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161Tb-PNT6555 is a radiopharmaceutical theranostic agent developed by POINT Biopharma (now a subsidiary of Eli Lilly) for the treatment of solid tumors expressing fibroblast activation protein-alpha (FAP). The agent consists of a FAP-targeting small molecule ligand (Bz-D-Ala-boroPro) conjugated to a DOTA chelator and radiolabeled with the isotope terbium-161. FAP is a transmembrane glycoprotein highly upregulated on cancer-associated fibroblasts (CAFs) within the tumor microenvironment of many epithelial cancers, making it a pan-cancer target. Terbium-161 is a unique radionuclide that emits both beta particles and Auger electrons; the latter provide high linear energy transfer over a very short range, which may enhance therapeutic efficacy against small tumor clusters and micrometastases compared to traditional beta-emitters like lutetium-177.
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