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Prostate Cancer, Part 2: PSMA and Beyond.

Geoffrey M Currie1, Eric M Rohren2,3

  • 1School of Dentistry and Medical Sciences, Charles Sturt University, Wagga Wagga, New South Wales, Australia; and gcurrie@csu.edu.au.

Journal of Nuclear Medicine Technology
|April 28, 2026
PubMed
Summary
This summary is machine-generated.

Prostate-specific membrane antigen (PSMA) targeted radioligands revolutionize prostate cancer imaging and therapy. Emerging strategies address treatment resistance and heterogeneity, moving towards personalized theranostics.

Keywords:
PSMAimagingnuclear medicineprostate cancerradioligandradionuclide therapytheranostics

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Area of Science:

  • Oncology
  • Nuclear Medicine
  • Radiopharmaceutical Chemistry

Background:

  • Prostate-specific membrane antigen (PSMA) has transformed prostate cancer management.
  • PSMA-targeted agents offer a theranostic link between imaging and radionuclide therapy.

Purpose of the Study:

  • To review PSMA biology and radiopharmaceutical performance.
  • To discuss emerging strategies for PSMA-directed theranostics.
  • To explore next-generation approaches for prostate cancer treatment.

Main Methods:

  • Review of contemporary PSMA PET agents and radioligand therapy.
  • Analysis of chelator chemistry, linker design, and binding sites.
  • Discussion of emerging radionuclides, ligand engineering, and multi-target agents.

Main Results:

  • 177Lu-PSMA-617 demonstrates improved survival in metastatic castration-resistant prostate cancer.
  • 225Ac-PSMA offers potential for micrometastatic and radioresistant disease but faces challenges.
  • Ligand engineering and novel radionuclides aim to enhance tumor retention and theranostic pairing.

Conclusions:

  • PSMA theranostics are evolving beyond a single-target approach.
  • Personalized radioligand selection and sequencing are crucial for optimal outcomes.
  • Future strategies will broaden molecular targets to address disease heterogeneity.