PSMA-Targeting Imaging and Theranostic Agents—Current Status and Future Perspective

Sashi Debnath, Ning Zhou, Mark McLaughlin, Samuel Rice, Anil K. Pillai, Guiyang Hao, Xiankai Sun

Research output: Contribution to journalReview articlepeer-review

8 Scopus citations


In the past two decades, extensive efforts have been made to develop agents targeting prostate-specific membrane antigen (PSMA) for prostate cancer imaging and therapy. To date, represented by two recent approvals of [68Ga]Ga-PSMA-11 and [18F]F-DCFPyL by the United States Food and Drug Administration (US-FDA) for positron emission tomography (PET) imaging to identify suspected metastases or recurrence in patients with prostate cancer, PSMA-targeting imaging and theranostic agents derived from small molecule PSMA inhibitors have advanced to clinical practice and trials of prostate cancer. The focus of current development of new PSMA-targeting agents has thus shifted to the improvement of in vivo pharmacokinetics and higher specific binding affinity with the aims to further increase the detection sensitivity and specificity and minimize the toxicity to non-target tissues, particularly the kidneys. The main strategies involve systematic chemical modifications of the linkage between the targeting moiety and imaging/therapy payloads. In addition to a summary of the development history of PSMA-targeting agents, this review provides an overview of current advances and future promise of PSMA-targeted imaging and theranostics with focuses on the structural determinants of the chemical modification towards the next generation of PSMA-targeting agents.

Original languageEnglish (US)
Article number1158
JournalInternational journal of molecular sciences
Issue number3
StatePublished - Feb 1 2022


  • Binding affinity
  • Inhibitor
  • Positron emission tomography
  • Prostate cancer
  • Prostate-specific antigen
  • Prostate-specific membrane antigen
  • Radionuclide therapy
  • Theranostics

ASJC Scopus subject areas

  • Catalysis
  • Molecular Biology
  • Spectroscopy
  • Computer Science Applications
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry


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