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¹⁶¹Tb-PSMA-617 is a terbium-161-labeled radioligand therapy developed by Torpedo Pharmaceuticals for the treatment of metastatic castration-resistant prostate cancer (mCRPC). The drug utilizes the PSMA-617 ligand, which binds with high affinity to the prostate-specific membrane antigen (PSMA) expressed on the surface of prostate cancer cells. The ligand is conjugated to terbium-161 (¹⁶¹Tb), a radioisotope that emits beta particles, Auger electrons, and conversion electrons. This combination of emissions provides a higher linear energy transfer (LET) and a higher absorbed dose to small tumor clusters and single cells compared to traditional beta-emitters like lutetium-177. The short-range Auger electrons are particularly effective at inducing lethal DNA damage when the radioligand is internalized, potentially overcoming resistance mechanisms in advanced prostate cancer. It is currently undergoing Phase 1 clinical evaluation.
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