Effective cancer therapy with the alpha-particle emitter [211At]astatine in a mouse model of genetically modified sodium/iodide symporter-expressing tumors

Clin Cancer Res. 2006 Feb 15;12(4):1342-8. doi: 10.1158/1078-0432.CCR-05-1576.

Abstract

Purpose: The sodium/iodide symporter (NIS) gene is currently explored in several trials to eradicate experimental cancer with radiodine ((131)I) by its beta-emission. We recently characterized NIS-specific cellular uptake of an alternative halide, radioastatine ((211)At), which emits high-energy alpha-particles. The aim of this study was to investigate in vivo effects of the high linear energy transfer (LET) emitter (211)At on tumor growth and outcome in nude mice.

Experimental design: We administered radioastatide in a fractionated therapy scheme to NMRI nude mice harboring rapidly growing solid tumors established from a papillary thyroid carcinoma cell line genetically modified to express NIS (K1-NIS). Animals were observed over 1 year. Tumor growth, body weight, blood counts, survival, and side effects were measured compared with control groups without therapy and/or lack of NIS expression.

Results: Within 3 months, radioastatide caused complete primary tumor eradication in all cases of K1-NIS tumor-bearing nude mice (n = 25) with no tumor recurrence during 1 year follow-up. Survival rates of the K1-NIS/(211)At group were 96% after 6 months and 60% after 1 year, in contrast to those of control groups (maximum survival 40 days).

Conclusion: Our study indicates that (211)At represents a promising substrate for NIS-mediated therapy of various cancers either with endogenous or gene transfer-mediated NIS expression.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Astatine / adverse effects
  • Astatine / pharmacokinetics
  • Astatine / therapeutic use*
  • Atrophy
  • Cell Line, Tumor
  • Follow-Up Studies
  • Gene Expression
  • Humans
  • Liver / pathology
  • Liver / radiation effects
  • Mice
  • Mice, Inbred Strains
  • Mice, Nude
  • Neoplasms, Experimental / diagnostic imaging
  • Neoplasms, Experimental / metabolism
  • Neoplasms, Experimental / radiotherapy*
  • Radionuclide Imaging
  • Survival Analysis
  • Symporters / genetics
  • Symporters / metabolism*
  • Thyroid Gland / pathology
  • Thyroid Gland / radiation effects
  • Time Factors
  • Tissue Distribution
  • Transfection
  • Xenograft Model Antitumor Assays / methods

Substances

  • Symporters
  • sodium-iodide symporter
  • Astatine