Theranostics 2012; 2(5):523-540. doi:10.7150/thno.3582


Pretargeted Molecular Imaging and Radioimmunotherapy

David M. Goldenberg, Chien-Hsing Chang, Edmund A. Rossi, William J. McBride, Robert M. Sharkey

Center for Molecular Medicine and Immunology/Garden State Cancer Center, Morris Plains, NJ; Immunomedics, Inc., Morris Plains, NJ; IBC Pharmaceuticals, Inc., Morris Plains, NJ, USA.

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Goldenberg DM, Chang CH, Rossi EA, McBride WJ, Sharkey RM. Pretargeted Molecular Imaging and Radioimmunotherapy. Theranostics 2012; 2(5):523-540. doi:10.7150/thno.3582. Available from

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Pretargeting is a multi-step process that first has an unlabeled bispecific antibody (bsMAb) localize within a tumor by virtue of its anti-tumor binding site(s) before administering a small, fast-clearing radiolabeled compound that then attaches to the other portion of the bsMAb. The compound's rapid clearance significantly reduces radiation exposure outside of the tumor and its small size permits speedy delivery to the tumor, creating excellent tumor/nontumor ratios in less than 1 hour. Haptens that bind to an anti-hapten antibody, biotin that binds to streptavidin, or an oligonucleotide binding to a complementary oligonucleotide sequence have all been radiolabeled for use by pretargeting. This review will focus on a highly flexible anti-hapten bsMAb platform that has been used to target a variety of radionuclides to image (SPECT and PET) as well as treat tumors.

Keywords: bispecific antibody, cancer detection, pretargeting, radioimmunodetection, radioimmunotherapy.