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Pharmacokinetic Properties of Peptidic Radiopharmaceuticals: Reduced Uptake of (EH)3-Conjugates in Important Organs

Matthias Eder, Thomas Löhr, Ulrike Bauder-Wüst, Markus Reber, Walter Mier, Martin Schäfer, Uwe Haberkorn and Michael Eisenhut
Journal of Nuclear Medicine August 2013, 54 (8) 1327-1330; DOI: https://doi.org/10.2967/jnumed.112.114512

Article Figures & Data

Figures

  • FIGURE 1.
    FIGURE 1.

    Chemical structures of (EH)3-conjugates investigated: Glu-urea-Lys(Ahx)-HBED-CC-(EH)3 (A) and TATE-PEG2-HBED-CC-(EH)3 (B).

  • FIGURE 2.
    FIGURE 2.

    Organ distribution at 1 h after injection of 0.1–0.2 nmol of PSMA inhibitor Glu-urea-Lys(Ahx) labeled with either 68Ga-HBED-CC or 68Ga-HBED-CC-(EH)3 (A) and octreotate-PEG2 (TATE-PEG2) labeled with either 68Ga-HBED-CC or 68Ga-HBED-CC-(EH)3 (B). Data are expressed as mean %ID/g tissue ± SD (n = 3). Graphs in C and D show respective tumor-to-organ (T/O) ratios at 1 h after injection.

Tables

  • TABLE 1

    Analytic and Binding Data of Investigated Conjugates

    Compoundm/z*m/z calculated as [M+H]+Cell surface bound (%ID/106 cells)Internalized (%ID/106 cells)Affinity-related IC50 (nM) determined in cell-based assay
    Glu-urea-Lys(Ahx)-HBED-CC947.7947.418.4 ± 1.84.8 ± 0.310.3 ± 1.2
    Glu-urea-Lys(Ahx)-HBED-CC-(EH)31,746.31,745.724.6 ± 2.76.7 ± 2.031.8 ± 1.2
    TATE-PEG2-HBED-CC1,709.01,708.76.9 ± 0.54.8 ± 0.345.1 ± 1.3
    TATE-PEG2-HBED-CC-(EH)32,507.22,507.04.8 ± 1.54.0 ± 1.348.9 ± 1.1

    • ↵* Mass spectrometry data of free ligands ([M+H]+).

    • IC50 = 50% inhibitory concentration.

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