Preparation, biological characterization and preliminary human imaging studies of ⁶⁸Ga-DOTA-IBA

In this study, DOTA-IBA was radiolabeled with ⁶⁸Ga and we determined the optimum labelling conditions and assessed the biological properties of ⁶⁸Ga-DOTA-IBA. We investigated the biodistribution of ⁶⁸Ga-DOTA-IBA in normal animals and undertook PET/CT imaging in humans. Finally, we explored the feasibility ⁶⁸Ga-DOTA-IBA as a bone imaging agent and demonstrated its potential for the therapeutic release of ¹⁷⁷Lu/²²⁵Ac-DOTA-IBA.

The controlled variables method was used to assess the impact of variables on the radiochemical purity of ⁶⁸Ga-DOTA-IBA. The biological properties of ⁶⁸Ga-DOTA-IBA were investigated.⁶⁸Ga-DOTA-IBA micro-PET/CT imaging was performed on animals. Volunteers were recruited for ⁶⁸Ga-DOTA-IBA imaging and data were compared to ^99mTc-MDP imaging studies to calculate the target to non-target ratio (T/NT) of the lesions.

The prepared ⁶⁸Ga-DOTA-IBA had a radiochemical purity of >97% and demonstrated good biological properties with a good safety profile in normal mice. PET/CT imaging of the animals showed rapid blood clearance with high contrast between the bone and stroma. Human imaging showed that ⁶⁸Ga-DOTA-IBA could detect more lesions compared to ^99mTc-MDP and had a higher targeted to untargeted ratio.

⁶⁸Ga-DOTA-IBA is an osteophilic radiopharmaceutical that can be synthesized using a simple labelling method. ⁶⁸Ga-DOTA-IBA has high radiochemical purity and is stable in vitro stability. It is rapidly cleared from the blood, has low toxicity and has strong targeting to the bone with long retention times. We also found that it is rapidly cleared in non-target tissues and has high contrast on whole-body bone imaging. ⁶⁸Ga-DOTA-IBA PET/CT has potential as a novel bone imaging bone modality in patients with metastatic disease.