lutetium (177Lu) zavadotide guraxetan

Lutetium (177Lu) zavadotide guraxetan is a targeted radiopharmaceutical developed by the Norwegian University of Science and Technology (NTNU) for the treatment of recurrent glioma, specifically glioblastoma multiforme. It consists of a modified version of the neuropeptide Substance P (zavadotide) conjugated to a DOTA-derived chelator (guraxetan) and labeled with the beta-emitting radioisotope Lutetium-177. The drug targets the neurokinin-1 receptor (NK1R), which is significantly overexpressed in high-grade gliomas compared to healthy brain tissue. Upon binding to NK1R on the surface of tumor cells, the compound is internalized, allowing the localized delivery of ionizing radiation to induce DNA damage and cell death in the malignant cells while sparing surrounding healthy tissue. It is typically administered locally into the tumor or the resection cavity to maximize the therapeutic index and minimize systemic exposure.

Other names

lutetium-177 zavadotide guraxetanlutetium177 zavadotide guraxetanlutetium 177 zavadotide guraxetan177Lu-zavadotide guraxetanLutetium-177 DOTA-Substance PLutetium177 DOTA-Substance PLutetium 177 DOTA-Substance P