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

Mol Imaging Biol. 2015 Aug;17(4):565-74. doi: 10.1007/s11307-015-0850-8.

Abstract

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 (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).

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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Antigens, Surface / metabolism*
  • Feasibility Studies
  • Glutamate Carboxypeptidase II / metabolism*
  • Humans
  • Lysine / adverse effects
  • Lysine / analogs & derivatives*
  • Lysine / pharmacokinetics
  • Lysine / therapeutic use
  • Male
  • Middle Aged
  • Positron-Emission Tomography / methods*
  • Prostate / metabolism
  • Prostatic Neoplasms / diagnostic imaging*
  • Prostatic Neoplasms / metabolism
  • Radiometry
  • Tissue Distribution
  • Urea / adverse effects
  • Urea / analogs & derivatives*
  • Urea / pharmacokinetics
  • Urea / therapeutic use

Substances

  • 2-(3-(1-carboxy-5-((6-fluoropyridine-3-carbonyl)amino)pentyl)ureido)pentanedioic acid
  • Antigens, Surface
  • Urea
  • FOLH1 protein, human
  • Glutamate Carboxypeptidase II
  • Lysine