Gallium-68-labeled DOTA-rhenium-cyclized alpha-melanocyte-stimulating hormone analog for imaging of malignant melanoma

Nucl Med Biol. 2007 Nov;34(8):945-53. doi: 10.1016/j.nucmedbio.2007.07.003. Epub 2007 Sep 4.

Abstract

Introduction: Diagnosis of malignant melanoma is critical, since a patient's prognosis is poor. Previous studies have shown that 64Cu- and 86Y-DOTA-ReCCMSH(Arg11) have the potential for early detection of malignant melanoma by exploiting the sensitivity and high resolution of positron emission tomography (PET). This encouraged us to investigate DOTA-ReCCMSH(Arg11) labeled with another beta+-emitting radionuclide, 68Ga.

Methods: DOTA-ReCCMSH(Arg11) was successfully labeled with 68Ga at pH 3.8-4 at 85 degrees C. Acute biodistribution and small-animal PET imaging studies were performed in mice bearing B16/F1 melanoma tumor.

Results: Biodistribution studies showed moderate receptor-mediated tumor uptake, fast nontarget organ clearance and high tumor to nontarget tissue ratios. Preadministration of d-lysine significantly reduced kidney uptake without affecting the uptake of the agent in the tumor. Small-animal PET images showed that the tumor could be clearly visualized at all time points examined (0.5-2 h) with the standardized uptake value analysis following a similar trend as the biodistribution data.

Conclusions: The preliminary data obtained suggest that 68Ga-DOTA-ReCCMSH(Arg11) is a promising PET imaging agent for early detection of malignant melanoma.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Female
  • Isotope Labeling / methods
  • Melanoma / diagnostic imaging*
  • Melanoma / metabolism*
  • Metabolic Clearance Rate
  • Mice
  • Mice, Inbred C57BL
  • Organ Specificity
  • Organometallic Compounds / pharmacokinetics*
  • Radionuclide Imaging
  • Radiopharmaceuticals / pharmacokinetics
  • Tissue Distribution
  • alpha-MSH / analogs & derivatives*
  • alpha-MSH / pharmacokinetics

Substances

  • 68Ga-1,4,7,10-tetraazacyclododecane 1,4,7,10-tetraacetic acid (ReO-acetyl(Cys(3,4,10),Phe(7),Arg(7))aplha-MSH(3-13))
  • Organometallic Compounds
  • Radiopharmaceuticals
  • alpha-MSH