Copper (Cu) is an essential element for many cellular functions, including proliferation and angiogenesis. High serum Cu levels have been demonstrated in patients with neoplasia as well as high intra-tumoral Cu levels have been reported. Preclinical and clinical evidences suggest its use, in the form of 64Copper chloride (64CuCl<inf>2</inf>), as metabolic PET tracer in cancer diagnosis and therapy. Specifically, the use of 64CuCl<inf>2</inf> in human prostate cancer (PCa) evidenced a high uptake of 64CuCl<inf>2</inf> in tumoral prostate and involved regional lymph nodes in a staging setting and high sensitivity for local recurrence and lymph nodes detection in restaging, indicating its great potential. However, further and more solid clinical evidences are needed. On the other hand, 64CuCl<inf>2</inf> seems to be a promising radiometabolic drug with great cytotoxic abilities on PCa cells. We have collected the most recent and relevant findings on its potential uses and limitations for the study and treatment of PCa, together with its possible translation in daily clinical practice.