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5-[¹²³I/¹²⁵I]Iodo-2'-Deoxyuridine in Metastatic Lung Cancer: Radiopharmaceutical Formulation Affects Targeting

Department of Radiology, Harvard Medical School, Boston, Massachusetts

View larger version (9K): [in a new window]   FIGURE 1. Pathways used for synthesis of 125I-IUdR and 123I-IUdR. TTPP = tetrakis(triphenylphosphine)palladium; PBS = phosphate-buffered saline.

View larger version (17K): [in a new window]   FIGURE 2. HPLC analysis of 125I-IUdR synthesized with varying amounts of SnUdR (127I-IUdR coinjected with 125I-IUdR). (A) SnUdR formulation: 1 µg. (B) SnUdR formulation: 100 µg. (Top) Radioactivity trace: 125I-IUdR tR = 7.5 min. (Bottom) 254-nm UV trace: 127I-IUdR tR = 7.1 min, SnUdR tR = 2.4 min.

View larger version (78K): [in a new window]   FIGURE 3. Lung from mouse bearing 14-d-old B16F10 lung tumor metastases. (A) Photograph of lung indicates melanin-filled, tumor-cell foci. (B) Section (5 µm) shows tumor growth.

View larger version (30K): [in a new window]   FIGURE 4. Biodistribution of radioactivity in B16F10 tumor-bearing mice (n = 8–14) 24 h after intravenous injection of 125I-IUdR preparations containing varying amounts of SnUdR (%ID/g, mean ± SEM).

View larger version (28K): [in a new window]   FIGURE 5. Biodistribution of radioactivity in control (nontumor-bearing) mice (n = 8–12) 24 h after intravenous injection of 125I-IUdR preparations containing varying amounts of SnUdR (%ID/g, mean ± SEM).

View larger version (19K): [in a new window]   FIGURE 6. Uptake (%ID/g) of 125I within lungs of B16F10- melanoma-bearing (2-wk-old tumors) and control mice after intravenous injection of 125I-IUdR synthesized with varying amounts of SnUdR.

View larger version (15K): [in a new window]   FIGURE 7. T/NT ratios (mean ± SEM) calculated from lung data in Figure 6.

View larger version (60K): [in a new window]   FIGURE 8. Images of control (A) and tumor-bearing (B) mice. (Top) Phosphor images (3-h exposure) of lung of control mouse (left) and tumor-bearing mouse (right) injected 24 h earlier with 185 kBq 125I-IUdR preparation containing 5 µg SnUdR. (Bottom) Scintigraphic images of control mouse (left) and tumor-bearing mouse (right) injected 3 h earlier with 7.4 MBq 123I-IUdR preparation containing 5 µg SnUdR. T = thyroid; L = lung (± tumor foci); S = stomach; B = bladder.