Radiolabeled enzyme inhibitors and binding agents targeting PSMA: Effective theranostic tools for imaging and therapy of prostate cancer

Because of the broad incidence, morbidity and mortality associated with prostate-derived cancer, the development of more effective new technologies continues to be an important goal for the accurate detection and treatment of localized prostate cancer, lymphatic involvement and metastases. Prostate-specific membrane antigen (PSMA; Glycoprotein II) is expressed in high levels on prostate-derived cells and is an important target for visualization and treatment of prostate cancer. Radiolabeled peptide targeting technologies have rapidly evolved over the last decade and have focused on the successful development of radiolabeled small molecules that act as inhibitors to the binding of the N-acetyl-l-aspartyl-l-glutamate (NAAG) substrate to the PSMA molecule. A number of radiolabeled PSMA inhibitors have been described in the literature and labeled with SPECT, PET and therapeutic radionuclides. Clinical studies with these agents have demonstrated the improved potential of PSMA-targeted PET imaging agents to detect metastatic prostate cancer in comparison with conventional imaging technologies. Although many of these agents have been evaluated in humans, by far the most extensive clinical literature has described use of the (68)Ga and (177)Lu agents. This review describes the design and development of these agents, with a focus on the broad clinical introduction of PSMA targeting motifs labeled with (68)Ga for PET-CT imaging and (177)Lu for therapy. In particular, because of availability from the long-lived (68)Ge (T1/2=270days)/(68)Ga (T1/2=68min) generator system and increasing availability of PET-CT, the (68)Ga-labeled PSMA targeted agent is receiving widespread interest and is one of the fastest growing radiopharmaceuticals for PET-CT imaging.

Nuclear medicine and biology. 2016 Aug 11 [Epub ahead of print]

Maroor Raghavan Ambikalmajan Pillai, Raviteja Nanabala, Ajith Joy, Arun Sasikumar, Furn F Russ Knapp

Molecular Group of Companies, Puthuvype, Ernakulam, Kerala, 682508, India. Electronic address: ., KIMS DDNMRC PET Scans, KIMS Hospital, Trivandrum, Kerala, India, 691601., Molecular Group of Companies, Puthuvype, Ernakulam, Kerala, 682508, India., Emeritus, Medical Radioisotope Program, Oak Ridge National Laboratory, Oak Ridge, TN, USA, 37830.

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