PT - JOURNAL ARTICLE AU - Damian Wild AU - Melpomeni Fani AU - Richard Fischer AU - Luigi Del Pozzo AU - Felix Kaul AU - Simone Krebs AU - Richard Fischer AU - Jean E.F. Rivier AU - Jean Claude Reubi AU - Helmut R. Maecke AU - Wolfgang A. Weber TI - Comparison of Somatostatin Receptor Agonist and Antagonist for Peptide Receptor Radionuclide Therapy: A Pilot Study AID - 10.2967/jnumed.114.138834 DP - 2014 Aug 01 TA - Journal of Nuclear Medicine PG - 1248--1252 VI - 55 IP - 8 4099 - http://jnm.snmjournals.org/content/55/8/1248.short 4100 - http://jnm.snmjournals.org/content/55/8/1248.full SO - J Nucl Med2014 Aug 01; 55 AB - Preclinical and clinical studies have indicated that somatostatin receptor (sst)–expressing tumors demonstrate higher uptake of radiolabeled sst antagonists than of sst agonists. In 4 consecutive patients with advanced neuroendocrine tumors, we evaluated whether treatment with 177Lu-labeled sst antagonists is feasible. Methods: After injection of approximately 1 GBq of 177Lu-DOTA-[Cpa-c(DCys-Aph(Hor)-DAph(Cbm)-Lys-Thr-Cys)-DTyr-NH2] (177Lu-DOTA-JR11) and 177Lu-DOTATATE, 3-dimensional voxel dosimetry analysis based on SPECT/CT was performed. A higher tumor-to-organ dose ratio for 177Lu-DOTA-JR11 than for 177Lu-DOTATATE was the prerequisite for treatment with 177Lu-DOTA-JR11. Results: Reversible minor adverse effects of 177Lu-DOTA-JR11 were observed. 177Lu-DOTA-JR11 showed a 1.7–10.6 times higher tumor dose than 177Lu-DOTATATE. At the same time, the tumor-to-kidney and tumor–to–bone marrow dose ratio was 1.1–7.2 times higher. All 4 patients were treated with 177Lu-DOTA-JR11, resulting in partial remission in 2 patients, stable disease in 1 patient, and mixed response in the other patient. Conclusion: Treatment of neuroendocrine tumors with radiolabeled sst antagonists is clinically feasible and may have a significant impact on peptide receptor radionuclide therapy.