Patent Number: 8,575,100

Title: Tc and Re labeled radioactive glycosylated octreotide derivatives

Abstract: Improved sst-receptor binding peptidic ligands for diagnostic and therapeutic applications in nuclear medicine are provided. The improved ligands contain either natural or unnatural amino acids or peptidomimetic structures that are modified at either the N-terminal or the C-terminal end or at both termini, a carbohydrate unit and a chelator or prosthetic group to provide a complexation of a radioisotope binding or holding the radioisotope. The sst- or SSTR-receptor binding peptidic ligands may also contain one or more multifunctional linker units optionally coupling the peptide, and/or the sugar moiety and/or the chelator and/or the prosthetic group. Upon administering the ligand to a mammal through the blood system the ligand provides improved availability, clearance kinetics, sst-receptor targeting and internalization over the non-carbohydrated ligands.

Inventors: Wester; Hans-Jurgen (Illmmuenster, DE), Schottelius; Margret (Munich, DE), Schwaiger; Markus (Munich, DE)

Assignee: Mallinckrodt LLC

International Classification: A61K 38/31 (20060101); A61P 5/06 (20060101)

Expiration Date: 1/05/12017