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Journal of Nuclear Medicine

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Research ArticleThe State of the Art

The Use of Microdosing in the Development of Small Organic and Protein Therapeutics

Mats Bergstrom
Journal of Nuclear Medicine August 2017, 58 (8) 1188-1195; DOI: https://doi.org/10.2967/jnumed.116.188037
Mats Bergstrom
Department of Pharmacology and PET Centre, Uppsala University, Uppsala, Sweden [retired]
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    FIGURE 1.

    Schematic illustration of cell components that may be relevant to heterogeneous cellular distribution.

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    FIGURE 2.

    Typical plasma pharmacokinetics of an antibody.

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    FIGURE 3.

    Typical plasma radiopharmacokinetics at fixed amount of radioactivity and different mass doses.

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    FIGURE 4.

    Different possible cellular fates of radiolabeled antibodies. (A) Binding to and dissociation from extracellular receptor. (B) Binding to extracellular receptor followed by internalization. (C and D) Transfer among lysosomal compartments. (E) Release of receptor and ligand from cell. (F) Lysosomal degradation of receptor or ligand. (G) Release of radionuclide from cell.

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Journal of Nuclear Medicine: 58 (8)
Journal of Nuclear Medicine
Vol. 58, Issue 8
August 1, 2017
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The Use of Microdosing in the Development of Small Organic and Protein Therapeutics
Mats Bergstrom
Journal of Nuclear Medicine Aug 2017, 58 (8) 1188-1195; DOI: 10.2967/jnumed.116.188037

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The Use of Microdosing in the Development of Small Organic and Protein Therapeutics
Mats Bergstrom
Journal of Nuclear Medicine Aug 2017, 58 (8) 1188-1195; DOI: 10.2967/jnumed.116.188037
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    • Abstract
    • PHARMACOLOGIC CONSIDERATIONS IN DEVELOPING A THERAPEUTIC DRUG
    • CONSIDERATIONS IN INTERPRETATING IMAGING STUDIES
    • MODELING OF UPTAKE BY TISSUE
    • INDICATIONS FOR MICRODOSING STUDIES IN DRUG DEVELOPMENT
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Keywords

  • molecular imaging
  • microdosing
  • drug development
  • PET
  • pharmacokinetics
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