Prostate-specific membrane antigen (PSMA) is a type II integral membrane glycoprotein, specifically expressed in prostatic epithelial cells and strongly upregulated in prostate cancer. PSMA is also present in the neovasculature of other solid tumors. These findings have spurred the development of PSMA-targeted therapies for prostate cancer, including immunotherapy, radioimmunotherapy, chemotherapy and gene therapy, and initiated the clinical trials of the first-generation products. However, general clinical application of these therapies still requires extensive clinical studies to test their clinical safety, stability and efficacy.