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177Lu-rhPSMA-7.3 is a radiohybrid (rh) prostate-specific membrane antigen (PSMA)-targeted radiopharmaceutical developed for the treatment of prostate cancer. It consists of the rhPSMA-7.3 ligand, a small molecule peptidomimetic, labeled with the beta-emitting radioisotope Lutetium-177. The radiohybrid technology is unique in that it allows the same chemical entity to be labeled with either Fluorine-18 for PET imaging or radiometals like Lutetium-177 for therapy, ensuring identical biological behavior across diagnostic and therapeutic applications. 177Lu-rhPSMA-7.3 binds with high affinity to PSMA, a protein highly expressed on the surface of prostate cancer cells. Once bound and internalized, the Lutetium-177 isotope emits beta particles that cause lethal DNA damage to the tumor cells. Clinical data suggests it offers high tumor uptake and a favorable therapeutic index, potentially allowing for effective treatment with lower injected activities compared to other PSMA-targeted agents.
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