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

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 (68)Ga for positron-emission-tomography (PET) or (177)Lu for radionuclide therapy.

In this literature review we evaluate the diagnostic value of (68)Ga PSMA PET/CT and the therapeutic potential of (177)Lu PSMA radioligand therapy (RLT) in patients with prostate cancer. (68)Ga 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 (177)Lu 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.

Expert review of molecular diagnostics. 2016 Sep 29 [Epub ahead of print]

Martin Barrio, Wolfgang P Fendler, Johannes Czernin, Ken Herrmann

a Department of Molecular and Medical Pharmacology , David Geffen School of Medicine at UCLA , Los Angeles , USA.