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VECTORISATIONS ACTIVE ET PASSIVE DE RADIOPHARMACEUTIQUES DU TECHNETIUM-99m ET DU RHENIUM-188 POUR L'IMAGERIE MEDICALE ET LA THERAPIE

Abstract : Research for new molecules for nuclear medicine is a field in constant development. Over the past few years, development of new radiopharmaceuticals for radiotherapy has renewed interest for rhenium chemistry. Indeed, its two isotopes 186Re and 188Re, owing to their ideal properties and their similitude with 99mTc, which is widely used as a radiotracer for diagnostic imaging, seem very promising for the preparation of radiopharmaceuticals.
In the first part of this manuscript, the synthesis of rhenium and technetium-99 complexes, [M(RPhCS3)2(RPhCS2)] (M = Re, Tc), is described. The preparation of technetium-99m based radiopharmaceuticals, analogues to the pondered complexes, is also described. The stability/reactivity of these complexes has been studied by exchange reactions with potential ligands, specially dithiocarbamates, and also by UV-visible absorption spectroscopy and thermogravimetry.
The reactivity of the complexes towards dithiocarbamates leads to the possibility to bind biomolecules to the metallic core, via the dithiocarbamate moiety. This method represents a potential alternative to current ones using the so-called bifunctional approach.

In the second part of this manuscript, a new kit formulation for the 188Re labeling of lipiodol is described, using a complex analogous to those described in the previous part. The labeled oil is a potential cure for hepatocellular carcinoma. The in vitro and in vivo stability of this 188Re-SSS lipiodol and of its analogue 99mTc-SSS lipiodol has been studied, and also their in vivo behavior in healthy pigs.
This study has shown the quasi-exclusive hepatic fixation of the radiopharmaceutical, and has proven its good stability. Its selectivity for tumors remains to be shown before trying it on humans.
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Submitted on : Friday, February 2, 2007 - 10:08:00 AM
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Nicolas Lepareur. VECTORISATIONS ACTIVE ET PASSIVE DE RADIOPHARMACEUTIQUES DU TECHNETIUM-99m ET DU RHENIUM-188 POUR L'IMAGERIE MEDICALE ET LA THERAPIE. Autre. Université Rennes 1; Università degli studi di Ferrara, 2003. Français. ⟨tel-00128645⟩

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