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The purpose of this Special Issue was to host research and review papers on Radiopharmaceuticals in line with the three previous Special Issues that I have Guest Edited for Molecules. This subject may vary from radioactive isotope production, the synthesis of precures, radioactive labeling reactions, to the purification of radiopharmaceuticals to quality control and regulatory efforts, which are required prior to using radiopharmaceuticals in humans. This Special Issue contains 17 original research papers, 1 communication, 5 reviews, and 1 editorial review all within the area of radiochemistry.