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[177Lu]Lu-FAP-2886 is a targeted radioligand therapy (RLT) comprising the beta-emitting radioisotope lutetium-177 conjugated to FAP-2886, a peptide ligand with high affinity for Fibroblast Activation Protein (FAP). FAP is a cell-surface serine protease that is significantly upregulated in the tumor microenvironment, specifically on cancer-associated fibroblasts (CAFs) and certain malignant cells like those in glioblastoma, while remaining largely absent in healthy adult tissues. By binding to FAP, [177Lu]Lu-FAP-2886 delivers ionizing radiation directly to the tumor site, causing lethal DNA damage to both the cancer cells and the supportive stroma. Developed by Perceptive, this agent is being investigated for its potential to treat aggressive solid tumors, including glioblastoma, where it has shown preclinical efficacy in xenograft models.
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