Approaching 'kit-type' labelling with ⁶⁸Ga: The DATA chelators

Abstract The DATA chelators are a novel class of tri-anionic ligands based on 6-amino-1,4-diazepine-triacetic acid, which have been introduced recently for the chelation of ⁶⁸Ga. Compared with macrocyclic chelators based on the cyclen scaffold (i.e., DOTA, DO3A, and DO2A derivatives), DATA chelators undergo quantitative radiolabelling more rapidly and under milder conditions. In this study, a systematic evaluation of the labelling of four DATA chelators - DATA^M, DATA^P, DATA^Ph, and DATA^PPh - with ⁶⁸Ga is presented. The results highlight the extraordinary potential of this new class of chelators for application in molecular imaging using ⁶⁸Ga positron emission tomography (PET). Made easier with DATA: The development of kit-type labelling of ⁶⁸Ga radiopharmaceuticals is a crucial goal that has gathered momentum, with the desire for even simpler radiolabelling protocols and the development of GMP-compliant ⁶⁸Ge/⁶⁸Ga generators. The DATA chelators facilitate quantitative complexation of ⁶⁸Ga at ambient temperature quickly, simply, and efficiently - characteristics that have the potential to make the elusive ⁶⁸Ga labelling kit a reality.