公开(公告)号：US06608174B1

公开(公告)日：2003-08-19

申请号：US09629632

申请日：2000-07-31

申请人： Anand C. Burman ,  Sudhanand Prasad ,  Rama Mukherjee ,  Sarjana Dutt ,  Rajan T. Sharma ,  Rinku Ahuja ,  Anil K. Mishra ,  Lazar T. Mathew

发明人： Anand C. Burman ,  Sudhanand Prasad ,  Rama Mukherjee ,  Sarjana Dutt ,  Rajan T. Sharma ,  Rinku Ahuja ,  Anil K. Mishra ,  Lazar T. Mathew

IPC分类号： A61K3816

CPC分类号： C07K14/57563 ,  A61K38/00 ,  A61K51/08

摘要： The present invention encompasses radiolabeled peptide analogs of vasoactive intestinal peptide (VIP) labeled with a radionuclide useful for imaging target sites within mammalian living systems. The invention particularly provides radiolabeled VIP derivatives that bind selectively to the VIP receptor on target cells. Specifically, the invention relates to the radiolabeling of VIP-receptor specific agents and their subsequent use for radiodiagnostic and radiotherapeutic purposes. The invention encompasses methods for radiolabeling these peptides with radio-nuclides and the use of these peptides as scintigraphic imaging agents. The radiolabeled VIP derivatives of the present invention exhibit pharmacological activity and therefore are useful as either imaging agent for visualization of VIP-receptor positive tumors and metastases, as a radiodiagnostic agent or as a radio-therapeutic agent for the treatment of such tumors in vivo by specifically targeting the cytotoxic radionuclide selectively to the tumor site in mammalian living systems.

摘要翻译： 本发明包括用放射性核素标记的血管活性肠肽（VIP）的放射性标记肽类似物，其用于成像哺乳动物生物系统内的靶位点。 本发明特别提供了放射性标记的VIP衍生物，其选择性地结合靶细胞上的VIP受体。 具体地，本发明涉及VIP-受体特异性试剂的放射性标记及其随后用于放射诊断和放射治疗目的。 本发明包括用放射性核素放射性标记这些肽的方法以及这些肽作为闪烁照相成像剂的用途。 本发明的放射性标记的VIP衍生物显示药理活性，因此可用作VIP-受体阳性肿瘤和转移的可视化显像剂，作为放射诊断剂或作为放射治疗剂，用于通过 特别是将细胞毒性放射性核素选择性地靶向哺乳动物生命系统中的肿瘤部位。