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Current Pharmaceutical Design

Editor-in-Chief

ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

Biological Carrier Molecules of Radiopharmaceuticals for Molecular Cancer Imaging and Targeted Cancer Therapy

Author(s): A. Aerts, N.R.E.N. Impens, M. Gijs, M. D'Huyvetter, H. Vanmarcke, B. Ponsard, T. Lahoutte, A. Luxen and S. Baatout

Volume 20, Issue 32, 2014

Page: [5218 - 5244] Pages: 27

DOI: 10.2174/1381612819666140110114902

Price: $65

Abstract

Many tumors express one or more proteins that are either absent or hardly present in normal tissues, and which can be targeted by radiopharmaceuticals for either visualization of tumor cells or for targeted therapy. Radiopharmaceuticals can consist of a radionuclide and a carrier molecule that interacts with the tumor target and as such guides the attached radionuclide to the right spot. Radiopharmaceuticals hold great promise for the future of oncology by providing early, precise diagnosis and better, personalized treatment. Most advanced developments with marketed products are based on whole antibodies or antibody fragments as carrier molecules. However, a substantial number of (pre)clinical studies indicate that radiopharmaceuticals based on other carrier molecules, such as peptides, nonimmunoglobulin scaffolds, or nucleic acids may be valuable alternatives. In this review, we discuss the biological molecules that can deliver radionuclide payloads to tumor cells in terms of their structure, the selection procedure, their (pre)clinical status, and advantages or obstacles to their use in a radiopharmaceutical design. We also consider the plethora of molecular targets existing on cancer cells that can be targeted by radiopharmaceuticals, as well as how to select a radionuclide for a given diagnostic or therapeutic product.

Keywords: Radiopharmaceuticals, molecular imaging, targeted therapy, antibody, peptides, non-immunoglobulin scaffolds, nucleic acids.

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