Abstract: Cherenkov light is a luminescence phenomenon during the decay of radionuclides. Cherenkov light can be directly captured by the camera to achieve Cherenkov luminescence imaging and is expected to be used for intraoperative navigation. In addition, Cherenkov light has also been applied as a source of light to activate nanoparticles for photodynamic therapy. However, due to its low photon production yield, the application of Cherenkov light in biomedicine is still limited. To meet the above challenges, Cherenkov light activable nanomedicine has been developed in the last few years, shedding the light on the future application of Cherenkov light in biomedical research.