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Summary: Comparison of Four Bifunctional Chelates for Radiolabeling
Monoclonal Antibodies with Copper Radioisotopes: Biodistribution
and Metabolism
Buck E. Rogers,,#
Carolyn J. Anderson,*,
Judith M. Connett,
Li Wu Guo,
W. Barry Edwards,
Elizabeth L. C. Sherman,
Kurt R. Zinn,§,#
and Michael J. Welch
The Edward Mallinckrodt Institute of Radiology and Department of Surgery, Washington University School of
Medicine, St. Louis, Missouri 63110, and University of Missouri Research Reactor, Columbia, Missouri 65211.
Received March 22, 1996X
The bifunctional chelating agents (BFCs), 6-[p-(bromoacetamido)benzyl]-1,4,8,11-tetraazacyclotet-
radecane-1,4,8,11-tetraacetic acid (BAT), 6-[p-(isothiocyanato)benzyl]-1,4,8,11-tetraazacyclotetradecane-
1,4,8,11-tetraacetic acid (SCN-TETA), 4-[(1,4,8,11-tetraazacyclotetradec-1-yl)methyl]benzoic acid
(CPTA), and 1-[(1,4,7,10,13-pentaazacyclopentadec-1-yl)methyl]benzoic acid (PCBA), were synthesized
and conjugated to the anti-colorectal monoclonal antibody (mAb), 1A3, and antibody fragments, 1A3-
F(ab)2, for radiolabeling with 64,67Cu and comparison in animal models. In vivo metabolism studies
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