Comparison of 225actinium chelates: tissue distribution and radiotoxicity

Nuclear Medicine and Biology
I A DavisStephen J Kennel

Abstract

The biodistribution and tissue toxicity of intravenously administered 225-actinium (225Ac) complexed with acetate, ethylene diamine tetraacetic acid (EDTA), 1, 4, 7, 10, 13-pentaazacyclopentadecane-N, N', N", N"', N"-pentaacetic acid (PEPA), or the "a" isomer of cyclohexyl diethylenetriamine pentaacetic acid (CHX-DTPA), were examined. The percent of injected dose per organ and per gram of tissue for each chelate complex was determined. 225Ac-CHX-DTPA was evaluated further for radiotoxic effects. Mice receiving > or =185 kBq 225Ac-CHX-DTPA suffered 100% morbidity by 5 days and 100% mortality by 8 days postinjection, and all animals evaluated had significant organ damage. The in vivo instability of the 225Ac-CHX-DTPA complex likely allowed accumulation of free 225Ac in organs, which resulted in tissue pathology.

References

Sep 1, 1970·Health Physics·D M Taylor
Feb 1, 1993·Nuclear Medicine Communications·M W GeerlingsR van der Hout
Jun 10, 1998·Nuclear Medicine and Biology·Stephen J Kennel, Saed Mirzadeh
May 15, 2002·Radiation Research·Stephen J KennelMartin W Brechbiel
Feb 1, 1960·Health Physics·P W DURBIN

Citations

Apr 21, 2005·European Journal of Nuclear Medicine and Molecular Imaging·Olivier CouturierMichel Cherel
Dec 7, 2011·Tumour Biology : the Journal of the International Society for Oncodevelopmental Biology and Medicine·Young-Seung Kim, Martin W Brechbiel
Aug 17, 2002·Pharmacology & Therapeutics·Andreas Goutopoulos, Alexandros Makriyannis
Sep 28, 2001·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·D MaDavid A Scheinberg
Oct 31, 2002·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·Michael R McDevittDavid A Scheinberg
Jun 8, 2001·Nuclear Medicine and Biology·Kayhan GarmestaniMartin W Brechbiel
Aug 15, 2000·Cancer Biotherapy & Radiopharmaceuticals·Stephen J KennelSaed Mirzadeh
May 28, 2002·Cancer Biotherapy & Radiopharmaceuticals·Stephen J KennelSaed Mirzadeh
Feb 26, 2014·Biochimica Et Biophysica Acta·Pinakin SukthankarJohn M Tomich
Jun 13, 2015·Pharmaceuticals·Robin M de KruijffAntonia G Denkova
Jun 3, 2008·Advanced Drug Delivery Reviews·Matthias MiedererMichael R McDevitt
Apr 15, 2014·Nihon rinsho. Japanese journal of clinical medicine·Nozomi Niitsu
Apr 20, 2004·Nuclear Medicine and Biology·Gjermund HenriksenRoy H Larsen
Feb 17, 2015·Nuclear Medicine and Biology·Justin J WilsonEva R Birnbaum
Sep 19, 2006·International Journal of Radiation Oncology, Biology, Physics·Gerald L DeNardoSally J DeNardo
Mar 15, 2005·Applied Radiation and Isotopes : Including Data, Instrumentation and Methods for Use in Agriculture, Industry and Medicine·Rose A BollSaed Mirzadeh
Aug 18, 2017·Chemistry : a European Journal·Peter CombaMiriam Starke
Jun 12, 2018·Cancer Biotherapy & Radiopharmaceuticals·Nikki A Thiele, Justin J Wilson
Oct 1, 2017·Angewandte Chemie·Nikki A ThieleJustin J Wilson
Feb 21, 2020·Cancer Biotherapy & Radiopharmaceuticals·Sture LindegrenEmma Aneheim
May 23, 2020·The Quarterly Journal of Nuclear Medicine and Molecular Imaging : Official Publication of the Italian Association of Nuclear Medicine (AIMN) [and] the International Association of Radiopharmacology (IAR), [and] Section of the Society of Radiopharmaceutica·Dayana Castillo SeoaneMichel Koole
Aug 14, 2019·Scientific Reports·R M de KruijffA G Denkova
Nov 30, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Narges K TafreshiDavid L Morse
May 8, 2004·Clinical Cancer Research : an Official Journal of the American Association for Cancer Research·Zhengsheng YaoJorge A Carrasquillo
Jun 3, 2005·Cancer Research·Jaspreet S JaggiDavid A Scheinberg
Feb 10, 2021·Nuclear Medicine and Biology·Jasmine L Hatcher-LamarreLynn C Francesconi

Related Concepts

(1alpha(R*),2beta)-(+-) of N-(2-amino-3-(4-isothiocyanatophenyl)propyl)cyclohexane-1,2-diamine-N, N', N', N'', N''-pentaacetic acid
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