Comparison of somatostatin receptor agonist and antagonist for peptide receptor radionuclide therapy: A pilot study Journal Article


Authors: Wild, D.; Fani, M.; Fischer, R.; Pozzo, L. D.; Kaul, F.; Krebs, S.; Rivier, J. E. F.; Reubi, J. C.; Maecke, H. R.; Weber, W. A.
Article Title: Comparison of somatostatin receptor agonist and antagonist for peptide receptor radionuclide therapy: A pilot study
Abstract: 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-DOTAJR11 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. COPYRIGHT © 2014 by the Society of Nuclear Medicine and Molecular Imaging, Inc.
Keywords: cancer chemotherapy; aged; unclassified drug; clinical trial; case report; drug efficacy; drug safety; multiple cycle treatment; thrombocytopenia; neuroendocrine tumor; lung tumor; cancer regression; feasibility study; diagnostic agent; drug uptake; isotope labeling; pilot study; dosimetry; radiopharmaceutical agent; drug half life; bladder carcinoma; single photon emission computer tomography; drug excretion; neuroendocrine tumors; antagonists; comparative effectiveness; ileum tumor; human; male; female; priority journal; article; somatostatin receptor targeting; lutetium tetraxetan jr11 lu 177; lutetium tetraxetan octreotide[3 tyrosine] lu 177
Journal Title: Journal of Nuclear Medicine
Volume: 55
Issue: 8
ISSN: 0161-5505
Publisher: Society of Nuclear Medicine  
Date Published: 2014-06-24
Start Page: 1248
End Page: 1252
Language: English
DOI: 10.2967/jnumed.114.138834
PROVIDER: scopus
PUBMED: 24963127
DOI/URL:
Notes: Export Date: 2 September 2014 -- CODEN: JNMEA -- Source: Scopus
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  1. Wolfgang Andreas Weber
    173 Weber