Summary In vivo molecular imaging has become a key technology for medical innovation, i.e., integrated live science, patho-physiological science, molecular evidence-based diagnosis, and innovative drug development. Rapid progress in life science in the latter half of the 20^th century brought the stage up to the living subjects, even functioning human beings. The invention of molecular imaging techniques such as PET/SPECT, MRI, and optical imaging, accelerated the paradigm shift in life science mostly from in vitro experimental system to live science in vivo, and also patho-physiological science in disease model animals to that realized in patients. When the biomarkers for early detection of signs toward diseases and also those for surrogate end-point were established and their changes could be followed by molecular imaging, it might be quite beneficial for preemptive medicine and evaluation of therapeutic outcome, especially the outcome of regenerative medicine. Recently, betaamyloid imaging and pancreatic beta-cell mass imaging have been highlighted for prediction of Alzheimer’s disease and diabetes mellitus, respectively. Such types of the valuable biomarkers related to the cause or influencing factors are also really important to develop the new drugs and preemptive medicine. In this sense, mutual collaboration between the research consortia in biomarker exploration and in molecular imaging would be of great value. Here, the concept, outline of our activities, pharmacokinetics studies, and preemptive medicine studies with efficient application of molecular imaging is presented.