Gallium-68: methodology and novel radiotracers for positron emission tomography (2012-2017)

Commercial Ge-68/Ga-68 generators provide a means to produce positron emission tomography agents on site without use of a cyclotron. This development has led to a rapid growth of academic literature and patents ongallium-68 (Ga-68). As Ga-68 positron emission tomography agents usually involve a targeting moiety attached to a metal chelator, the development lends itself to the investigation of theragnostic applications; the Ga-68-based diagnostic is utilized to determine if the biological target is present and, if so, a therapeutic isotope (e.g., Lu-177, Ac-225) can be complexed with the same scaffold to generate a corresponding radiotherapeutic. This review considers patents issued between 2012 and 2017 that contain a Ga-68-labeled molecule indexed by Chemical Abstract Services (a division of the American Chemical Society).