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

• Published in: Molecular imaging and biology Vol. 17; no. 4; pp. 565 - 574
• Main Authors: Szabo, Zsolt, Mena, Esther, Rowe, Steven P., Plyku, Donika, Nidal, Rosa, Eisenberger, Mario A., Antonarakis, Emmanuel S., Fan, Hong, Dannals, Robert F., Chen, Ying, Mease, Ronnie C., Vranesic, Melin, Bhatnagar, Akrita, Sgouros, George, Cho, Steve Y., Pomper, Martin G.
• Format: Journal Article
• Language: English
• Published: New York Springer US 01.08.2015; Springer Nature B.V
• Subjects: Aged; Antigens, Surface - metabolism; Feasibility Studies; Glutamate Carboxypeptidase II - metabolism; Humans; Imaging; Lysine - adverse effects; Lysine - analogs & derivatives; Lysine - pharmacokinetics; Lysine - therapeutic use; Male; Medicine; Medicine & Public Health; Middle Aged; Positron-Emission Tomography - methods; Prostate - metabolism; Prostatic Neoplasms - diagnostic imaging; Prostatic Neoplasms - metabolism; Radiology; Radiometry; Research Article; Tissue Distribution; Urea - adverse effects; Urea - analogs & derivatives; Urea - pharmacokinetics; Urea - therapeutic use; Molecular imaging; PSMA; Fluorine-18; Prostate cancer; PET
• ISSN: 1536-1632; 1860-2002
• DOI: 10.1007/s11307-015-0850-8

Purpose 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. Procedures 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. Results 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 (SUV max 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). Conclusions [ 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.