Gallium-68-labeled radiopharmaceuticals: a review

Abstract

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.