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Development of tyrosine-based radiotracer 99mTc-N4-Tyrosine for breast cancer imaging.

Abstract
The purpose of this study was to develop an efficient way to synthesize (99m)Tc-O-[3-(1,4,8,11-tetraazabicyclohexadecane)-propyl]-tyrosine ((99m)Tc-N4-Tyrosine), a novel amino acid-based radiotracer, and evaluate its potential in breast cancer gamma imaging. Precursor N4-Tyrosine was synthesized using a 5-step procedure, and its total synthesis yield was 38%. It was successfully labeled with (99m)Tc with high radiochemical purity (>95%). Cellular uptake of (99m)Tc-N4-Tyrosine was much higher than that of (99m)Tc-N4 and the clinical gold standard (18)F-2-deoxy-2-fluoro-glucose ((18)F-FDG) in rat breast tumor cells in vitro. Tissue uptake and dosimetry estimation in normal rats revealed that (99m)Tc-N4-Tyrosine could be safely administered to humans. Evaluation in breast tumor-bearing rats showed that although (99m)Tc-N4-Tyrosine appeared to be inferior to (18)F-FDG in distinguishing breast tumor tissue from chemical-induced inflammatory tissue, it had high tumor-to-muscle uptake ratios and could detect breast tumors clearly by planar scintigraphic imaging. (99m)Tc-N4-Tyrosine could thus be a useful radiotracer for use in breast tumor diagnostic imaging.
AuthorsFan-Lin Kong, Mohammad S Ali, Alex Rollo, Daniel L Smith, Yinhan Zhang, Dong-Fang Yu, David J Yang
JournalJournal of biomedicine & biotechnology (J Biomed Biotechnol) Vol. 2012 Pg. 671708 ( 2012) ISSN: 1110-7251 [Electronic] United States
PMID22496612 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)
Chemical References
  • Heterocyclic Compounds, 1-Ring
  • Organotechnetium Compounds
  • Radioactive Tracers
  • Radiopharmaceuticals
  • technetium Tc 99m cyclam
  • Fluorodeoxyglucose F18
  • Tyrosine
Topics
  • Animals
  • Cell Line, Tumor
  • Female
  • Fluorodeoxyglucose F18 (pharmacokinetics)
  • Heterocyclic Compounds, 1-Ring (chemical synthesis, pharmacokinetics)
  • Inflammation (diagnostic imaging, metabolism)
  • Mammary Neoplasms, Experimental (diagnostic imaging, metabolism)
  • Organotechnetium Compounds (chemical synthesis, pharmacokinetics)
  • Radiation Dosage
  • Radioactive Tracers
  • Radionuclide Imaging
  • Radiopharmaceuticals (chemical synthesis, pharmacokinetics)
  • Rats
  • Rats, Inbred F344
  • Tissue Distribution
  • Tyrosine (analogs & derivatives, pharmacokinetics)

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