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[212Pb]-pentixather is an experimental radioligand therapy consisting of the molecule pentixather labeled with the alpha-emitting radionuclide lead-212.[1][3][7] It is designed to target the chemokine receptor CXCR4, which is highly expressed on various types of cancer cells, including neuroendocrine tumors and small-cell lung cancer.[1][4][7] Upon binding to CXCR4, [212Pb]-pentixather delivers targeted alpha particle radiation directly to malignant cells, leading to localized DNA damage and cell death.[4][7] Its primary indication under investigation is the treatment of tumors that express CXCR4, such as atypical carcinoid tumors and small-cell lung cancer, with ongoing phase 1 clinical trials assessing safety and dosimetry.[1][3] The drug is administered intravenously and is part of a broader platform of CXCR4-targeted radiopharmaceuticals, where pentixather can be labeled with different isotopes for either diagnostic or therapeutic purposes.[7]
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