Considering the role of hypoxia in cancer progression and poor prognosis, hypoxia-centric theranostic approaches may have immense potential in clinical cancer management. We have successfully developed a hypoxia-selective theranostic nanoplatform, which can be used to deliver a therapeutic dose of radiation to the hypoxic tumor tissue through systemic administration. In addition to delivering a radiation dose to the hypoxic tumor tissue, the versatile nanoplatform developed can also be used to load radiosensitizers or chemotherapeutic drugs to enhance the therapeutic effect.