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177Lu-DOTA-Pol3026 is a preclinical-stage therapeutic radiopharmaceutical (targeted radionuclide therapy) being developed by the Belgian Nuclear Research Centre (SCK CEN) and the University of Liège for the treatment of glioblastoma. It consists of the beta-hairpin peptidomimetic CXCR4 antagonist POL3026 conjugated to the chelator DOTA and radiolabeled with the beta-emitting radionuclide lutetium-177 (177Lu). 177Lu-DOTA-Pol3026 selectively binds to C-X-C chemokine receptor type 4 (CXCR4), which is highly expressed in glioblastoma and glioblastoma cancer stem cells, delivering localized ionizing radiation to induce DNA double-strand breaks and tumor cell apoptosis.
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