The Discovery of Prostate-specific Membrane Antigen Ligands: The Long Road to Changes in Clinical Practice for

Martina Benešová-Schäfer1, Uwe Haberkorn2, John W Babich3

  • 1Translational Radiotheranostics Research Group, German Cancer Research Center, Heidelberg, Germany.

European Urology
|January 15, 2026
PubMed

Insights

Prostate-specific membrane antigen (PSMA) targeted therapies have advanced significantly for prostate cancer. Continued innovation is crucial due to tumor heterogeneity and treatment resistance in metastatic disease.

Area of Science:

  • Oncology
  • Molecular Imaging
  • Radiopharmaceuticals

Background:

  • Prostate-specific membrane antigen (PSMA) is a key target in prostate cancer.
  • PSMA-targeting agents have evolved from diagnostic tools to therapeutics.
  • Metastatic prostate cancer presents challenges due to biological heterogeneity and resistance.

Purpose of the Study:

  • To review the evolution of PSMA-targeting strategies in prostate cancer.
  • To highlight the current role of PSMA in metastatic disease.
  • To emphasize the need for ongoing innovation and combination therapies.

Main Methods:

  • Literature review of PSMA-targeting agents.
  • Analysis of diagnostic and therapeutic applications.
  • Discussion of challenges and future directions.

Main Results:

  • PSMA-targeting strategies have shown significant advancements.
  • PSMA remains a critical biomarker in metastatic prostate cancer.
  • Heterogeneity and resistance necessitate novel approaches.

Conclusions:

  • PSMA-targeting agents are vital in prostate cancer management.
  • Further research into combination strategies is essential.
  • Innovation is key to overcoming treatment resistance.