Proof of principle for the use of 11C-labelled peptides in tumour diagnosis with PET

G. Henriksen, M. Schottelius, T. Poethko, A. Hauser, I. Wolf, M. Schwaiger, Hans Jürgen Wester

Research output: Contribution to journalArticlepeer-review

29 Scopus citations

Abstract

Purpose: The future significance of peptide radiopharmaceuticals in diagnostic imaging with PET will be dependent on methodological aspects, as well as other requirements such as availability of the radionuclide and cost-effectiveness of its production. The aim of this study was to evaluate whether recent improvements in the modification of peptide pharmacokinetics by carbohydration may open a niche for the use of 11C-labelled peptide receptor binding tracers. Methods: A carbohydrated analogue of Tyr 3-octreotate was used as a clinically relevant peptide. Oxime-mediated coupling between 4-[11C]methoxy-benzaldehyde and an aminooxy-conjugated peptide precursor provided the 11C-labelled peptide in 21±5% decay-corrected yield (n=4) in a synthesis time of about 1 h. Results: In rat pancreas carcinoma xenografted mice, the compound displayed predominant and fast renal clearance combined with high tumour uptake (18.5±2.8% ID/g) at 30 min post injection. Corresponding values for kidney, liver and intestine were 18.5±2.4% ID/g, 3.2±0.5% ID/g and 2.1±0.3% ID/g, respectively. In a PET study with xenografted mice, the tumour (0.2-0.3 g) was clearly delineated as early as 20 min after injection. Somatostatin receptor (sstr)-specific uptake was demonstrated by reduction of tumour uptake to 20% of control by co-injection of TOC (0.4 mg/kg; 30 min p.i.). Conclusion: A 11C-labelled octreotate derivative has been prepared which shows suitable pharmacokinetics for in vivo imaging of sstr-overexpressing tumours and thus represents the first proof of principle for the potential of 11C-labelled peptides in tumour imaging.

Original languageEnglish
Pages (from-to)1653-1657
Number of pages5
JournalEuropean Journal of Nuclear Medicine and Molecular Imaging
Volume31
Issue number12
DOIs
StatePublished - Dec 2004

Keywords

  • Carbon-11
  • Octreotate
  • Octreotide
  • PET
  • Somatostatin receptor

Fingerprint

Dive into the research topics of 'Proof of principle for the use of 11C-labelled peptides in tumour diagnosis with PET'. Together they form a unique fingerprint.

Cite this