Abstract: Radiopharmaceuticals could not only serve as effective diagnostic and therapeutic tools in human diseases, but also allow the assessment of metabolism and functional processes by providing quick, non-invasive and real-time visualization of physiological and pathological processes in the living humans at the molecular level together with PET (positron emission tomography) and SPECT (single photon emission computed tomography) imaging modalities. They could provide new methods and new approaches of truly early diagnosis and therapy and possible pathways for the preventative medicine, translational medicine and personalized medicine. The present review provides an overview of current status of in vivo radiopharmaceuticals in China. Moreover, some prospects of research and development of radiopharmaceuticals in the near future was discussed. The addressed future trends include the following aspects. (1) Production of medical radioisotopes including ⁹⁹Mo, ¹³¹I, ^188/186Re and ¹²³I. (2) Investigation on the basic radiopharmaceutical chemistry. (3) Development of receptor-based imaging agents. (4) Development of multi-modality imaging probes.