[Direct and indirect labeling with 99mTc of an antireceptor monoclonal antibody of EGF]

Radiolabeled monoclonal antibodies (MAbs) have been a useful tool for diagnostic imaging and therapy in Oncology. The aim of this study was to carry out the indirect 99mTc radiolabeling of ior egf/r3, monoclonal antibody (MAb) specific for epidermal growth factor (EGF) receptor, and the comparison with a direct 99mTc radiolabeling approach.

Cyclic anhydride of the diethylenetriaminepentaacetic acid (ADTPA) was employed as bifunctional chelating agent in the indirect monoclonal antibody radiolabeling and it was coupled to MAb at molar ratios of 20:1, 50:1 and 200:1 (ADTPA:MAb). For the direct radiolabeling, the reduction of MAb was performed with 2-mercaptoethanol (2ME), based on Schwarz's method. Biological activity was measured by Flow Cytometry. Biodistribution studies were performed at 1, 3 and 24 h after injection of the radiolabeled antibody in Wistar rats.

After 30 min of 99mTc radiolabeling of the ior egf/r3 MAb, the radiochemical purity values were between 80.0 +/- 1.8 and 90.0 +/- 1.2 % for the indirect method using ADTPA, while it was 94.8 +/- 1.6 % for the direct approach using 2ME. Stability of the 99mTc-radiopharmaceuticals was similar for both methods. The biological activity was similar for both antibody formulations. There were no significant differences for the biodistribution to normal organs for both radiolabeled antibodies.

Use of ADTPA was shown to be an efficient method for the 99mTc labeling of the monoclonal antibody ior egf/r3. Radiolabeling using 2ME showed higher radiochemical purity.