Gallium-68 has gained substantial momentum since 2003 as a versatile radiometal that is extremely useful for application in the development of novel oncology targeting diagnostic radiopharmaceuticals. It is available through both generator produced radioactivity and via cyclotron production methods and can therefore be implemented in either small- or large-scale production facilities. It can also be implemented within different spectrum of infrastructure settings with relative ease. Whilst many of the radiopharmaceuticals are being development and investigated, which is summarized in this manuscript, [68Ga]Ga-SSTR2 and [68Ga]Ga-PSMA has prominence in current clinical guidelines. The novel tracer [68Ga]Ga-FAPi has also gained significant interest in the clinical context. A comparison of the labelling strategies followed to incorporate gallium-68 and fluorine-18 into the same molecular targeting constructs clearly demonstrate that gallium-68 complexation is the most convenient approach. Recently, cold kit based starting products are available to make the small-scale production of gallium-68 radiopharmaceuticals even more efficient when combined with generator produced gallium-68. The regulatory aspects is currently changing to support the implementation of gallium-68 and other diagnostic radiopharmaceuticals, simplifying the translation towards clinical use. Overall, the development of gallium-68 based radiopharmaceuticals is not only rapidly changing the landscape of diagnosis in oncology, but this growth also promotes innovation and progress in new applications of therapeutic radiometals such as lutetium-177 and actinium-225.
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