(UroToday.com) There has been a dramatic and rapid proliferation of systemic therapy options in advanced prostate cancer since the introduction of docetaxel for metastatic castration resistant prostate cancer (mCRPC) in 2004. These newer treatments have included a number of novel hormonal therapies (including abiraterone acetate and enzalutamide), second-line chemotherapy (cabazitaxel), bone-targeting agents (radium-223), and other targeted agents (including olaparib, rucaparib, and pembrolizumab), each of which has proven survival benefits. However, none of these agents have proven to be curative and there is, as a result, an ongoing need to identify novel treatment approaches. One of the approaches gaining the most interest is molecularly-targeted radionuclide therapy, leveraging molecularly targeting of cancer cells using prostate-specific membrane antigen (PSMA)-directed radioligands.