Journal
ADVANCED DRUG DELIVERY REVIEWS
Volume 60, Issue 12, Pages 1347-1370Publisher
ELSEVIER
DOI: 10.1016/j.addr.2008.04.006
Keywords
radiopharmaceuticals; radionuclides; target-specific delivery; diagnosis; radiotherapy
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Funding
- NCI NIH HHS [R01 CA115883-02, R01 CA115883, R01 CA115883-01A2] Funding Source: Medline
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Receptor-based radiopharmaceuticals are of great current interest in molecular imaging and radiotherapy of cancers, and provide a unique tool for target-specific delivery of radionuclides to the diseased tissues. In general, a target-specific radiopharmaceutical can be divided into four parts: targeting biomolecule (BM), pharmacokinetic modifying (PKM) linker, bifunctional coupling or chelating agent (BFC), and radionuclide. The targeting biomolecule serves as a carrier for specific delivery of the radionuclide. PKM linkers are used to modify radiotracer excretion kinetics. BFC is needed for radiolabeling of biomolecules with a metallic radionuclide. Different radiometals have significant difference in their coordination chemistry, and require BFCs with different donor atoms and chelator frameworks. Since the radiometal chelate can have a significant impact on physical and biological properties of the target-specific radiopharmaceutical, its excretion kinetics can be altered by modifying the coordination environment with various chelators orcoligand, if needed. This review will focus on the design of BFCs and their coordination chemistry with technetium, copper, gallium, indium, yttrium and lanthanide radiometals. (c) Published by Elsevier B.V.
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