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[Ga]Ga-PSMA-11: The First FDA-Approved Ga-Radiopharmaceutical for PET Imaging of Prostate Cancer

Overview
Publisher MDPI
Specialty Chemistry
Date 2021 Aug 28
PMID 34451810
Citations 46
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Abstract

For the positron emission tomography (PET) imaging of prostate cancer, radiotracers targeting the prostate-specific membrane antigen (PSMA) are nowadays used in clinical practice. Almost 10 years after its discovery, [Ga]Ga-PSMA-11 has been approved in the United States by the Food and Drug Administration (FDA) as the first Ga-radiopharmaceutical for the PET imaging of PSMA-positive prostate cancer in 2020. This radiopharmaceutical combines the peptidomimetic Glu-NH-CO-NH-Lys(Ahx)-HBED-CC with the radionuclide Ga, enabling specific imaging of tumor cells expressing PSMA. Such a targeting approach may also be used for therapy planning as well as potentially for the evaluation of treatment response.

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References
1.
Muchnik Kurash M, Gill R, Khairulin M, Harbosh H, Keidar Z . 68Ga-labeled PSMA-11 (68Ga-isoPROtrace-11) synthesized with ready to use kit: normal biodistribution and uptake characteristics of tumour lesions. Sci Rep. 2020; 10(1):3109. PMC: 7033090. DOI: 10.1038/s41598-020-60099-y. View

2.
Kesch C, Vinsensia M, Radtke J, Schlemmer H, Heller M, Ellert E . Intraindividual Comparison of F-PSMA-1007 PET/CT, Multiparametric MRI, and Radical Prostatectomy Specimens in Patients with Primary Prostate Cancer: A Retrospective, Proof-of-Concept Study. J Nucl Med. 2017; 58(11):1805-1810. DOI: 10.2967/jnumed.116.189233. View

3.
Brandt M, Cardinale J, Aulsebrook M, Gasser G, Mindt T . An Overview of PET Radiochemistry, Part 2: Radiometals. J Nucl Med. 2018; 59(10):1500-1506. DOI: 10.2967/jnumed.117.190801. View

4.
Eder M, Schafer M, Bauder-Wust U, Hull W, Wangler C, Mier W . 68Ga-complex lipophilicity and the targeting property of a urea-based PSMA inhibitor for PET imaging. Bioconjug Chem. 2012; 23(4):688-97. DOI: 10.1021/bc200279b. View

5.
Thisgaard H, Kumlin J, Langkjaer N, Chua J, Hook B, Jensen M . Multi-curie production of gallium-68 on a biomedical cyclotron and automated radiolabelling of PSMA-11 and DOTATATE. EJNMMI Radiopharm Chem. 2021; 6(1):1. PMC: 7790954. DOI: 10.1186/s41181-020-00114-9. View