Research ArticleBasic Science Investigation
Open Access

Receptor-Targeted Peptide Conjugates Based on Diphosphines Enable Preparation of 99mTc and 188Re Theranostic Agents for Prostate Cancer

Truc T. Pham, Ingebjørg N. Hungnes, Charlotte Rivas, Julie Cleaver, George Firth, Philip J. Blower, Jane Sosabowski, Gary J.R. Cook, Lefteris Livieratos, Jennifer D. Young, Paul G. Pringle and Michelle T. Ma
Journal of Nuclear Medicine July 2024, 65 (7) 1087-1094; DOI: https://doi.org/10.2967/jnumed.124.267450

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  • Figure
  • FIGURE 1.
    FIGURE 1.

    (A) Chemical structures of M-DP1-PSMAt and M-DP2-PSMAt, M = Tc (99mTc or 99gTc) and Re (natRe or 188Re). (B) Reverse-phase C18-HPLC radiochromatograms showing coelution of [188Re]Re-DP1-PSMAt, [99mTc]Tc-DP1-PSMAt, and [natRe]Re-DP1-PSMAt and coelution of [188Re]Re-DP2-PSMAt, [99mTc]Tc-DP2-PSMAt, and [natRe]Re-DP2-PSMAt. UV = ultraviolet.

  • FIGURE 2.
    FIGURE 2.

    (A) Uptake of radiotracers in PSMA-positive and PSMA-negative prostate cancer cells. (B) Time course uptake and localization of 99mTc radiotracers in DU145-PSMA cells and LNCaP cells. Data are presented as mean ± SD; n = 3–4 biologic repeats performed in triplicate.

  • FIGURE 3.
    FIGURE 3.

    (A) Biodistribution (2 h after injection) of SCID/beige mice bearing DU145-PSMA+ prostate cancer tumors, administered either 99mTc or 188Re radiotracers intravenously. To assess specificity of radiotracer uptake, additional groups of mice were also coadministered radiotracer and PMPA (Supplemental Tables 3 and 4). (B) Whole-body SPECT/CT maximum-intensity projections of SCID/beige mice bearing either DU145-PSMA+ tumors or DU145 tumors, administered either [99mTc]Tc-DP1-PSMAt or [99mTc]Tc-DP2-PSMAt, 2 h after injection. To inhibit uptake in DU145-PSMA+ tumors, animals were also coadministered PMPA.

  • FIGURE 4.
    FIGURE 4.

    (A–C) Biodistribution of 188Re in athymic nude mice bearing LNCaP prostate cancer tumors, administered either [188Re]Re-DP1-PSMAt or [188Re]Re-DP2-PSMAt at 2 h after injection (A), at 24 h after injection (B), and at 2 h after injection (C) with coadministration of Gelofusine. (D) Additionally, biodistributions of [99mTc]Tc-DP1-PSMAt and [99mTc]Tc-DP2-PSMAt at 2 h after injection were measured (Supplemental Tables 5–8). GI = gastrointestinal tract.

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