A DOTA analog containing a weak Michael acceptor group (a maleimide group; AmMABD) was utilized to covalently bind through a cysteine moiety to peptides that could be fused to tumor-binding antibody. Tumor targeting antibodies, known for their poor pharamcokinetics, are conjugated to the cysteine containing peptide and administered prior to the radiolabeled DOTA analog and allowed to accumulate at the tumor sites. A subsequent injection of radiolabeled DOTA analog with high affinity to the cysteine containing peptide linked to the antibody allows in vivo targeting to the tumor. Small peptides with high affinity for the metallated chelate (Ga- or Lu-AmMABD) are selected from a random phage display library. The peptide selection process is underway, however evaluation of the stability and biodistribution of radiolabeled 68Ga- and 177Lu-AmMABD in vivo has been determined and shows the potential utility of this method.

Stability and biodistribution of a radiolabeled “small peptide selector” complex

243rd National Meeting (2012)

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