Current Status of Radiolabeled Monoclonal Antibodies Targeting PSMA for Imaging and Therapy

Simple Summary The prostate-specific membrane antigen (PSMA) protein present in most prostate cancer cells has emerged as a promising target for the imaging and treatment of prostate cancer. With the development of monoclonal antibodies (mAbs) against PSMA, cancer cells can be targeted effectively while minimizing side effects to patients. Radioactivity can be attached to mAbs for imaging and treatment. This manuscript provides an overview of the current development and future prospects of radioactive mAbs conjugates targeting PSMA in prostate cancer. The current FDA approved PSMA radioligand therapy (PluvictoTM) faces some barriers in the form of frequent side-effects such as dry mouth. As a result, prostate cancer treatment based on radioactive mAbs conjugates hopes to reduce side-effects while still providing effective treatment to patients with prostate cancer.Abstract Prostate cancer (PCa) is one of the most prevalent cancer diagnoses among men in the United States and in several other developed countries. The prostate specific membrane antigen (PSMA) has been recognized as a promising molecular target in PCa, which has led to the development of specific radionuclide-based tracers for imaging and radiopharmaceuticals for PSMA targeted therapy. These compounds range from small molecule ligands to monoclonal antibodies (mAbs). Monoclonal antibodies play a crucial role in targeting cancer cell-specific antigens with a high degree of specificity while minimizing side effects to normal cells. The same mAb can often be labeled in different ways, such as with radionuclides suitable for imaging with Positron Emission Tomography (& beta;+ positrons), Gamma Camera Scintigraphy (& gamma; photons), or radiotherapy (& beta;- electrons, & alpha;-emitters, or Auger electrons). Accordingly, the use of radionuclide-based PSMA-targeting compounds in molecular imaging and therapeutic applications has significantly grown in recent years. In this article, we will highlight the latest developments and prospects of radiolabeled mAbs that target PSMA for the detection and treatment of prostate cancer.