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Quality Assurance of Radiolabeled Proteins, Peptides and Antisense Oligonucleotides

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Chemists’ Views of Imaging Centers

Summary

Radiopharmaceuticals (RP) labeled with nonmetallic (I–123, C-11, F-18) and metallic radionuclides (Tc-99m, Ga-67, In-111) are used for diagnosis and therapy; they could be classified as blood flow markers, metabolic substrates, receptor ligands, peptide/proteins and antisense oligonucleotide analogs (F-18, 1–123, In-111, Tc-99m). The oligopeptide/nucleotide based tracers, are designed to adhere as “molecular velcro” to target molecules in diseased cells for early, high-contrast imaging. For safety, efficacy and further improvement of the tests using these tracers, quality assurance (QA) of tracers (chemical, radionuclidiC., radiochemical impurities, enantiomers, immunoreactivity, sterility, apyrogenicity, cell-viability) is required. These tests are more critical for the RP under clinical investigations. FDA allows a maximum permissible limit of 10% of the injected radionuclide as impurity. Quality assurance of RP is carried out by thin-layer, size-exclusion/ion-exchange (high pressure liquid transport) chromatography and gel electrophoresis. For therapeutic RP labeled with 1–131 (β, γ), Re-186 (β, γ), Re-188 (β), Y-90 (β), At-211(α) and Bi-212 (α), etc., the level of chemical alterations/degradations, directly by energetic particles or indirectly by free-radicals, is higher for the α-, β- than γ-emitting RP and chemical alterations are time-dependent processes. Considering the adverse reactions (marrow-suppression), unnecessary radiation due to unbound tracers and impurities, QA of RP should be performed and impurities eliminated before RP administration.

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Dewanjee, M.K. (1995). Quality Assurance of Radiolabeled Proteins, Peptides and Antisense Oligonucleotides. In: Emran, A.M. (eds) Chemists’ Views of Imaging Centers. Springer, Boston, MA. https://doi.org/10.1007/978-1-4757-9670-4_22

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  • DOI: https://doi.org/10.1007/978-1-4757-9670-4_22

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-1-4757-9672-8

  • Online ISBN: 978-1-4757-9670-4

  • eBook Packages: Springer Book Archive

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