Toward 18 F-Labeled Theranostics: A Single Agent that Can Be Labeled with 18 F, 64 Cu, or 177 Lu

Chembiochem. 2020 Apr 1;21(7):943-947. doi: 10.1002/cbic.201900632. Epub 2019 Dec 4.

Abstract

We report a single-molecule radiotracer that can be labeled independently with 18 F-fluoride or radiometals (64 Cu, 177 Lu) in a single step. A prostate-specific membrane antigen (PSMA)-targeting ligand, armed with both an organotrifluoroborate and a metal-chelator (DOTA), was designed to optionally afford 18 F-, 64 Cu- or 177 Lu-labeled products that were injected into mice bearing prostate cancer (LNCaP) xenografts. PET/CT images and ex vivo biodistribution data show high, specific tumor uptake irrespective of which radionuclide is used, thereby demonstrating a new approach to combining, in a single molecule, 18 F-labeling capabilities for PET imaging with radiometalation for potential imaging and therapeutic applications.

Keywords: 18F labeling; peptides; radiotracers; theranostics.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antigens, Surface / chemistry
  • Cell Line, Tumor
  • Copper Radioisotopes / chemistry
  • Fluorine Radioisotopes / chemistry
  • Glutamate Carboxypeptidase II / chemistry
  • Heterocyclic Compounds, 1-Ring / chemistry
  • Humans
  • Ligands
  • Lutetium / chemistry
  • Male
  • Mice
  • Positron Emission Tomography Computed Tomography
  • Precision Medicine*
  • Prostatic Neoplasms / diagnostic imaging
  • Prostatic Neoplasms / pathology
  • Radioisotopes / chemistry
  • Radiopharmaceuticals / chemistry*
  • Radiopharmaceuticals / metabolism
  • Tissue Distribution
  • Transplantation, Heterologous

Substances

  • Antigens, Surface
  • Copper Radioisotopes
  • Copper-64
  • Fluorine Radioisotopes
  • Heterocyclic Compounds, 1-Ring
  • Ligands
  • Radioisotopes
  • Radiopharmaceuticals
  • 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
  • Lutetium
  • Lutetium-177
  • FOLH1 protein, human
  • Glutamate Carboxypeptidase II
  • Fluorine-18