title: Effect of different linkages between chelates and monoclonal antibodies on levels of radioactivity in the liver.
abstract: After injection of radiometal labeled antibodies, the radionuclide accumulates in the liver. This might be altered by a metabolizable linkage between metal chelate and antibody. Four benzyl-EDTA chelating agents were synthesized and conjugated to mouse monoclonal antibody Lym-1. Liver uptake of 111In in nontumored mice 72 h after injection was 2.2, 13.4, 7.6 and 20% for disulfide, thioether, thiourea or peptide linkages, respectively. 111In excreted in the urine was still in the benzyl-EDTA chelate form, as shown by binding to a specific anti-chelate antibody.
authors.affiliation: Department of Internal Medicine, University of California, Davis, Medical Center, Sacramento 95817.
authors.forename: S V
authors.initials: SV
authors.lastname: Deshpande
authors.forename: S J
authors.initials: SJ
authors.lastname: Denardo
authors.forename: C F
authors.initials: CF
authors.lastname: Meares
authors.forename: M J
authors.initials: MJ
authors.lastname: McCall
authors.forename: G P
authors.initials: GP
authors.lastname: Adams
authors.forename: G L
authors.initials: GL
authors.lastname: Denardo
mesh_terms: D000818:Animals; D000911:Antibodies, Monoclonal / Q000627:therapeutic use; D002614:Chelating Agents / Q000138:chemical synthesis; D007205:Indium Radioisotopes / Q000493:pharmacokinetics*; D008099:Liver / Q000378:metabolism*; D051379:Mice; D008807:Mice, Inbred BALB C
chemical_list: D000911:Antibodies, Monoclonal; D002614:Chelating Agents; D007205:Indium Radioisotopes