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  • Title: Monoclonal antibodies as reversible equilibrium carriers of radiopharmaceuticals.
    Author: Goodwin DA, Meares CF, David GF, McTigue M, McCall MJ, Frincke JM, Stone MR, Bartholomew RM, Leung JP.
    Journal: Int J Rad Appl Instrum B; 1986; 13(4):383-91. PubMed ID: 3098706.
    Abstract:
    We have prepared monoclonal antibodies (MoAbs) with the specific ability to bind metal chelates such as 111In benzyl EDTA. One, 10, 50 and 100 micrograms MoAb CHA255 Kb = 4 X 10E9 was complexed with 111In BLEDTA II, BLEDTA IV, and benzyl EDTA and injected i.v. in Balb/c mice with KHJJ tumor. The biological half-life by whole body counting was profoundly altered for all three compounds; from minutes to hours with 10 micrograms; to days with 100 micrograms. Tumor uptake increased 50 fold at 24 h with increasing MoAb but satisfactory tumor concentrations (3% per g) and tumor/blood ratios (1.8:1) were obtained with an amount equivalent to 7 mg for a human. Blood level and whole body activity were decreased 30-50% within 3 h or i.v. injection of a "flushing" dose of unlabeled indium benzyl EDTA, increasing tumor/blood ratios to 50:1.
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