Full Text | PDF

Theranostics 2024; 14(8):3043-3079. doi:10.7150/thno.92612 This issue Cite

Review

PSMA-targeted radiotheranostics in modern nuclear medicine: then, now, and what of the future?

Mohamed Sallam^1,2,3,✉, Nam-Trung Nguyen¹, Frank Sainsbury^2,3, Nobuo Kimizuka^4,5,6, Serge Muyldermans⁷, Martina Benešová-Schäfer^8,✉

1. Queensland Micro- and Nanotechnology Centre (QMNC), Griffith University, Nathan Campus, Nathan, QLD 4111, Australia.
2. School of Environment and Science (ESC), Griffith University, Nathan Campus, Nathan, QLD 4111, Australia.
3. Griffith Institute for Drug Discovery (GRIDD), Griffith University, Nathan Campus, Nathan, QLD 4111, Australia.
4. Department of Applied Chemistry, Graduate School of Engineering, Kyushu University, 744 Moto-oka, Nishi-ku, Fukuoka 819-0395, Japan.
5. Center for Molecular Systems (CMS), Kyushu University, 744 Moto-oka, Nishi-ku, Fukuoka 819-0395, Japan.
6. Research Center for Negative Emissions Technologies (K-NETs), Kyushu University, 744 Moto-oka, Nishi-ku, Fukuoka 819-0395, Japan.
7. Laboratory of Cellular and Molecular Immunology (CMIM), Vrije Universiteit Brussel, 1050 Brussels, Belgium.
8. Research Group Molecular Biology of Systemic Radiotherapy, German Cancer Research Center (DKFZ), Im Neuenheimer Feld 280, 69120 Heidelberg, Germany.

✉ Corresponding author: M.S. (mohamed.sallamedu.au); M.B.S. (m.benesovade).

Abstract

In 1853, the perception of prostate cancer (PCa) as a rare ailment prevailed, was described by the eminent Londoner surgeon John Adams. Rapidly forward to 2018, the landscape dramatically altered. Currently, men face a one-in-nine lifetime risk of PCa, accentuated by improved diagnostic methods and an ageing population. With more than three million men in the United States alone grappling with this disease, the overall risk of succumbing to stands at one in 39. The intricate clinical and biological diversity of PCa poses serious challenges in terms of imaging, ongoing monitoring, and disease management. In the field of theranostics, diagnostic and therapeutic approaches that harmoniously merge targeted imaging with treatments are integrated. A pivotal player in this arena is radiotheranostics, employing radionuclides for both imaging and therapy, with prostate-specific membrane antigen (PSMA) at the forefront. Clinical milestones have been reached, including FDA- and/or EMA-approved PSMA-targeted radiodiagnostic agents, such as [¹⁸F]DCFPyL (PYLARIFY^®, Lantheus Holdings), [¹⁸F]rhPSMA-7.3 (POSLUMA^®, Blue Earth Diagnostics) and [⁶⁸Ga]Ga-PSMA-11 (Locametz^®, Novartis/ ILLUCCIX^®, Telix Pharmaceuticals), as well as PSMA-targeted radiotherapeutic agents, such as [¹⁷⁷Lu]Lu-PSMA-617 (Pluvicto^®, Novartis). Concurrently, ligand-drug and immune therapies designed to target PSMA are being advanced through rigorous preclinical research and clinical trials. This review delves into the annals of PSMA-targeted radiotheranostics, exploring its historical evolution as a signature molecule in PCa management. We scrutinise its clinical ramifications, acknowledge its limitations, and peer into the avenues that need further exploration. In the crucible of scientific inquiry, we aim to illuminate the path toward a future where the enigma of PCa is deciphered and where its menace is met with precise and effective countermeasures. In the following sections, we discuss the intriguing terrain of PCa radiotheranostics through the lens of PSMA, with the fervent hope of advancing our understanding and enhancing clinical practice.

Keywords: Prostate cancer, Metastatic castration-resistant prostate cancer, Metastatic hormone-sensitive prostate cancer, Prostate-specific membrane antigen, PSMA-targeted theranostics, Radiotheranostics, Nanoparticles, Antibodies, Inhibitors, Nuclear medicine

Citation styles

©2025 Ivyspring International Publisher. Terms of use