Receptor-mediated targeting of 67Ga-deferoxamine-folate to folate-receptor-positive human KB tumor xenografts.
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.
Mathias
C J
CJ
Department of Medical Chemistry, Purdue University, West Lafayette, Indiana 47907, USA.
Wang
S
S
Low
P S
PS
Waters
D J
DJ
Green
M A
MA
D000818:Animals; D014408:Biomarkers, Tumor / Q000138:chemical synthesis*; D002352:Carrier Proteins / Q000378:metabolism*; D003676:Deferoxamine / Q000031:analogs & derivatives* / Q000378:metabolism; D004307:Dose-Response Relationship, Radiation; D058973:Folate Receptors, GPI-Anchored; D005492:Folic Acid / Q000031:analogs & derivatives* / Q000378:metabolism; D005710:Gallium Radioisotopes; D006801:Humans; D007553:Isotope Labeling; D007624:KB Cells; D008297:Male; D051379:Mice; D008819:Mice, Nude; D019275:Radiopharmaceuticals / Q000378:metabolism*; D011956:Receptors, Cell Surface; D014018:Tissue Distribution
D014408:Biomarkers, Tumor; D002352:Carrier Proteins; D058973:Folate Receptors, GPI-Anchored; D005710:Gallium Radioisotopes; D019275:Radiopharmaceuticals; D011956:Receptors, Cell Surface; C099574:deferoxamine-gamma-folate conjugate; D005492:Folic Acid; D003676:Deferoxamine