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99mTc-TPP-BBN is a dual-targeted radiopharmaceutical designed for the study of targeted radionuclide therapy (TRT) in prostate cancer. It consists of a technetium-99m (99mTc) radionuclide core conjugated to two distinct targeting moieties: a bombesin (BBN) derivative and a triphenylphosphonium (TPP) group. The BBN component targets the gastrin-releasing peptide receptor (GRPR), which is frequently overexpressed on the surface of prostate cancer cells, while the TPP component is a lipophilic cation that facilitates the accumulation of the complex within the mitochondria. Although 99mTc is primarily used for SPECT imaging, it also emits Auger electrons with a very short range, allowing for highly localized irradiation of sensitive cellular structures. In preclinical studies using PC3 human prostate cancer cells, 99mTc-TPP-BBN has been shown to induce significant DNA damage, micronuclei formation, and a reduction in cell survival, serving as a model for the development of organelle-specific radiotherapeutics.
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