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Peptide Receptor Radionuclide Therapy In Vitro Using [¹¹¹In-DTPA⁰]Octreotide

Department of Nuclear Medicine, Erasmus Medical Center, Rotterdam, The Netherlands

View larger version (17K): [in a new window]   FIGURE 1. Internalization in CA20948 cells after 1-h incubation at 37°C with [111In-DTPA0]octreotide and 111In-DTPA. Bars represent mean ± SEM.

View larger version (38K): [in a new window]   FIGURE 2. Amount of internalized [111In-DTPA0]octreotide after 72 h in growth medium with 200–10,000 cells per well. Cells were incubated for 1 h at 37°C with increasing concentrations of [111In-DTPA0]octreotide. Amount of internalized [111In-DTPA0]octreotide was determined after 72 h. (A) Amount of internalized counts per minute. (B) Internalized amount presented as percentage of given dose. Bars represent mean ± SEM.

View larger version (26K): [in a new window]   FIGURE 3. Effects of incubation time, concentration, and specific activity of [111In-DTPA0]octreotide on cell survival of CA20948 cells after PRRT. Cells were incubated for 1, 3, and 5 h with 0.37 or 3.7 MBq [111In-DTPA0]octreotide at 37°C using 2 different specific activities (specific activity of B is different from that of A and C). Bars represent mean ± SEM.

View larger version (18K): [in a new window]   FIGURE 4. Inhibitory effect of [111In-DTPA0]octreotide on clonogenic cell survival of rat pancreatic tumor cell line CA20948. Cells were incubated for 1 h at 37°C with increasing amount of [111In-DTPA0]octreotide. Bars represent mean ± SEM.

View larger version (22K): [in a new window]   FIGURE 5. Effect of 111In-DTPA (A) and octreotide (B) on clonogenic cell survival of CA20948 cells. Cells were incubated for 1 h in increasing amount of 111In-DTPA (same amount was given as was used with [111In-DTPA]octreotide [Fig. 4]). Amount of radioactivity that is normally attached to cells was added to medium after 1-h incubation. 111In-DTPA was also added when medium was refreshed after 3 d. Bars represent mean ± SEM.

View larger version (23K): [in a new window]   FIGURE 6. Inhibitory effect of octreotide on tumor cell survival of CA20948 cell line. Cells were incubated for 1 h at 37°C with 10-6 mol/L octreotide (second bar from left) and cells were incubated with 10-6 mol/L octreotide plus increasing amount of [111In-DTPA]octreotide (third to fifth bars from left). Bars represent mean ± SEM.