Initial Evaluation of [18F]DCFPyL for Prostate-Specific Membrane Antigen (PSMA)-Targeted PET Imaging of Prostate Cancer

• DOI: 10.1007/s11307-015-0850-8
• Publication Date: 2015-04-20T09:17:38Z
• Authors: Zsolt Szabo; Esther Mena; Steven P. Rowe; Donika Plyku; Rosa Nidal; Mario A. Eisenberger; Emmanuel S. Anton...; Hong Fan; Robert F. Dannals; Ying Chen; Ronnie C. Mease; Melin Vranesic; Akrita Bhatnagar; George Sgouros; Steve Y. Cho; Martin G. Pomper
• Keywords: Biodistribution; Glutamate carboxypeptidase II

Prostate-specific membrane antigen (PSMA) is a recognized target for imaging prostate cancer. Here we present initial safety, biodistribution, and radiation dosimetry results with [(18)F]DCFPyL, a second-generation fluorine-18-labeled small-molecule PSMA inhibitor, in patients with prostate cancer.Biodistribution was evaluated using sequential positron-emission tomography (PET) scans in nine patients with prostate cancer. Time-activity curves from the most avid tumor foci were determined. The radiation dose to selected organs was estimated using OLINDA/EXM.No major radiotracer-specific adverse events were observed. Physiologic accumulation was observed in known sites of PSMA expression. Accumulation in putative sites of prostate cancer was observed (SUVmax up to >100, and tumor-to-blood ratios up to >50). The effective radiation dose from [(18)F]DCFPyL was 0.0139 mGy/MBq or 5 mGy (0.5 rem) from an injected dose of 370 MBq (10 mCi).[(18)F]DCFPyL is safe with biodistribution as expected, and its accumulation is high in presumed primary and metastatic foci. The radiation dose from [(18)F]DCFPyL is similar to that from other PET radiotracers.