CONTEXT: Advanced prostate cancer (PCa) is a prominent cause of cancer death in men; positron emission tomography (PET) imaging may play a relevant role in detecting metastases and thus allowing a more tailored therapy in these patients. Radioligand therapy (RLT) may also gain relevance as a treatment strategy in advanced disease. OBJECTIVE: The aim of this review is to highlight how the recently developed theranostic processes may become a part of both the available diagnostic and the therapy arsenal in advanced PCa patients. EVIDENCE ACQUISITION: An expert panel of nuclear medicine physicians and a urologist, highly experienced in the fields of radionuclide imaging and RLT in advanced PCa, performed a nonsystematic review of the current indications, performance, limitations, and potential future developments of the currently available options in PCa theranostics. EVIDENCE SYNTHESIS: Among PET radiotracers, prostate-specific membrane antigen (PSMA)-based compounds in advanced PCa are the focus of a continuously growing interest, mostly due to their potential relevance as theranostic agents. The impact of PSMA-based PET/computed tomography imaging on treatment strategies and prognosis is promising, but still not unquestionably clear. Potential applications may include a role as a gatekeeper to PSMA-directed RLT, as well as monitoring the spread of systemic disease. Currently, initial results seem to substantiate the role of PSMA-directed RLT in terms of feasibility and efficacy. CONCLUSIONS: PSMA is a promising molecule for both imaging and therapy in advanced PCa patients; nevertheless, further studies are needed to investigate its role and to determine the impact of its side effects and its overall strategy outcome. PATIENT SUMMARY: Prostate-specific membrane antigen (PSMA), a protein, is highly expressed on prostate cancer cells. The possibility to perform diagnostic imaging and subsequently administer therapies by the means of the same molecule is called "theranostics". In patients with advanced prostate cancer, PSMA might have a role in detecting disease spread through both positron emission tomography and single-photon emission computed tomography imaging, while treating prostate cancer systemic localizations with radioligand therapy. Further studies are needed to better determine patients' risks and benefits of these therapeutic approaches.