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177Lu-TRD4425 is a radiopharmaceutical therapeutic candidate consisting of the beta-emitting radioisotope Lutetium-177 conjugated to TRD4425, a targeting ligand directed against the Gastrin-Releasing Peptide Receptor (GRPR). GRPR is a G protein-coupled receptor that is frequently overexpressed in various solid tumors, including estrogen receptor-positive breast cancer and hormone-sensitive prostate cancer. The agent is designed for targeted radioligand therapy, where the TRD4425 ligand binds specifically to GRPR on the surface of tumor cells, facilitating the delivery of ionizing radiation directly to the malignant tissue to induce DNA damage and cell death. In clinical development, it is often evaluated as part of a theranostic pair alongside its gallium-68 labeled imaging counterpart, 68Ga-TRD4425, to identify patients with high GRPR expression who are most likely to benefit from the treatment.
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