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Country report: Italy (Duatti). Development of a Kit Formulation for Labeling Biotin-Derived Ligands with the Re-188 Nitrido Core

Abstract

Within the scope of this CRP, we developed a series of small-molecule biotinylated Re-188 complexes containing the [{sup 188}Re≡N]{sup 2+} core. These complexes have been prepared using different chemical strategies, but all of them incorporate a biologically active biotin group. The main interest for this effort was brought to us after the introduction by Paganelli et al. of a new approach for the treatment of residual malignant cells after surgical removal of a primary breast tumour, and dubbed IART (Intraoperative Avidination for Radionuclide Therapy) [1]. Since now, the IART approach has been applied using {sup 90}Y as therapeutic radionuclide and a DOTA-functionalized biotin ligand for coordination to the radiometal. A major drawback for using {sup 90}Y as a therapeutic radionuclide comes from the absence of any radioactive decay, associated with the main β-emission, that may allow imaging of the actual biodistribution of injected radioactivity in any individual patient. Other therapeutic radionuclides, such as {sup 177}Lu and {sup 188}Re, possess an additional γ emission that easily allows imaging of target’s uptake, and could be conveniently utilized to monitor the course of therapy. In particular, {sup 188}Re emits a β- particle having almost the same energy as that emitted by {sup 90}Y,  More>>
Authors:
Pasquali, M.; Boschi, A.; Uccelli, L.; Duatti, A.; [1]  Janevik-Ivanovska, E. [2] 
  1. Laboratory of Nuclear Medicine, Department of Radiological Sciences, University of Ferrara, 44121 Ferrara (Italy)
  2. University of Stip (Macedonia, The Former Yugoslav Republic of)
Publication Date:
Jul 01, 2010
Product Type:
Conference
Report Number:
IAEA-RC-1088.2
Resource Relation:
Conference: 2. Research Coordination Meeting on The Development of Therapeutic Radiopharmaceuticals Based on {sup 188}Re and {sup 90}Y for Radionuclide Therapy, Vienna (Austria), 22-26 Mar 2010; Other Information: Refs., 3 figs.; Related Information: In: Report on the 2{sup nd} Research Coordination Meeting on The Development of Therapeutic Radiopharmaceuticals Based on {sup 188}Re and {sup 90}Y for Radionuclide. Working Document| 185 p.
Subject:
62 RADIOLOGY AND NUCLEAR MEDICINE; BIOTIN; EMISSION; ITALY; LABELLING; LIGANDS; LUTETIUM 177; MAMMARY GLANDS; NUCLEAR DECAY; PATIENTS; RADIOPHARMACEUTICALS; RADIOTHERAPY; RHENIUM; RHENIUM 188; TECHNETIUM; TECHNETIUM 99; TUNGSTEN 188; YTTRIUM 90
OSTI ID:
22270094
Research Organizations:
International Atomic Energy Agency, Division of Physical and Chemical Sciences, Vienna (Austria)
Country of Origin:
IAEA
Language:
English
Other Identifying Numbers:
TRN: XA14M3062091326
Availability:
Available from INIS in electronic form. Also available on-line: http://www-naweb.iaea.org/napc/iachem/meetings/RCMs/RC-1088-2_report_complete.pdf
Submitting Site:
INIS
Size:
page(s) 81-87
Announcement Date:
Oct 22, 2014

Citation Formats

Pasquali, M., Boschi, A., Uccelli, L., Duatti, A., and Janevik-Ivanovska, E. Country report: Italy (Duatti). Development of a Kit Formulation for Labeling Biotin-Derived Ligands with the Re-188 Nitrido Core. IAEA: N. p., 2010. Web.
Pasquali, M., Boschi, A., Uccelli, L., Duatti, A., & Janevik-Ivanovska, E. Country report: Italy (Duatti). Development of a Kit Formulation for Labeling Biotin-Derived Ligands with the Re-188 Nitrido Core. IAEA.
Pasquali, M., Boschi, A., Uccelli, L., Duatti, A., and Janevik-Ivanovska, E. 2010. "Country report: Italy (Duatti). Development of a Kit Formulation for Labeling Biotin-Derived Ligands with the Re-188 Nitrido Core." IAEA.
@misc{etde_22270094,
title = {Country report: Italy (Duatti). Development of a Kit Formulation for Labeling Biotin-Derived Ligands with the Re-188 Nitrido Core}
author = {Pasquali, M., Boschi, A., Uccelli, L., Duatti, A., and Janevik-Ivanovska, E.}
abstractNote = {Within the scope of this CRP, we developed a series of small-molecule biotinylated Re-188 complexes containing the [{sup 188}Re≡N]{sup 2+} core. These complexes have been prepared using different chemical strategies, but all of them incorporate a biologically active biotin group. The main interest for this effort was brought to us after the introduction by Paganelli et al. of a new approach for the treatment of residual malignant cells after surgical removal of a primary breast tumour, and dubbed IART (Intraoperative Avidination for Radionuclide Therapy) [1]. Since now, the IART approach has been applied using {sup 90}Y as therapeutic radionuclide and a DOTA-functionalized biotin ligand for coordination to the radiometal. A major drawback for using {sup 90}Y as a therapeutic radionuclide comes from the absence of any radioactive decay, associated with the main β-emission, that may allow imaging of the actual biodistribution of injected radioactivity in any individual patient. Other therapeutic radionuclides, such as {sup 177}Lu and {sup 188}Re, possess an additional γ emission that easily allows imaging of target’s uptake, and could be conveniently utilized to monitor the course of therapy. In particular, {sup 188}Re emits a β- particle having almost the same energy as that emitted by {sup 90}Y, but with an associated 155-keV γ-emission that can be efficiently employed for imaging the biodistribution of the injected radiocompound. Considering also that {sup 188}Re is produced through a {sup 188}W/{sup 188}Re transportable generator system, and that deep similarities between the chemistry of congener rhenium and technetium usually allow {sup 99m}Tc compounds to be used for a preliminary evaluation of the biodistribution of the analogous {sup 188}Re compounds, this makes {sup 188}Re as an interesting candidate for application to the IART approach.}
place = {IAEA}
year = {2010}
month = {Jul}
}