Gallium-68-labeled radiopharmaceuticals: a review

This review delves into the realm of gallium-68 (68Ga)-labeled radiopharmaceuticals. Over the last decade, 68Ga-labeled radiopharmaceuticals have gained prominence and shown tremendous growth in both preclinical evaluation and clinical translation due to their accessibility, favourable physical properties, and simple chemistry. Despite the high positron emission energy of 836 keV, it has been extensively used in diagnostic imaging. The present review aims to elucidate the status of various potential and clinically relevant 68Ga-labeled radiopharmaceuticals, as well as their preclinical and clinical stages. In this review article, we briefly discuss the physical characteristics, mode of production, suitable bifunctional chelators, and radiolabeling chemistry of 68Ga. Various 68Ga-labeled radiopharmaceuticals are discussed with respect to their biological targets, preclinical results, clinical results if available, and their current state of readiness for clinical translation and application in humans.