PT - JOURNAL ARTICLE AU - Wild, Damian AU - Fani, Melpomeni AU - Behe, Martin AU - Brink, Ingo AU - Rivier, Jean E.F. AU - Reubi, Jean Claude AU - Maecke, Helmut R. AU - Weber, Wolfgang A. TI - First Clinical Evidence That Imaging with Somatostatin Receptor Antagonists Is Feasible AID - 10.2967/jnumed.111.088922 DP - 2011 Sep 01 TA - Journal of Nuclear Medicine PG - 1412--1417 VI - 52 IP - 9 4099 - http://jnm.snmjournals.org/content/52/9/1412.short 4100 - http://jnm.snmjournals.org/content/52/9/1412.full SO - J Nucl Med2011 Sep 01; 52 AB - Preclinical studies have indicated that somatostatin receptor (sst)–expressing tumors demonstrate higher uptake of radiolabeled sst antagonists than of sst agonists. In this study, we evaluated whether imaging with sst antagonists was feasible in patients. Methods: Biodistribution and tumor uptake of the sst antagonist 111In-DOTA-pNO2-Phe-c(DCys-Tyr-DTrp-Lys-Thr-Cys)DTyrNH2 (111In-DOTA-BASS) were studied in 5 patients with metastatic thyroid carcinoma or neuroendocrine tumors. Findings were compared with 111In-pentetreotid (111In-DTPA-octreotide) scan. Results: No adverse effects of 111In-DOTA-BASS (20 μg) were observed. 111In-DOTA-BASS detected 25 of 28 lesions, whereas 111In-DTPA-octreotide detected only 17 of 28 lesions. In the same patient, 111In-DOTA-BASS showed higher tumor and lower renal uptake than 111In-DTPA-octreotide (3.5 ± 2.8 percentage injected activity [%IA] vs. 1.0 ± 0.99%IA and 1.5 ± 0.3 %IA vs. 2.3 ± 0.7 %IA) at 4 h after injection. Conclusion: Imaging of neuroendocrine tumors with sst antagonists is clinically feasible. The favorable human biodistribution data suggest that sst antagonists could significantly affect peptide receptor–mediated imaging and therapy.