In the Last decades, nanotechnology has provided novel and alternative methodologies and tools in the field of medical oncology, in order to tackle the issues regarding the control and treatment of cancer in modern society. In particular, the use of gold nanoparticles (AuNPs) in radiopharmaceutical development has provided various nanometric platforms for the delivery of medically relevant radioisotopes for SPECT/PET diagnosis and/or radionuclide therapy. In this review, we intend to provide insight on the methodologies used to obtain and characterize radiolabeled AuNPs while reporting relevant examples of AuNPs developed during the last decade for applications in nuclear imaging and/or radionuclide therapy, and highlighting the most significant preclinical studies and results.