Preliminary in vivo evaluation of [131I]-2-iodo-D-phenylalanine as a potential radionuclide therapeutic agent in R1M-fluc rhabdomyosarcoma tumor-bearing NuNu mice using bioluminescent imaging

Cancer Biother Radiopharm. 2010 Apr;25(2):225-31. doi: 10.1089/cbr.2009.0705.

Abstract

Background: Carrier-added [(123)I]-2-iodo-D-phenylalanine (CA [(123)I]-2-I-D-Phe) was previously found to have a preferential retention in tumors with a high tumor background contrast in animal models. A previous human dosimetry study demonstrated a favorable biodistribution and radiation burden in human subjects.

Aim: The aim of this study was to investigate the potential of CA [(131)I]-2-I-D-Phe as an agent for radionuclide therapy.

Methods: Sixty (60) nude athymic mice were inoculated subcutaneously with firefly luciferase-transduced R1M rhabdomyosarcoma cells. The mice in the therapy group were injected intravenously (i.v.) with 148 MBq [(131)I]-2-I-D-Phe (432 GBq/mmol) in kit solution. Controls were injected with kit solution without radioactivity, with physiological saline, or with 148 MBq [(131)I](-) in physiological saline. Tumor growth was quantified using bioluminescent imaging and caliper measurements.

Results: [(131)I]-2-I-D-Phe clearly reduced tumor growth in the treated mice compared with the control groups. A tumor growth-rate reduction of at least 33% was found for mice receiving a therapeutic dose. There were no serious adverse side-effects of the therapy.

Conclusions: In conclusion, i.v. injection of CA 148 MBq [(131)I]-2-I-D-Phe specifically reduces tumor growth in athymic nude mice without relevant side-effects on the animals' health.

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Humans
  • Iodine Radioisotopes*
  • Luciferases / metabolism*
  • Luminescent Measurements
  • Mice
  • Mice, Nude
  • Phenylalanine / analogs & derivatives*
  • Radionuclide Imaging
  • Radiopharmaceuticals*
  • Rhabdomyosarcoma / diagnostic imaging*
  • Tissue Distribution
  • Tumor Cells, Cultured
  • Xenograft Model Antitumor Assays

Substances

  • 2-iodophenylalanine
  • Iodine Radioisotopes
  • Radiopharmaceuticals
  • Phenylalanine
  • Luciferases