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The aim of this study is to verify the in vivo stability, to determine the biodistribution and to estimate the unspecific radiotoxicity of an (211)At-labelled CD33-antibody ((211)At-antiCD33) in mice with a view to therapeutic application in treating leukaemia. METHODS (211)At was produced via the (209)Bi(a,2n)(211)At reaction and was linked via 3-(211)At-succinimidyl-benzoate to the antiCD33-antibody. The biodistribution and the in vivo stability in serum were determined after i.v.-injection in NMRI nu/nu-mice. For toxicity experiments, mice received either three times 315-650 kBq (211)At-antiCD33 or unlabelled antibody and NaCl-solution respectively. RESULTS (211)At-antiCD33 showed a characteristic biodistribution complying with the unspecific antibody retention in the reticular endothelial system. The largest proportion of radioactivity remained in blood and blood-rich tissues with a minor accumulation in the thyroid and stomach. After 21 h, >85% of activity in serum still represented intact antibody. Mice showed no difference in unspecific toxicity of (211)At-labelled antibodies over six months compared to those treated with unlabelled antibody and NaCl-solution respectively, with regard to histopathologic lesions, survival time, behaviour and haemograms. CONCLUSIONS The radiolabelling method yielded adequate in vivo stability of (211)At-antiCD33. Biodistribution with rapid elimination of free (211)At via kidneys and urine complies with requirements for targeted therapy. Activity doses potentially required for treatment do not elicit radiotoxicity to normal organs in mice. Further development is required to enhance the apparent specific activity and to verify the efficacy in an adequate animal model before phase I clinical studies in leukaemia can be envisaged.
Almut Walte, and
S Sriyapureddy, and
D Krull, and
T Petrich, and
G-J Meyer, and
W H Knapp
June 1996,
International journal of oncology,
Almut Walte, and
S Sriyapureddy, and
D Krull, and
T Petrich, and
G-J Meyer, and
W H Knapp
February 2004,
Basic & clinical pharmacology & toxicology,
Almut Walte, and
S Sriyapureddy, and
D Krull, and
T Petrich, and
G-J Meyer, and
W H Knapp
January 1980,
Zeitschrift fur Versuchstierkunde,
Almut Walte, and
S Sriyapureddy, and
D Krull, and
T Petrich, and
G-J Meyer, and
W H Knapp
September 1985,
The Journal of urology,
Almut Walte, and
S Sriyapureddy, and
D Krull, and
T Petrich, and
G-J Meyer, and
W H Knapp
January 1982,
Progress in clinical and biological research,
Almut Walte, and
S Sriyapureddy, and
D Krull, and
T Petrich, and
G-J Meyer, and
W H Knapp
March 1974,
Acta pathologica et microbiologica Scandinavica. Section A, Pathology,
Almut Walte, and
S Sriyapureddy, and
D Krull, and
T Petrich, and
G-J Meyer, and
W H Knapp
July 1989,
Strahlentherapie und Onkologie : Organ der Deutschen Rontgengesellschaft ... [et al],
Almut Walte, and
S Sriyapureddy, and
D Krull, and
T Petrich, and
G-J Meyer, and
W H Knapp
January 1987,
Urologia internationalis,
Almut Walte, and
S Sriyapureddy, and
D Krull, and
T Petrich, and
G-J Meyer, and
W H Knapp
January 1984,
The Journal of urology,
Almut Walte, and
S Sriyapureddy, and
D Krull, and
T Petrich, and
G-J Meyer, and
W H Knapp
April 1996,
International journal of radiation oncology, biology, physics,
