Although management of advanced prostate cancer is evolving, a lot of work remains to be done for patients who have exhausted all options. Molecular targeting of prostate specific membrane antigen (PSMA) is valuable not only for diagnostic but also for therapeutic reasons. PSMA is thus considered to be useful in a theranostic approach. PSMA scans are upcoming diagnostic modalities which detect metastatic lesions that are missed by conventional imaging modalities. PSMA ligand therapy is also an upcoming treatment modality that has been proven to be beneficial with minimal toxicity in patients with advanced prostate cancer that have progressed on prior therapy. In this review article, we summarize the current knowledge regarding PSMA diagnostics and PSMA ligand therapies and discuss their implication in the treatment of advanced prostate cancer.