Targeting of renal carcinoma with 67/64Cu-labeled anti-L1-CAM antibody chCE7: selection of copper ligands and PET imaging.

Abstract

In order to optimize radiocopper labeling of anti-L1-CAM antibody chCE7, five bifunctional copper chelators were synthesized and characterized (CPTA-N-hydoxysuccinimide, DO3A-L-p-isothiocyanato-phenylalanine, DOTA-PA-L-p-isocyanato-phenylalanine, DOTA-glycyl-L-p-isocyanato-phenylalanine and DOTA-triglycyl-L-p-isocyanato-phenylalanine). Substitution with more than 11 chelators per antibody molecule was found to influence immunoreactivity and biodistributions of (67)Cu-MAb chCE7 significantly. CPTA-labeled antibody achieved the best tumor to normal tissue ratios when biodistributions of the different (67)Cu-chCE7 conjugates were assessed in tumor-bearing mice. High resolution PET imaging with (64)Cu-CPTA-labeled MAb chCE7 showed uptake in lymph nodes and heterogeneous distribution in tumor xenografts.

• Authors: Kurt Zimmermann, Jürgen Grünberg, Michael Honer, Simon Ametamey, P August Schubiger, Ilse Novak-Hofer
• Journal: Nuclear medicine and biology (Nucl Med Biol) Vol. 30 Issue 4 Pg. 417-27 (May 2003) ISSN: 0969-8051 [Print] United States
• PMID: 12767399 (Publication Type: Journal Article)

Chemical References

• Chelating Agents
• Copper Radioisotopes
• Ligands
• Radiopharmaceuticals

Topics

• Animals
• Carcinoma, Renal Cell (metabolism, radiotherapy)
• Chelating Agents (chemical synthesis, metabolism, pharmacokinetics)
• Copper Radioisotopes
• Kidney Neoplasms (metabolism, radiotherapy)
• Ligands
• Mice
• Radioimmunotherapy (methods)
• Radiopharmaceuticals (chemical synthesis, metabolism, pharmacokinetics)
• Structure-Activity Relationship
• Tissue Distribution
• Tomography, Emission-Computed