The fundamental foundation for precision medicine is accurate and specific targeting of cancer cells. Advances in the understanding of cancer biology, developments in diagnostic technologies, and expansion of therapeutic options have all contributed to the concept of personalized cancer care. Theranostics is the systematic integration of targeted diagnostics and therapeutics. The theranostic platform includes an imaging component that "sees" the lesions followed by administration of the companion therapy agent that "treats" the same lesions. This strategy leads to enhanced therapy efficacy, manageable adverse events, improved patient outcome, and lower overall costs. Radiotheranostics refers to the use of radionuclides for the paired imaging and therapy agents. Radioiodine is the classic radiotheranostic agent that has been used clinically in management of thyroid diseases for nearly 75 years. More recently there have been major exciting strides in radiotheranostics for neuroendocrine tumors and prostate cancer, among other conditions. Regulatory approval of a number of radiotheranostic pairs is anticipated in the near future. Continued support will be needed in research and development to keep pace with the current momentum in radiotheranostics innovations. Moreover, regulatory and reimbursement agencies need to streamline their requirements for seamless transfer of the radiotheranostic agents from the bench to the bedside. In this review, the concept, history, recent developments, current challenges, and outlook for radiotheranostics in the treatment of patients with cancer will be discussed. © RSNA, 2018.