lysylglycine and cyclen

Improvement of the accuracy of dosimetry in radionuclide therapy has the potential to increase patient safety and therapeutic outcomes. Although positron emission tomography (PET) is ideally suited for acquisition of dosimetric data because PET is inherently quantitative and offers high sensitivity and spatial resolution, it is not directly applicable for this purpose because common therapeutic radionuclides lack the necessary positron emission. This work reports on the synthesis of dual-nuclide labeled radiopharmaceuticals with therapeutic and PET functionality, which are based on common and widely available metal radionuclides. Dual-chelator conjugates, featuring interlinked cyclen- and triazacyclononane-based polyphosphinates DOTPI and TRAP, allow for strictly regioselective complexation of therapeutic (e.g.,

Topics: Animals; Aza Compounds; Chelating Agents; Cyclams; Dipeptides; Heterocyclic Compounds; Heterografts; Humans; Male; Mice, SCID; Neoplasm Transplantation; Phosphatidylinositol Phosphates; Phosphinic Acids; Piperidines; Positron-Emission Tomography; Prostatic Neoplasms; Radioisotopes; Radiopharmaceuticals; Structure-Activity Relationship