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Lutetium-177 PSMA radioligand is a targeted radiopharmaceutical therapy used for the treatment of prostate cancer. It consists of the beta-emitting radioisotope lutetium-177 conjugated to a small-molecule ligand that specifically targets prostate-specific membrane antigen (PSMA), a protein highly expressed on the surface of prostate cancer cells. Upon intravenous administration, the compound binds to PSMA-expressing tumor cells and is internalized, where the lutetium-177 delivers localized ionizing radiation, causing DNA damage and subsequent cell death. This modality, known as radioligand therapy (RLT), allows for the precise delivery of radiation to both primary tumors and metastatic lesions while sparing most healthy tissue. The platform includes several specific agents, most notably lutetium (177Lu) vipivotide tetraxetan (Pluvicto), and is being investigated across various stages of prostate cancer, including metastatic castration-resistant and hormone-sensitive disease.
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