213Bi-[DOTA0, Tyr3]octreotide peptide receptor radionuclide therapy of pancreatic tumors in a preclinical animal model

Clinical Cancer Research : an Official Journal of the American Association for Cancer Research
Jeffrey P NorenbergLarry K Kvols

Abstract

The somatostatin analogue [DOTA0, Tyr3]octreotide (DOTATOC) has previously been labeled with low linear energy transfer (LET) beta-emitters, such as 177Lu or 90Y, for tumor therapy. In this study, DOTATOC labeled with the high-LET alpha-emitter, 213Bi, was evaluated. The radiolabeling, stability, biodistribution, toxicity, safety, and therapeutic efficacy of 213Bi-DOTATOC (specific activity 7.4 MBq/microg) were investigated. Biodistribution studies to determine somatostatin receptor specificity were done in Lewis rats at 1 and 3 hours postinjection. Histopathology of various organs was used to evaluated toxicity and safety. Therapeutic efficacy of 4 to 22 MBq 213Bi-DOTATOC was determined in a rat pancreatic carcinoma model. Radiolabeling of the 213Bi-DOTATOC was achieved with radiochemical purity >95% and an incorporation yield > or = 99.9%. Biodistribution data showed specific binding to somatostatin receptor-expressing tissues. Administration of free 213Bi, compared with 213Bi-DOTATOC, resulted in higher radioactivity accumulation at 3 hours postinjection in the kidneys [34.47 +/- 1.40% injected dose/g (ID/g) tissue versus 11.15 +/- 0.46%, P < 0.0001] and bone marrow (0.31 +/- 0.01% ID/g versus 0.06 +/- 0.02%, P < 0.0324). A ...Continue Reading

References

Jun 1, 1992·Journal of Neurochemistry·S Rens-Domiano, T Reisine
Sep 1, 1992·Metabolism: Clinical and Experimental·J C ReubiLarry K Kvols
Mar 1, 1990·Baillière's Clinical Endocrinology and Metabolism·S W LambertsJ C Reubi
Feb 1, 1993·Nuclear Medicine Communications·M W GeerlingsR van der Hout
Jan 1, 1996·Acta Oncologica·Michael R Zalutsky, D D Bigner
Sep 2, 1998·European Journal of Nuclear Medicine·Michael R McDevittDavid A Scheinberg
Aug 6, 1999·Frontiers in Neuroendocrinology·Y C Patel
Aug 2, 2001·Endocrine Pathology·A Quintanar-StephanoK Kovacs
Sep 28, 2001·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·D MaDavid A Scheinberg
Dec 18, 2001·International Journal of Cancer. Journal International Du Cancer·J S LewisC J Anderson
Jan 5, 2002·Annals of Oncology : Official Journal of the European Society for Medical Oncology·K Oberg
May 11, 2002·European Journal of Nuclear Medicine and Molecular Imaging·Tilmann SchumacherHelmut R Maecke
May 29, 2002·Cell Death and Differentiation·Michael R McDevitt, David A Scheinberg
Jan 29, 2003·European Journal of Nuclear Medicine and Molecular Imaging·Lisa BodeiGiovanni Paganelli
Jun 7, 2003·Colorectal Disease : the Official Journal of the Association of Coloproctology of Great Britain and Ireland·S M RizviS Sarkar
Jan 10, 2004·Endocrine-related Cancer·V J Lewington
Jan 27, 2004·Nuclear Medicine and Biology·Qin WangW Mier
May 22, 2004·Annals of the New York Academy of Sciences·Eric P KrenningMarion de Jong
May 27, 2004·Radiation Research·Bieke LambertAndreas Otte
Jun 3, 2004·Nature Reviews. Drug Discovery·Diane E MilenicMartin W Brechbiel

Citations

Jan 17, 2007·European Journal of Nuclear Medicine and Molecular Imaging·P AntunesHelmut R Maecke
Jan 13, 2012·European Journal of Nuclear Medicine and Molecular Imaging·Markus EsslerChristof Seidl
Dec 4, 2012·Chemical Reviews·Cathy S CutlerSilvia S Jurisson
Nov 10, 2007·Dalton Transactions : an International Journal of Inorganic Chemistry·Martin W Brechbiel
Nov 23, 2006·Cancer Imaging : the Official Publication of the International Cancer Imaging Society·Martin GotthardtWim J G Oyen
May 11, 2012·Neuroendocrinology·Eva Forssell-AronssonHåkan Ahlman
Jun 8, 2012·BioDrugs : Clinical Immunotherapeutics, Biopharmaceuticals and Gene Therapy·Hetal Pandya, Waldemar Debinski
Feb 26, 2011·Endocrinology and Metabolism Clinics of North America·Guillaume NicolasFlavio Forrer
Mar 31, 2010·Seminars in Nuclear Medicine·E Dadachova
Jun 3, 2008·Advanced Drug Delivery Reviews·Matthias MiedererMichael R McDevitt
Mar 27, 2007·Best Practice & Research. Clinical Endocrinology & Metabolism·Flavio ForrerEric P Krenning
May 24, 2008·International Journal of Cancer. Journal International Du Cancer·Mitsuyoshi YoshimotoKeiichi Kawai
Aug 1, 2015·Cancer Gene Therapy·M ShahE Dadachova
Feb 17, 2015·Nuclear Medicine and Biology·Justin J WilsonEva R Birnbaum
Apr 17, 2015·BioMed Research International·Caiyun Xu, Hong Zhang
Feb 25, 2015·Cancer Biotherapy & Radiopharmaceuticals·Ashutosh DashFurn F Russ Knapp
Nov 1, 2013·Chemical Society Reviews·Eric W Price, Chris Orvig
Mar 17, 2016·PloS One·Laëtitia DorsoFrançois Davodeau
Feb 10, 2018·Targeted Oncology·Mehran MakvandiJeffrey P Norenberg
Apr 4, 2018·Chemical Biology & Drug Design·Agnieszka Majkowska-PilipAlfred Morgenstern
Mar 24, 2020·Cancer Biotherapy & Radiopharmaceuticals·Hossein Jadvar
Apr 20, 2013·Chemical Communications : Chem Comm·Caterina F Ramogida, Chris Orvig
Jul 6, 2019·Clinical and Translational Medicine·Mariangela TorniaiRossana Berardi
Nov 30, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Narges K TafreshiDavid L Morse
Sep 6, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Romain EychenneNicolas Lepareur
Jun 4, 2008·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Matthias MiedererMarkus Essler
Mar 31, 2019·Molecular Cancer Therapeutics·Tania A Rozgaja StallonsJulien J Torgue

Related Concepts

Octreotide, DOTA-Tyr(3)-
Bismuth
Medicinal Plants Testing, Preclinical
Malignant Neoplasm of Pancreas
Radioisotopes
Rats, Inbred Lew
Sandostatin
Somatostatin Receptor

Related Feeds

Cancer Genomics (Keystone)

Cancer genomics approaches employ high-throughput technologies to identify the complete catalog of somatic alterations that characterize the genome, transcriptome and epigenome of cohorts of tumor samples. Discover the latest research using such technologies in this feed.