Research ArticleBasic Science Investigations

“To Serve and Protect”: Enzyme Inhibitors as Radiopeptide Escorts Promote Tumor Targeting

Berthold A. Nock, Theodosia Maina, Eric P. Krenning and Marion de Jong
Journal of Nuclear Medicine January 2014, 55 (1) 121-127; DOI: https://doi.org/10.2967/jnumed.113.129411

Article Figures & Data

Figures

  • FIGURE 1.
    FIGURE 1.

    (A and B) HPLC analysis of blood collected 5 min after injection of [111In-DOTA-Ala1]SS14 into healthy mice without (A) or with (B) coinjection of PA. (C) Tissue distribution data at 4 h after injection of [111In-DOTA-Ala1]SS14 without PA, with PA, or with PA plus excess sst2 blocker coinjection into male SCID mice bearing AR4-2J xenografts; values for tumors are shown in inset. Ad = adrenal glands; Bl = blood; Fe = femur; He = heart; In = intestines; Ki = kidneys; Li = liver; Lu = lungs; Mu = muscle; Pa = pancreas; Sp = spleen; St = stomach; Tu = AR4-2J tumors.

  • FIGURE 2.
    FIGURE 2.

    (A and B) HPLC analysis of blood collected 5 min after injection of 111In-PanSB1 into healthy mice without (A) or with (B) coinjection of PA. (C) Tissue distribution data at 4 h after injection of 111In-PanSB1 without PA, with PA, or with PA plus excess GRPR blocker coinjection into female SCID mice bearing human PC-3 xenografts; values for tumors are shown in inset. Bl = blood; Fe = femur; He = heart; In = intestines; Ki = kidneys; Li = liver; Lu = lungs; Mu = muscle; Pa = pancreas; Sp = spleen; St = stomach; Tu = PC-3 tumors.

  • FIGURE 3.
    FIGURE 3.

    (A and B) HPLC analysis of blood collected 5 min after injection of [111In-DOTA]MG11 into healthy mice without (A) or with (B) coinjection of PA. (C) Tissue distribution data at 4 h after injection of [111In-DOTA]MG11 without PA or with PA coinjection into male SCID mice bearing A431-CCK2R(+) and A431-CCK2R(−) xenografts; values for tumors are shown in inset. Bl = blood; Fe = femur; He = heart; In = intestines; Ki = kidneys; Li = liver; Lu = lungs; Mu = muscle; Pa = pancreas; Sp = spleen; St = stomach; Tu − = A431-CCK2R(−) tumors; Tu + = A431-CCK2R(+) tumors.

  • FIGURE 4.
    FIGURE 4.

    (A) Biodistribution of [111In-DOTA]MG11 at 4 h after injection without PA, with PA, or with PA plus excess CCK2R blocker coinjection into AR4-2J tumor–bearing mice; values for tumors are shown in inset. Bl = blood; Fe = femur; He = heart; In = intestines; Ki = kidneys; Li = liver; Lu = lungs; Mu = muscle; Pa = pancreas; Sp = spleen; St = stomach; Tu = AR4-2J tumors. (B and C) SPECT/CT at 4 h after injection of [111In-DOTA]MG11 without (B) or with (C) coinjection of PA (n = 3 per group). Note the highly improved tumor visualization in C.

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