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177Lu-AMBA is a targeted radiopharmaceutical designed for the systemic radiotherapy of cancers overexpressing the Gastrin-Releasing Peptide Receptor (GRP-R), such as prostate, breast, and lung cancers. It consists of the beta-emitting radioisotope Lutetium-177 complexed with a DO3A-based chelator and conjugated to a bombesin (BBN) peptide analog. As a GRP-R agonist, it binds with high affinity to the receptor, leading to internalization and the delivery of therapeutic ionizing radiation directly into the tumor cells. Developed by Bracco, it was primarily investigated for the treatment of hormone-refractory prostate cancer, though clinical development was eventually halted.
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