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Updated: Jan 5, 2026

A Bioluminescent and Fluorescent Orthotopic Syngeneic Murine Model of Androgen-dependent and Castration-resistant Prostate Cancer
Published on: March 6, 2018
Prostate-specific membrane antigen-targeted endoradiotherapy in metastatic prostate cancer
Ismaheel O Lawal1, Frank Bruchertseifer, Mariza Vorster
1Department of Nuclear Medicine, University of Pretoria, Pretoria, South Africa European Commission, Joint Research Centre, Directorate for Nuclear Safety and Security, Karlsruhe, Germany.
Purpose Of Review:
In this review, we present an update on the safety and efficacy of prostate-specific membrane antigen (PSMA) radioligand therapy (PRLT) of metastatic castration-resistant prostate cancer (mCRPC).
Recent Findings:
Treatment of mCRPC with approved treatment agents leads to a survival advantage. The disease often progresses despite these treatments. PRLT with Lutetium-177 and Actinium-225 labeled with PSMA (LuPSMA and AcPSMA) have recently been shown to be effective and well tolerated for mCRPC treatment. LuPSMA is currently applied in patients who have exhausted approved treatment options or in whom these approved treatments are contraindicated. In this category of heavily pretreated patients, prostate-specific antigen (PSA) response (≥50% decline) is achieved in about 46% of patients. Side-effects are tolerable with rare reports of grade III-IV treatment-induced toxicity. AcPSMA is currently applied on a smaller scale in patients who relapsed after LuPSMA or in whom LuPSMA is contraindicated. PSA response occurs in up to 88% of patients treated with AcPSMA.
Summary:
PRLT with LuPSMA and AcPSMA is a well-tolerated and effective treatment modality for mCRPC. Prospective randomized control trials are necessary to facilitate its application as an approved therapy option.

