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177Lu-PSMA for prostate cancer: progress, challenges and future perspectives.

Zhen Xi1, Shi-Yu Ji, Yu Zhang

  • 1Department of Urology, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200080, China.

Asian Journal of Andrology
|February 13, 2026
PubMed
Summary
This summary is machine-generated.

Lutetium-177-labeled prostate-specific membrane antigen (177Lu-PSMA) therapy offers new hope for advanced prostate cancer. While effective for metastatic castration-resistant prostate cancer (mCRPC), further research is needed for standardization and broader application.

Keywords:
biomarkersclinical trialscombination therapyprecision medicineprostate cancerradioligand therapyradiopharmaceuticals

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Area of Science:

  • Oncology
  • Nuclear Medicine
  • Radiopharmaceutical Therapy

Background:

  • Prostate cancer, particularly metastatic castration-resistant prostate cancer (mCRPC), presents significant global health challenges with limited conventional treatment efficacy.
  • The progression to castration-resistant disease involves complex mechanisms and carries a poor prognosis.

Purpose of the Study:

  • To review recent advancements, efficacy, and safety of Lutetium-177-labeled prostate-specific membrane antigen (177Lu-PSMA) therapy.
  • To analyze current limitations and propose future research directions for PSMA-targeted radioligand therapy (RLT).

Main Methods:

  • Comprehensive literature review of recent studies on 177Lu-PSMA therapy.
  • Analysis of clinical trial data and published research on efficacy and safety.
  • Evaluation of current challenges and future research needs in PSMA-targeted RLT.

Main Results:

  • 177Lu-PSMA therapy, approved by the FDA in 2022, is a promising radioligand transforming mCRPC treatment.
  • The therapy has demonstrated significant efficacy in patients with mCRPC.
  • Recent advancements include improved understanding of its safety profile and therapeutic potential.

Conclusions:

  • 177Lu-PSMA-617 is revolutionizing mCRPC treatment, offering a new therapeutic paradigm.
  • Challenges persist in standardizing its use for non-mCRPC cases, optimizing treatment sequencing, and developing standardized imaging biomarkers.
  • Further prospective validation is required for toxicity management and broader clinical application.