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[177Lu]Lu-A9-0631 is a radioligand therapy (RLT) developed by Alpha-9 Oncology for the treatment of advanced solid tumors that express the Gastrin-Releasing Peptide Receptor (GRPR). The drug is composed of a high-affinity peptide ligand specific for GRPR, conjugated to the beta-emitting radioisotope Lutetium-177 (177Lu). GRPR is a G protein-coupled receptor that is frequently overexpressed in various malignancies, including prostate, breast, and colorectal cancers, while maintaining low expression in healthy tissues. Upon intravenous administration, [177Lu]Lu-A9-0631 selectively binds to GRPR-positive tumor cells, where the Lutetium-177 isotope delivers localized ionizing radiation, causing DNA damage and subsequent cell death. It is currently being investigated in Phase 1/1b clinical trials as part of a theranostic platform that includes alpha-emitting and imaging counterparts.
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