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177Lu-NeoB (AAA603) is a Gastrin-Releasing Peptide Receptor (GRPR)-targeted radioligand therapy (RLT) developed by Advanced Accelerator Applications, a Novartis company. The drug consists of a high-affinity bombesin-derived peptide antagonist (NeoB) conjugated to the beta-emitting radioisotope Lutetium-177 (177Lu). GRPR is a G-protein coupled receptor frequently overexpressed in several solid tumors, including breast, prostate, and lung cancers. Upon intravenous administration, 177Lu-NeoB binds specifically to GRPR-expressing tumor cells, where the 177Lu isotope delivers localized ionizing radiation, inducing DNA double-strand breaks and subsequent apoptosis. It is currently being evaluated in Phase 1/2 clinical trials for the treatment of advanced solid tumors, with a particular focus on GRPR-positive breast cancer.
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