Article Figures & Data
Figures
- FIGURE 1.
Comparison of 177Lu-DOTATATE and 177Lu-DOTA-BASS receptor autoradiographic binding in successive sections of various types of human cancers (ileal carcinoid, pheochromocytoma, breast carcinoma, renal cell carcinoma, and non-Hodgkin lymphoma) expressing sst2. Columns from left to right represent hematoxylin and eosin staining, total and nonspecific binding of 177Lu-DOTATATE, and total and nonspecific binding of 177Lu-DOTA-BASS. Binding is markedly stronger with antagonist 177Lu-DOTA-BASS. HE = hematoxylin and eosin; NHL = non-Hodgkin lymphoma; NS = nonspecific; Pheo = pheochromocytoma; RCC = renal cell carcinoma.
- FIGURE 2.
Quantitation of in vitro receptor autoradiography experiments with various types of human cancers (ileal carcinoid, pheochromocytoma, breast carcinoma, renal cell carcinoma, and non-Hodgkin lymphoma) using 177Lu-DOTATATE and 177Lu-DOTA-BASS as radioligands. Shown are bar graphs of specific binding (counts/h) of radioligands to tumor sections after quantitation using InstantImager. For all tested human tumor types, antagonist 177Lu-DOTA-BASS exhibited markedly better binding behavior. NHL = non-Hodgkin lymphoma; Pheo = pheochromocytoma; RCC = renal cell carcinoma; Spec. = specific.
Tables
- TABLE 1
sst1–sst5 Affinity Profile of 2 Somatostatin Analogs, Compared with SRIF-28 as Reference
Compound sst1 sst2 sst3 sst4 sst5 SRIF-28, reference 3.2 ± 0.4 (7) 2.4 ± 0.2 (7) 4.0 ± 1.1 (7) 2.3 ± 0.5 (7) 2.3 ± 0.3 (7) DOTATATE, agonist >1,000 (3) 1.5 ± 0.4 (3) >1,000 (3) 453 ± 179 (3) 547 ± 160 (3) DOTA-BASS, antagonist >1,000 (4) 1.5 ± 0.4 (4) >1,000 (4) 287 ± 27 (4) >1,000 (4) Data are expressed as 50% inhibitory concentration in nM (mean ± SEM).
Number of experiments are in parentheses.
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