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The Future of PSMA-Targeted Radionuclide Therapy: An Overview of Recent Preclinical Research

1
Dept. of Radiology and Nuclear Medicine, Erasmus MC, 3015 GD Rotterdam, The Netherlands
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Dept. of Experimental Urology, Erasmus MC, 3015 GD Rotterdam, The Netherlands
3
Dept. of Molecular Genetics, Erasmus MC, 3015 GD Rotterdam, The Netherlands
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Oncode Institute, Erasmus MC, 3015 GD Rotterdam, The Netherlands
*
Author to whom correspondence should be addressed.
Authors equally contributed to the work.
Pharmaceutics 2019, 11(11), 560; https://doi.org/10.3390/pharmaceutics11110560
Received: 27 September 2019 / Revised: 23 October 2019 / Accepted: 24 October 2019 / Published: 29 October 2019
(This article belongs to the Special Issue Targeted Radionuclide Tumor Therapy)
Prostate specific membrane antigen (PSMA) has become a major focus point in the research and development of prostate cancer (PCa) imaging and therapeutic strategies using radiolabeled tracers. PSMA has shown to be an excellent target for PCa theranostics because of its high expression on the membrane of PCa cells and the increase in expression during disease progression. Therefore, numerous PSMA-targeting tracers have been developed and (pre)clinically studied with promising results. However, many of these PSMA-targeting tracers show uptake in healthy organs such as the salivary glands, causing radiotoxicity. Furthermore, not all patients respond to PSMA-targeted radionuclide therapy (TRT). This created the necessity of additional preclinical research studies in which existing tracers are reevaluated and new tracers are developed in order to improve PSMA-TRT by protecting the (PSMA-expressing) healthy organs and improving tumor uptake. In this review we will give an overview of the recent preclinical research projects regarding PCa-TRT using PSMA-specific radiotracers, which will give an indication of where the PSMA-TRT research movement is going and what we can expect in future clinical trials. View Full-Text
Keywords: prostate specific membrane antigen; prostate cancer; targeted radionuclide therapy prostate specific membrane antigen; prostate cancer; targeted radionuclide therapy
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Ruigrok, E.A.; van Weerden, W.M.; Nonnekens, J.; de Jong, M. The Future of PSMA-Targeted Radionuclide Therapy: An Overview of Recent Preclinical Research. Pharmaceutics 2019, 11, 560.

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