Nuclear medicine plays an irreplaceable role in the diagnosis, therapy, and prognosis of various diseases. Radiopharmaceuticals are the cornerstone of nuclear medicine; their systematic development could accelerate the innovation and clinical application of radiopharmaceuticals to ensure people's health. In this study, we conducted in-depth research on the literature on the research direction of radiopharmaceuticals, visited over 10 domestic universities, institutes, hospitals, and enterprises related to nuclear medicine, and invited experts to conduct consultation, exchange, and industry discussion, to grasp the development trend and pattern of the research and application of radiopharmaceuticals in a relatively comprehensive way. Based on the analysis of the current status, technical level, and trend of radiopharmaceuticals in China and abroad, the development status of radiopharmaceuticals in China is summarized and the urgent problems faced are identified. This study introduces the contents that need to be focused on from two aspects: the technology research and development (R&D) system and the technology supervision system, and proposes key technological breakthroughs including the study on radiopharmaceutical targets and development of targeted structures; new radio-labelling; automatic, intelligent, and large-scale controllable preparation of radiopharmaceuticals; detection and evaluation of radiation dose of radiopharmaceuticals; and combined diagnosis and therapy of radiopharmaceuticals. The study suggests to (1) encourage the innovative development of interdisciplinary integration with a clinical orientation; (2) accelerate the construction of a technological innovation system for radiopharmaceuticals; and (3) strengthen the construction of a professional team for the R&D of radioactive drugs, so as to promote the overall improvement of nuclear medicine.