabolism
Gallium Radioisotopes - administration & dosage
Gallium Radioisotopes - metabolism
Glutamate Carboxypeptidase II
Humans
Imaging
Ligands
Male
Prostate cancer
Prostatic Neoplasms - diagnostic imaging
Prostatic Neoplasms - metabolism
PSMA
Radioisotopes - administration & dosage
Radioisotopes - metabolism
Theranostic Nanomedicine - methods
Theranostic Nanomedicine - standards
Theranostics
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Summary:•PSMA ligands allow highly specific diagnostic imaging and radioligand therapy of PCa.•Structural changes may affect the pharmacokinetics of the PSMA ligands.•Structural changes resulted in the development of novel theranostic applications. Due to its selective overexpression in prostate cancer (PCa), the prostate-specific membrane antigen (PSMA) has been recognized as a highly promising target for diagnostic and therapeutic applications. So far, various PSMA ligands have been developed for radiolabeling with radioisotopes such as 68Ga or 18F which can be used for specific visualization and diagnosis of PSMA-expressing PCa. In addition, PSMA ligands suitable for radiolabeling with 131I or 177Lu have become available to the clinics, allowing PSMA-based radioligand therapies. Here, we provide a comprehensive review of the most frequently used PSMA ligands, their structural modifications, and the impact of those on clinical applications.
ISSN:1046-2023
1095-9130
DOI:10.1016/j.ymeth.2017.06.026