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Technetium glucose complexes as potential cancer imaging agents.

Rosina Dapueto1, Rodrigo B Aguiar2, María Moreno3

  • 1Laboratorio de Radiofarmacia, Centro de Investigaciones Nucleares, Facultad de Ciencias, Universidad de la República, Mataojo 2055, 11400 Montevideo, Uruguay; Grupo de Química Medicinal, Laboratorio de Química Orgánica, Facultad de Ciencias-Facultad de Química, Universidad de la República, Iguá 4225, 11400 Montevideo, Uruguay.

Bioorganic & Medicinal Chemistry Letters
|August 31, 2015
PubMed
Summary

New technetium-99m labeled glucose analogs, (99m)Tc-IDAG and (99m)Tc-AADG), show promise as less expensive alternatives for cancer imaging. (99m)Tc-IDAG demonstrated significant tumor uptake in a melanoma model, suggesting its potential for SPECT imaging.

Keywords:
(18)F-FDGCancer imaging agentsGlucose complexesMelanomaTechnetium

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Area of Science:

  • Nuclear Medicine
  • Radiochemistry
  • Oncology

Background:

  • Over-expressed glucose transporters (GLUTs) in tumors enable detection via (18)F-FDG PET imaging.
  • Development of less expensive and more accessible SPECT imaging agents is needed.

Purpose of the Study:

  • To evaluate novel (99m)Tc-labeled glucose analogs, (99m)Tc-IDAG and (99m)Tc-AADG, as potential surrogates for (18)F-FDG in cancer imaging.
  • To assess the tumor uptake and biodistribution of these complexes in a melanoma model.

Main Methods:

  • Synthesis and radiolabeling of d-glucose ((99m)Tc-IDAG) and 2-d-deoxyglucose ((99m)Tc-AADG) complexes using iminodiacetic acid (IDA) and aminoacetate (AA) chelators.
  • In vitro cell uptake studies using B16 murine melanoma cells.
  • In vivo biodistribution and SPECT/micro-SPECT-CT imaging in melanoma-bearing C57BL/6 mice, with (18)F-FDG as a reference.

Main Results:

  • Both (99m)Tc-IDAG and (99m)Tc-AADG complexes were prepared with high yield and stability.
  • Maximum in vitro uptake was observed at 60 minutes for (99m)Tc-IDAG (6%) and (99m)Tc-AADG (2%).
  • (99m)Tc-IDAG showed significantly higher tumor uptake in vivo, with a tumor-to-muscle ratio of 12.1 ± 3.73 at 1 hour post-injection, and clear accumulation in SPECT images.

Conclusions:

  • The (99m)Tc-IDAG complex is a promising candidate for SPECT-based cancer imaging due to its favorable tumor uptake and retention.
  • This (99m)Tc-labeled glucose analog offers a potentially more accessible and cost-effective alternative to (18)F-FDG PET imaging for certain cancer types.