申请人:Centocor
公开号:US05144043A1
公开(公告)日:1992-09-01
A bifunctional coupling agent for joining a sulfhydryl containing protein or peptide and a metallic radionuclide comprising a sulfhydryl selective electrophile, a chelator containing at least one protected thiol and a organic linking radical containing at least one cleavable site which serves to join said electrophile and said chelator is disclosed. A radiodiagnostic or radiotherapeutic precursor comprising an antibody or antibody fragment and the specified bifunctional coupling agent bound to a sulfhydryl group on the antibody or antibody fragment and a radiodiagnostic or radiotherapeutic agent comprising such precursor having a metallic radionuclide bound thereto are also disclosed.
一种用于连接含有巯基的蛋白质或肽和金属放射性核素的双功能偶联剂,包括一种巯基选择性亲电试剂,至少含有一个受保护巯基的螯合剂和至少含有一个可切割位点的有机连接基团,用于连接所述亲电试剂和所述螯合剂的。还公开了一种放射诊断或放射治疗前体,包括抗体或抗体片段以及与抗体或抗体片段上的巯基结合的指定双功能偶联剂,以及包含所述前体的放射诊断或放射治疗剂,其中该前体具有与金属放射性核素结合的。