Preparation of 211At-labeled humanized anti-Tac using 211At produced in disposable internal and external bismuth targets

Nucl Med Biol. 1998 Feb;25(2):89-93. doi: 10.1016/s0969-8051(97)00165-0.

Abstract

These studies describe the production and purification of 211At as well as the procedure for labeling humanized anti-Tac, the antibody to the alpha-chain of the IL-2 receptor (IL-2R alpha), which has been shown to be a useful target for immunotherapy. The optimized protocol combines the advantages of the two-stage dry distillation procedure with the astatination of trialkylstannyl substances as labeling compounds for proteins. The 211At was produced by bombarding either an external or a recently developed disposable internal bismuth target with alpha-particles from a Cyclotron Corporation CS-30 cyclotron. The 211At was found to contain less than 0.01% 210At. The production rate for the external target was 0.15 mCi +/- 0.056 microA(-1) h(-1) (n = 9) (5.55 MBq mcroA[-1] h[-1]). The production rate for the internal target was 0.44 +/- 0.14 mCi microA(-1) h(-1) (n = 16) (16.28 MBq mcroA[-1] h[-1]).

MeSH terms

  • Astatine / chemistry*
  • Bismuth / metabolism*
  • Chromatography, High Pressure Liquid
  • Cyclotrons
  • Drug Stability
  • Humans
  • Isotope Labeling / methods
  • Radioisotopes
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / pharmacology
  • Receptors, Interleukin-2 / metabolism*

Substances

  • Radioisotopes
  • Radiopharmaceuticals
  • Receptors, Interleukin-2
  • Bismuth
  • Astatine