PRECLINICAL DEVELOPMENT OF THERAPEUTIC RADIOPHARMACEUTICALS

The development of new and improved approaches for targeted radionuclide therapy is currently one of the most intensively pursued areas of radiopharmaceutical research. This field has, in particular, been stimulated by recent successes such as those achieved with radiolabelled anti-CD20 antibodies and radiolabelled somatostatin analogues. The main goal of this coordinated research project was to identify and validate procedures that could be used for the preclinical assessment of therapeutic radiopharmaceuticals in order to refine their performance. Additionally, the aim of the work was to compare potential lead candidates prior to undertaking clinical trials. 

This work describes in some detail those parameters that were identified, at the start of the coordinated research project, as being important in this assessment process. Since a decision was taken at the start of the project to concentrate research on the model peptide DOTA-Tyr -octreotate (DOTATATE), examples from the field of radiolabelled neuropeptide research are included. Details concerning the following topics are discussed in this paper  

Cellular processing and metabolism In vivo biodistribution and targeting In vitro efficacy  

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