Pharmacokinetics and experimental PET imaging of a bromine-76-labeled monoclonal anti-CEA antibody.
Bromine-76 is potentially useful as a radiolabel for monoclonal antibodies (MAbs) in PET imaging. The purpose of the present study was to evaluate the 76Br-labeled anticarcinoembryonic antigen (-CEA) MAb 38S1 as a tumor imaging agent in an experimental tumor model and to study the pharmacokinetics of 76Br-38S1 in comparison with 125I-38S1.


METHODS
Nude rats carrying human colon carcinoma xenografts were co-injected with directly labeled 76Br-38S1 and 125I-38S1. Biodistribution of labeled 38S1 was monitored for 4 days after administration, in the case of 76Br activity, including PET imaging. In addition, catabolism of radiolabeled MAbs was analyzed by gel filtration chromatography of blood plasma and homogenized tissues.


RESULTS
Tumor sites could be readily identified by PET imaging from 46 hr after administration of 76Br-38S1 and onwards. The concentration of 76Br activity in tumors, blood and most normal tissues was higher than the corresponding 125I concentration at all time points. This was mainly due to catabolism of radiolabeled MAb, resulting in free radiohalides, of which 76Br- was retained in contrast to the rapidly excreted 125I- ion.


CONCLUSIONS
Bromine-76-labeled anti-CEA MAbs may be applied for experimental tumor imaging with PET.
Lövqvist
A
A
University PET Center, Uppsala University, Sweden.
Sundin
A
A
Ahlström
H
H
Carlsson
J
J
Lundqvist
H
H
D000230:Adenocarcinoma / Q000000981:diagnostic imaging* / Q000378:metabolism; D000818:Animals; D000911:Antibodies, Monoclonal / Q000493:pharmacokinetics*; D001967:Bromine Radioisotopes / Q000493:pharmacokinetics*; D002272:Carcinoembryonic Antigen / Q000032:analysis*; D003110:Colonic Neoplasms / Q000000981:diagnostic imaging* / Q000378:metabolism; D004064:Digestive System / Q000378:metabolism; D006801:Humans; D007457:Iodine Radioisotopes / Q000493:pharmacokinetics*; D007668:Kidney / Q000378:metabolism; D008168:Lung / Q000378:metabolism; D008970:Molecular Weight; D018482:Muscle, Skeletal / Q000378:metabolism; D009368:Neoplasm Transplantation; D051381:Rats; D011923:Rats, Nude; D014018:Tissue Distribution; D014055:Tomography, Emission-Computed; D014183:Transplantation, Heterologous; D001743:Urinary Bladder / Q000378:metabolism
D000911:Antibodies, Monoclonal; D001967:Bromine Radioisotopes; D002272:Carcinoembryonic Antigen; D007457:Iodine Radioisotopes