114mIn, a candidate for radionuclide therapy: low-energy cyclotron production and labeling of DTPA-D-phe-octreotide

Nucl Med Biol. 2000 Feb;27(2):183-8. doi: 10.1016/s0969-8051(99)00096-7.

Abstract

A method for production of carrier-free (114m)In (half-life 49.5 days), which is a potential radionuclide for radionuclide therapy of slowly growing tumors, is presented. A target consisting of five enriched cadmium ((114)Cd) foils, each 50 microm thick, was irradiated by protons (from 12.6-6.5 MeV) giving a target yield of 0. 8 MBq/microAh. A simple and cost-efficient thermal diffusion method was used for the separation. The irradiated target foils were heated for 2 h at 306 degrees C and then etched in 0.05 M HCl. The obtained cadmium/indium solution was purified using a cation ion-exchange resin (AG 1 x 8, Bio-Rad Laboratories, Hercules, CA USA). An overall yield of approximately 60% was obtained, whereas the loss of the target material was <1% per separation cycle. The (114m)In production gave (114m)In with high specific radioactivity and was successfully used to label diethylenetriamine pentaacetic acid (DTPA)-D-Phe-octreotide. Furthermore, no difference in biodistribution between [(114m)In]- and [(111)In]-DTPA-D-Phe(1)-octreotide in tumor-bearing nude mice was seen. The high radionuclide uptake in the tumors indicates a good receptor binding of the labeled octreotide.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cadmium Radioisotopes
  • Cyclotrons
  • Indium Radioisotopes / therapeutic use
  • Isotope Labeling
  • Mice
  • Mice, Nude
  • Neuroendocrine Tumors / radiotherapy*
  • Octreotide / analogs & derivatives*
  • Octreotide / chemical synthesis
  • Octreotide / pharmacokinetics
  • Octreotide / therapeutic use
  • Pentetic Acid / analogs & derivatives*
  • Pentetic Acid / chemical synthesis
  • Pentetic Acid / pharmacokinetics
  • Pentetic Acid / therapeutic use
  • Protons
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / pharmacokinetics
  • Radiopharmaceuticals / therapeutic use*
  • Tissue Distribution

Substances

  • Cadmium Radioisotopes
  • Indium Radioisotopes
  • Protons
  • Radiopharmaceuticals
  • SDZ 215-811
  • Pentetic Acid
  • Octreotide