CONTEXT

The direct imaging of living cells has become a fundamental tool to study biological processes in real-time, noninvasively, directly within a living organism.
Despite real progress in noninvasive imaging, methods and imaging agents that are more sensitive and more specific are still necessary. In particular, it is advantageous to have probes able to detect a broader spectrum of tumor types, to improve the contrast between the tumor zone and non-specific sites, and to minimize accumulation in healthy tissues.
Integrins are transmembrane cell adhesion receptors located on the cell’s surface which bind to molecules of the extracellular matrix. In particular, αVβ3 and αVβ5 integrins are expressed in many tumor cells such as glioblastoma, melanoma, and carcinomas of breast and ovaries. αVβ3 and αVβ5 integrins are strongly expressed in activated endothelial cells during tumor neovascularization but relatively absent in quiescent endothelial cells and in most healthy tissues. And clinical observations have shown a direct correlation between integrin expression rates and tumor progression. Consequently, αVβ3 and αVβ5 integrins are an attractive target in the detection of tumor and metastatic growth.

TECHNICAL DESCRIPTION

This invention concerns novel imaging agents comprising an integrin receptor targeting ligand, the process for the preparation thereof, and pharmaceutical compositions containing same and use thereof for diagnostic purposes.

BENEFITS

These compounds have important advantages over current imaging agents:

• Detection of a broader spectrum of tumor types
• Excellent discrimination between healthy tissue and tumor structures
• Minimum accumulation in healthy tissues

INDUSTRIAL APPLICATIONS

The main application is in the oncology area. This innovation could be used for:

• In vivo imaging / In vivo diagnosis : especially for diagnostic imaging of hard to detect cancers and in situations where the tumour environment complicates precise discrimination between healthy tissue and tumour structures. It is a matter in particular of deep thoracic and abdominal areas having tissue or vascular background noise in intraoperative imaging or fibroscopic imaging.
• Drug development / Screening

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