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Preclinical Comparison of ¹¹¹In-Labeled DTPA- or DOTA-Bombesin Analogs for Receptor-Targeted Scintigraphy and Radionuclide Therapy

¹ Department of Nuclear Medicine, Erasmus University Medical Center Rotterdam, Rotterdam, The Netherlands
² Mallinckrodt Medical, St. Louis, Missouri
³ Department of Internal Medicine, Erasmus University Medical Center Rotterdam, Rotterdam, The Netherlands

View larger version (27K): [in a new window]   FIGURE 1. Amino acid sequence of GRP and BN analogs. Common C-terminal 7 amino acids in GRP and BN analogs are indicated in boldface type.

View larger version (31K): [in a new window]   FIGURE 2. Specific binding and internalization (dotted) of 111In-labeled BN analogs by GRP receptor-positive CA20948 (A) and AR42J (B) rat pancreatic tumor cells. 5° and 37° = 5°C and 37°C, respectively. Data are expressed as % dose per mg of protein.

View larger version (40K): [in a new window]   FIGURE 3. Tissue distribution of 111In-labeled [DTPA-Pro1,Tyr4]BN, [DOTA-Pro1,Tyr4]BN, [DTPA--Lys3,Tyr4]BN, and [DOTA--Lys3,Tyr4]BN in rats 24 h after administration of radioligand. Nonspecific uptake of radioactivity (striped) was determined by coinjection of GRP receptor-blocking dose of 0.1 mg [Tyr4]BN. Difference between total uptake and nonspecific uptake represents specific binding of radioligand to GRP receptor. Data are expressed as %ID per gram of tissue and presented as means ± SD (n = 3).

View larger version (26K): [in a new window]   FIGURE 4. Tissue-to-blood ratio of 111In-labeled [DTPA-Pro1,Tyr4]BN, [DOTA-Pro1,Tyr4]BN, [DTPA--Lys3,Tyr4]BN, and [DOTA--Lys3,Tyr4]BN in rats 24 h after administration of radioligand. Nonspecific uptake of radioactivity (striped) was determined by coinjection of GRP receptor-blocking dose of 0.1 mg [Tyr4]BN. Data are expressed as ratio of %ID per gram of tissue versus that in blood and presented as means ± SD (n = 3).

View larger version (121K): [in a new window]   FIGURE 5. Distribution of radioactivity in AR42J tumor-bearing rat 24 h after administration of 15 MBq (0.1 µg) [111In-DOTA-Pro1,Tyr4]BN. Note uptake in tumor and physiologic uptake in kidneys.