Advanced Accelerator Applications

Bracco Imaging S.p.a.

Michele Saviano

Carlo Pedone

Laura Zaccaro

Annarita Del Gatto

Stefania De Luca

Giancarlo Morelli

Diego Tesauro

The present invention is related to new peptide antagonists of &#x3b1;&#x3b2;receptor, designed on the basis of the crystal structure of integrin &#x3b1;&#x3b2;in complex with c(RGDf[NMe]V) and the NMR structure of echistatin. These peptides are potent and selective antagonists of the &#x3b1;&#x3b2;receptor and can be used as novel anticancer drugs and/or new class of diagnostic non-invasive tracers as suitable tools for &#x3b1;&#x3b2;-targeted therapy and imaging.

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Selective &#x3b1;v&#x3b2;3 receptor peptide antagonist for therapeutic and diagnostic applications

This patent application describes the preparation of cyclic and branched peptides of general formula (I) and their conjugated derivatives labelled with a paramagnetic or radioactive metal. The compounds of the present invention are used as diagnostic agents to identify and locate primary tumours and their metastases which over-express type A and/or B cholecystokinin receptors, and as therapeutic agents and cholecystokinin agonists or antagonists.

Preparation and use of cyclic and branched peptides and their labelled derivatives as therapeutic agents, cholecystokinin agonists or antagonists, and diagnostic agents to identify and locate tumours

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Milan, Italy

Michele Saviano