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161Tb-labeled gastrin analogue is a targeted radioligand therapy being evaluated for the treatment of advanced medullary thyroid cancer (MTC). It consists of a gastrin-derived peptide analogue, likely CP04 (a minigastrin derivative), conjugated to the therapeutic radioisotope terbium-161 (161Tb). The peptide component specifically targets and binds to the cholecystokinin-2 receptor (CCK2R), which is highly overexpressed in medullary thyroid carcinoma cells. Terbium-161 is a lanthanide isotope that provides therapeutic radiation through the emission of beta-minus particles, as well as a high yield of Auger and conversion electrons. This combination of radiation types may offer enhanced therapeutic efficacy, particularly for small tumor clusters and micrometastatic disease, by delivering high linear energy transfer radiation directly to the target cells.
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