Copper-64-labeled antibodies for PET imaging

J Nucl Med. 1992 Sep;33(9):1685-91.

Abstract

In the imaging of tumors using radiolabeled monoclonal antibodies, the use of PET gives increased sensitivity over conventional gamma camera imaging techniques. Copper-64, a positron-emitting radionuclide, has been labeled to 1A3, an anticolorectal carcinoma monoclonal antibody, and its fragments 1A3-F(ab')2 utilizing the bifunctional chelate Br-benzyl-TETA. The 64Cu-labeled intact 1A3 and 1A3-F(ab')2 have been evaluated as potential imaging agents for PET. Biodistribution studies of 64Cu-benzyl-TETA-1A3 and 64Cu-benzyl-TETA-1A3-F(ab')2 in tumor-bearing hamsters were compared with those of 111In-Br phi HBED-1A3, 111In-Br phi HBED-1A3-F(ab')2 and 125I-labeled intact 1A3 and 1A3-F(ab')2. Tumor uptake of 64Cu-labeled intact 1A3 and fragments in the hamster model was superior to both 111In- and 125I-labeled intact 1A3 and fragments. Human dosimetry data for 64Cu- and 123I-labeled 1A3 and 1A3-F(ab')2 were calculated from biodistribution data in rats. High kidney uptake of 64Cu-benzyl-TETA-1A3-F(ab')2 precludes clinical study at this time; however, the data shows that 64Cu-benzyl-TETA-1A3 would be suitable for positron tomography imaging of colorectal cancer in patients.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Antibodies, Monoclonal*
  • Chelating Agents
  • Colonic Neoplasms / diagnostic imaging*
  • Copper Radioisotopes*
  • Cricetinae
  • Edetic Acid / analogs & derivatives
  • Female
  • Heterocyclic Compounds
  • Humans
  • Immunoglobulin Fab Fragments*
  • Indium Radioisotopes
  • Iodine Radioisotopes
  • Male
  • Mesocricetus
  • Rats
  • Rats, Inbred Strains
  • Tomography, Emission-Computed / methods*

Substances

  • Antibodies, Monoclonal
  • Chelating Agents
  • Copper Radioisotopes
  • Heterocyclic Compounds
  • Immunoglobulin Fab Fragments
  • Indium Radioisotopes
  • Iodine Radioisotopes
  • 6-(4-bromoacetamidobenzyl)-1,4,8,11-tetraazacyclotetradecane-N,N',N'',N'''-tetraacetic acid
  • N,N'-bis(5-bromo-2-hydroxybenzyl)ethylenediamine diacetic acid
  • Edetic Acid