OtherBASIC SCIENCE INVESTIGATIONS

Small-Animal PET of Tumors with 64Cu-Labeled RGD-Bombesin Heterodimer

Zhaofei Liu, Zi-Bo Li, Qizhen Cao, Shuanglong Liu, Fan Wang and Xiaoyuan Chen
Journal of Nuclear Medicine July 2009, 50 (7) 1168-1177; DOI: https://doi.org/10.2967/jnumed.108.061739

Article Figures & Data

Figures

  • FIGURE 1. 
    FIGURE 1. 

    Chemical structures of DOTA-RGD-bombesin and NOTA-RGD-bombesin. RGD-bombesin is a heterodimer of cyclic RGD peptide c(RGDyK) and Aca-bombesin(7–14) through a glutamate linker, with RGD attached to α-carboxylate and bombesin attached to γ-carboxylate. BBN = bombesin.

  • FIGURE 2. 
    FIGURE 2. 

    (A) Cell uptake assay of 64Cu-NOTA-RGD, 64Cu-NOTA-bombesin, 64Cu-NOTA-RGD-bombesin, and 64Cu-DOTA-RGD-bombesin on PC-3 cells (n = 3, mean ± SD). (B) Cell efflux assay of 64Cu-NOTA-RGD, 64Cu-NOTA-bombesin, and 64Cu-NOTA-RGD-bombesin on PC-3 tumor cells (n = 3, mean ± SD). BBN = bombesin.

  • FIGURE 3. 
    FIGURE 3. 

    Decay-corrected whole-body coronal small-animal PET images of PC-3 tumor-bearing mice at 30 min, 1 h, 4 h, and 20 h after injection of approximately 5.5 MBq (150 μCi) of 64Cu-NOTA-RGD, 64Cu-NOTA-bombesin, 64Cu-NOTA-RGD-bombesin, 64Cu-NOTA-RGD plus 64Cu-NOTA-bombesin, or 64Cu-DOTA-RGD-bombesin. Images shown are static scans of a single mouse, which is representative of the 4 mice tested in each group. Arrows indicate presence of PC-3 tumors. BBN = bombesin.

  • FIGURE 4. 
    FIGURE 4. 

    (A) Decay-corrected whole-body coronal small-animal PET images of 4T1 murine breast cancer–bearing mice at 2 h after injection of 3.7 MBq (100 μCi) of 64Cu-NOTA-RGD, 64Cu-NOTA-bombesin, or 64Cu-NOTA-RGD-bombesin. Images shown are 5-min static scans of a single mouse, which is representative of the 3 mice tested in each group. Arrows indicate presence of 4T1 tumors. (B) Comparison of quantified tumor uptake of 64Cu-NOTA-RGD, 64Cu-NOTA-bombesin, and 64Cu-NOTA-RGD-bombesin in 4T1 tumor-bearing mice. Regions of interest are shown as %ID/g ± SD (n = 3/group). (C) Comparison between uptake of 64Cu-NOTA-RGD-bombesin in PC-3 tumor with or without preinjection of blocking doses of RGD, bombesin, or RGD plus bombesin. Regions of interest are shown as %ID/g ± SD (n = 3–4/group). (D) Decay-corrected whole-body coronal small-animal PET images of PC-3 tumor-bearing mice at 1 h after injection of approximately 5.5 MBq (150 μCi) of 64Cu-NOTA-RGD-bombesin and in the presence of blocking dose of RGD, bombesin, or RGD plus bombesin (n = 3/group). BBN = bombesin.

  • FIGURE 5. 
    FIGURE 5. 

    Biodistribution and blocking studies of 64Cu-NOTA-RGD-bombesin (370 kBq/mouse) in normal BALB/c mice at 1 h after injection of tracer with or without blocking dose of RGD, bombesin, or RGD plus bombesin. Data are expressed as %ID/g ± SD (n = 4/group). BBN = bombesin.

Tables

  • TABLE 1

    Small-Animal PET Data of 64Cu-Labeled Tracers in PC-3 Mice

    TracerTissue or organ30 min1 h4 h20 h
    64Cu-NOTA-RGDBlood0.44 ± 0.150.43 ± 0.320.30 ± 0.110.34 ± 0.18
    Liver2.86 ± 1.062.68 ± 1.152.15 ± 0.791.67 ± 0.69
    Kidney3.37 ± 0.892.13 ± 0.851.43 ± 0.680.98 ± 0.48
    Tumor1.01 ± 0.290.83 ± 0.240.66 ± 0.210.55 ± 0.32
    64Cu-NOTA-bombesinBlood0.74 ± 0.360.23 ± 0.110.19 ± 0.100.15 ± 0.05
    Liver10.45 ± 2.278.85 ± 1.616.35 ± 0.574.20 ± 0.53
    Kidney3.55 ± 1.171.50 ± 0.390.76 ± 0.450.50 ± 0.44
    Tumor2.28 ± 0.351.25 ± 1.030.56 ± 0.400.44 ± 0.39
    64Cu-NOTA-RGD plus 64Cu-NOTA-bombesinBlood0.79 ± 0.240.71 ± 0.230.31 ± 0.260.26 ± 0.18
    Liver9.64 ± 4.156.74 ± 2.865.48 ± 0.843.24 ± 0.78
    Kidney3.58 ± 0.981.83 ± 1.011.57 ± 0.870.84 ± 0.60
    Tumor2.22 ± 0.411.27 ± 0.500.87 ± 0.350.54 ± 0.39
    64Cu-NOTA-RGD-bombesinBlood0.68 ± 0.030.66 ± 0.150.49 ± 0.070.50 ± 0.15
    Liver3.46 ± 0.262.80 ± 1.151.83 ± 0.680.98 ± 0.40
    Kidney4.09 ± 0.813.06 ± 0.252.30 ± 0.411.87 ± 0.41
    Tumor3.06 ± 0.112.78 ± 0.562.21 ± 0.492.04 ± 0.35
    64Cu-DOTA-RGD-bombesinBlood1.15 ± 0.490.69 ± 0.240.45 ± 0.200.31 ± 0.13
    Liver3.40 ± 1.423.05 ± 1.072.33 ± 0.881.74 ± 0.90
    Kidney5.99 ± 1.613.40 ± 1.252.51 ± 0.471.64 ± 0.34
    Tumor3.05 ± 0.561.87 ± 0.411.05 ± 0.490.97 ± 0.24

    • Injection dose was ∼5.5 MBq (150 μCi) per mouse. Data are %ID/g ± SD (n = 4/group).

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