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Updated: Jan 1, 2026
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Development of a 68Gallium-Labeled D-Peptide PET Tracer for Imaging Programmed Death-Ligand 1 Expression
Published on: February 3, 2023
1.9K
Radiolabeled prostate-specific membrane antigen small-molecule inhibitors
Leon Will1, Ida Sonni2, Klaus Kopka3,4
1Department of Nuclear Medicine, University of Heidelberg, Heidelberg, Germany.
Summary
Prostate-specific membrane antigen (PSMA) imaging significantly improves prostate cancer staging and recurrence detection. PSMA-targeted radioligand therapy shows promise for metastatic disease, offering new hope for treatment-resistant cases.
Area of Science:
- Oncology
- Nuclear Medicine
- Radiochemistry
Background:
- Prostate cancer (PC) is a global health concern.
- Prostate-specific membrane antigen (PSMA) is highly expressed in most PCs, making it a prime diagnostic and therapeutic target.
- Advancements in PSMA tracers offer new avenues for PC management.
Purpose of the Study:
- To review the clinical impact of PSMA tracers in PC diagnosis and therapy.
- To evaluate PSMA tracers in primary staging, biochemical recurrence (BCR), and advanced metastatic PC.
- To explore the role of PSMA tracers in radioligand therapy (RLT) for metastatic castration-resistant prostate cancer (mCRPC).
Main Methods:
- Comprehensive literature search of PubMed for studies on PSMA tracers in PC diagnosis and therapy.
- Analysis of evidence regarding PSMA positron-emission tomography/computed tomography (PET/CT) in various PC stages.
- Review of data on 177Lu-labeled PSMA tracers for systemic RLT.
Main Results:
- PSMA PET/CT demonstrates superior performance over conventional imaging for primary, recurrent, and advanced PC.
- PSMA PET/CT significantly increases detection rates in BCR, altering therapeutic management in up to 50% of cases.
- Early studies indicate positive clinical effects and minimal side effects with 177Lu-PSMA RLT.
Conclusions:
- PSMA targeting has a significant clinical impact on prostate cancer diagnosis.
- PSMA-based imaging enhances staging and recurrence detection compared to standard methods.
- Radioligand therapy with PSMA tracers holds substantial potential for treating refractory prostate cancer.
