Development and validation of a kit formulation of [⁶⁸Ga]Ga-P15-041 as a bone imaging agent

One of the commonly performed studies in nuclear medicine are bone scans with [^99mTc]Tc-methylene diphosphonate (MDP) for detecting various bone lesions, including cancer metastasis. The recent emergence of commercially available ⁶⁸Ge/⁶⁸Ga radionuclide generators makes it possible to provide ⁶⁸Ga-labelled bisphosphonates as positron emission tomography (PET) tracers for bone imaging. Preliminary human studies suggested that [⁶⁸Ga]Ga-HBED-CC-BP ([⁶⁸Ga]Ga-P15-041) in conjunction with PET/computed tomography (CT) showed accumulation in known bone lesions, fast clearance from blood and soft tissue, and an ability to provide high contrast images. A simple and efficient lyophilized P15-041 kit formulation for the rapid production of [⁶⁸Ga]Ga-P15-041 with excellent radiochemical purity (RCP) under ambient temperature without the need for purification is described. It is demonstrated that clinical doses of [⁶⁸Ga]Ga-P15-041 can be prepared manually within minutes with an excellent purity (> 90%) and readily meet the dose release criteria. When [⁶⁸Ga]Ga-P15-041 was evaluated in a patient with cancer, the imaging agent clearly showed accumulations in multiple lesions. In conclusion, [⁶⁸Ga]Ga-P15-041, prepared by a lyophilized kit, might be an excellent bone imaging agent for widespread clinical application.