Korean J Nucl Med.  1998 Dec;32(6):516-524.

In Vitro Properties and Biodistribution of Tc-99m and Re-188 Labeled Monoclonal Antibody CEA79.4

Abstract

PURPOSE: Radiolabeled CEA79.4 antibody has a possibility to be used in radioimmunoscintigraphy or radioimmunotheraphy of cancer. We investigated the in vitro properties and biodistribution of CEA79.4 antibody labeled with Re-188 or Tc-99m.
MATERIALS AND METHODS
CEA79.4 was reduced by 2-mercaptoethanol to produce-SH reside, and was labeled with Re-188 or Tc-99m. For direct labeling of Tc-99m, methylene-diphosphonate was used as transchelating agent. CEA79.4 in 50 mM Acetate Buffered Saline (ABS, pH 5.3) was labeled with Re-188, using stannous tartrate as reducing agent. In order to measure immunoreactivity and the affinity constant of radiolabeled antibody, cell binding assay and Scatchard analysis using human colon cancer cells SNU-C4, were performed. Biodistribution study of labeled CEA79.4 was carried out at 1, 14 and 24 hr in ICR mice.
RESULTS
. Labeling efficiencies of Tc-99m and Re-188 labeled antibodies were 92.4+/-5.9% and 84.7+/-4.6%, respectively. In vitro stability of Tc-99m-CEA79.4 in human serum was higher than Re-188-CEA79.4. Immunoreactivity and affinity constant of Tc-99m-CEA79.4 were 59.2% and 6.59x109 M-1, respectively, while those of Re-188-CEA79.4 were 41.6% and 4.2x109 M-1, respectively. After 24 hr of administrations of Re-188 and Tc-99m labeled antibody, the remaining antibody, the remaining antibodies in blood were 6.32 and 9.35% ID/g respectively. The biodistribution of each labeled antibody in other organs was similar because they did not accumulate in non-targeted organs.
CONCLUSION
In vitro properties and biodistribution of Re-188-CEA79.4 were similar to those of Tc-99m-CEA79.4. It appears that Re-188-CEA79.4 can be used as a suitable agent for radioimmunotherapy.

Keyword

Direct labeling method; Re-188; antibody; Radioimmunotherapy; Generator; Immunoreactivity; Affinity constant
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