Receptor-mediated targeting of 67Ga-deferoxamine-folate to folate-receptor-positive human KB tumor xenografts

Nucl Med Biol. 1999 Jan;26(1):23-5. doi: 10.1016/s0969-8051(98)00076-6.

Abstract

The radiochemical synthesis and stability of 67Ga-deferoxamine-folate ([67Ga]Ga-DF-Folate) were examined as a function of DF-Folate concentration. Optimal labeling occurred at DF-Folate concentrations > or =2.5 microg/mL. To define the possible biological significance of variations in product formulation, the biodistribution of [67Ga]Ga-DF-Folate was examined as a function of administered deferoxamine-folate dose in an athymic mouse KB tumor model. The folate-receptor-positive KB tumors were found to concentrate the 67Ga radiolabel in a dose-dependent fashion, consistent with saturable involvement of the folate receptor in mediating tumor accumulation of the radiopharmaceutical.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Biomarkers, Tumor / chemical synthesis*
  • Carrier Proteins / metabolism*
  • Deferoxamine / analogs & derivatives*
  • Deferoxamine / metabolism
  • Dose-Response Relationship, Radiation
  • Folate Receptors, GPI-Anchored
  • Folic Acid / analogs & derivatives*
  • Folic Acid / metabolism
  • Gallium Radioisotopes
  • Humans
  • Isotope Labeling
  • KB Cells
  • Male
  • Mice
  • Mice, Nude
  • Radiopharmaceuticals / metabolism*
  • Receptors, Cell Surface*
  • Tissue Distribution

Substances

  • Biomarkers, Tumor
  • Carrier Proteins
  • Folate Receptors, GPI-Anchored
  • Gallium Radioisotopes
  • Radiopharmaceuticals
  • Receptors, Cell Surface
  • deferoxamine-gamma-folate conjugate
  • Folic Acid
  • Deferoxamine