PSMA Theranostics

The prostate-specific membrane antigen (PSMA) (Fig. 1) is a very promising new molecular target for specific imaging and targeted therapy of prostate cancer because it is overexpressed on the cell surface of prostate cancer. PSMA expression is highly organ-specific, and the level of PSMA expression in prostate cancer cells is about 1000 times higher than the expression found in other tissues, such as the kidneys, small intestine, and brain. In view of high PSMA expression in almost all human prostate cancer types and further enhancement of its expression in poorly differentiated, metastatic, and hormone-refractory carcinomas, it has become a clinically useful target for developing PSMA-specific radiopharmaceuticals for precise diagnosis, staging, and treatment of prostate carcinoma. In addition, PSMA can be used as a vehicle to carry cytotoxic drugs specifically toward prostate cancer cells with low damage to adjacent healthy cells.