尿排泄性の高いIn標識馬尿酸誘導体の合成と評価

鈴木 博元; 金井 彩香*; 上原 知也*; 花岡 宏史*; 荒野 泰*

no journal, , 

Radiolabeled antibody fragments show rapid elimination rate from blood, which can improve bone marrow toxicities of radiolabeled intact IgG. However, high and persistent localization in kidney is observed, which impairs diagnostic accuracy and therapeutic effectiveness. Brush border strategy succeeded to reduce renal radioactivity by using the radioiodine labeled antibody fragment in which a cleavable peptide linker is introduced. In the strategy, the radiometabolite is liberated by the action of renal brush border enzymes before incorporating into renal cells, and excreted into urine. In order to apply this molecular design to radiometals such as In and Y, the radiometabolite with high urinary excretion, which includes a radiometal-chelating moiety is required. In this study, we synthesized and evaluated a hippuric acid derivative, Bn-CHX-A"-DTPA-Gly labeled with In as a radiometabolite.