Radioisotope‐Labeled Nanomedicines for Cancer Therapy: Recent Advances, Synergistic Strategies, and Future Challenges

ABSTRACT Radioisotope therapy (RIT), a form of internal radiotherapy, eliminates tumors at close range through the emission of α particles, β particles, or Auger electrons during radionuclide decay. It has been extensively applied in the treatment of advanced localized cancers. However, the precise delivery of radionuclides to tumor sites is essential to ensure both the safety and efficacy of RIT. Additionally, intrinsic or acquired tumor resistance can significantly compromise therapeutic outcomes. In recent decades, nanocarriers have been widely investigated for radioisotope delivery, enabling the development of diverse radionuclide‐labeled nanomaterials and innovative cancer treatment strategies. This review summarizes therapeutic radioisotopes emitting α, β, or Auger particles and highlights various radionuclide‐labeled nanomedicines, including inorganic nanoparticles, organic nanoparticles, and metal–organic frameworks (MOFs). We further discuss the integration of RIT with other modalities, such as chemotherapy, immunotherapy, hyperthermia, and photodynamic therapy, using nanomedicines. Finally, we outline the future prospects and challenges associated with the development and clinical translation of radionuclide‐labeled nanomedicines.