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177Lu-DOTA-IBA is a theranostic radiopharmaceutical developed for the treatment of bone metastases from various solid tumors. It consists of the beta-emitting radioisotope Lutetium-177 (177Lu) complexed with the chelating ligand DOTA-ibandronic acid. The ibandronic acid moiety, a third-generation nitrogen-containing bisphosphonate, provides high-affinity targeting to hydroxyapatite in the bone matrix, specifically at sites of active bone remodeling and metastatic activity. Once localized to the bone lesions, the 177Lu isotope delivers targeted ionizing radiation, inducing DNA damage and apoptosis in tumor cells and osteoclasts. This dual mechanism provides both pain palliation and anti-tumor effects. 177Lu-DOTA-IBA is typically used as part of a theranostic pair with 68Ga-DOTA-IBA, which allows for PET/CT-based patient selection and treatment response monitoring using parameters such as metabolic tumor volume (MTV).
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