Prostate specific membrane antigen (PSMA) ligands for diagnosis and therapy of prostate cancer.

INTRODUCTION: Prostate specific membrane antigen (PSMA) has become an attractive diagnostic and therapeutic target for small molecule ligands. Radionuclide-chelating ligands can be labeled with either 68Ga for positron-emission-tomography (PET) or 177Lu for radionuclide therapy. Areas covered: In this literature review we evaluate the diagnostic value of 68Ga PSMA PET/CT and the therapeutic potential of 177Lu PSMA radioligand therapy (RLT) in patients with prostate cancer. 68Ga PSMA PET/CT is more accurate than CT for nodal staging and superior to conventional imaging in patients with biochemical recurrence, translating into major changes in clinical management. The preliminary data for 177Lu PSMA indicates >50% reduction of PSA levels in up to 59% of patients. Severe adverse events occurred <10% of patients after RLT. Expert commentary: PSMA ligands for diagnostic and therapeutic purpose will significantly impact the management of patients with prostate cancer.