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Positron Emission Tomography (PET) is a medical imaging technique that provides crucial insights into the body's physiological functions at a molecular level. It is an indispensable resource for diagnosing, staging, and monitoring various illnesses, notably cancer, neurological disorders, and cardiovascular conditions.
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Related Experiment Video

Updated: Oct 9, 2025

18F-Labeling of Radiotracers Functionalized with a Silicon Fluoride Acceptor SiFA for Positron Emission Tomography
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Radiolabeled PSMA Inhibitors.

Oliver C Neels1, Klaus Kopka1,2, Christos Liolios3,4

  • 1Institute of Radiopharmaceutical Cancer Research, Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Bautzner Landstrasse 400, 01328 Dresden, Germany.

Cancers
|December 24, 2021
PubMed
Summary

Prostate-specific membrane antigen (PSMA) theranostics offer advanced prostate cancer diagnosis and therapy. Further refinement of PSMA radiopharmaceuticals is needed to improve treatment efficacy and reduce side effects.

Keywords:
PETPSMAPSMA inhibitorSPECTendoradiotherapyfluorescencefluorescence-guided surgeryprostate-specific membrane antigenradioguided surgeryradiolabelingradionuclidestargeted photodynamic therapytheranostics

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Area of Science:

  • Oncology
  • Radiochemistry
  • Nuclear Medicine

Background:

  • Prostate-specific membrane antigen (PSMA) is a key target for prostate cancer theranostics.
  • Current PSMA-targeting agents show promise in diagnosis and therapy.

Purpose of the Study:

  • To review recent developments in PSMA-targeting agents for prostate cancer.
  • To discuss radio- and fluorescence-guided surgery, photodynamic therapy, and multitargeting inhibitors.
  • To provide an overview of regulatory status, technical aspects, and radiolabeling strategies.

Main Methods:

  • Literature review of PSMA-targeting radiopharmaceuticals and therapies.
  • Analysis of multitargeting PSMA inhibitors and alternative radionuclides.
  • Discussion of regulatory landscapes in the USA and Europe.

Main Results:

  • PSMA inhibitors are being developed to target albumin, GRPr, and integrin αvβ3.
  • New radiolabeling strategies and alternative radionuclides are emerging.
  • Regulatory status and technical considerations for PSMA radiopharmaceuticals are presented.

Conclusions:

  • PSMA theranostics represent a significant advancement in prostate cancer care.
  • Further optimization of radiopharmaceuticals is crucial to mitigate dose-limiting toxicities like nephrotoxicity and salivary gland uptake.
  • Combining radionuclide therapy with alternative approaches holds potential for enhanced patient outcomes.