Introduction

The invention concerns compounds suitable as theranostics for inflammatory processes related to various diseases, including early atherosclerotic lesions and several tumors. The proposed systems involve the use of conjugate derivatives of a commercially available peptide, easily produced, to be associated either with PET imaging radiotracers or with nanoparticles for therapeutic application.

Technical features

These compounds allow to highlight and treat inflammatory processes overexpressing the VCAM-1 protein, exploiting a peptide with specific affinity for it. For imaging purposes, the VCAM-1 binding peptide conjugated with biotin is injected, followed by admistration of avidin (taking advantage its known very high affinity for biotin), and finally injecting a biotinylated radiotracer detectable by PET; for thepeutic purposes, instead, the final step involves the administration of biotinylated nanoparticles delivering drugs. The pretargeting procedure can even be carried out in 1 or 2 steps, pre-complexing the peptide conjugate to avidin and to the nanoparticles. As an alternative, the peptide has been directly conjugated with a radionuclide-chelating macrocycle, to be employed for PET imaging. The disclosed systems can be applied to all pathologies expressing VCAM-1, such as atherosclerosis and various tumors.

Possible Applications

• Atherosclerosis;
• Various forms of tumors (breast, colorectal, melanoma, glioblastoma, etc.);
• Some neurodegenerative pathologies (multiple sclerosis);
• Allograft rejection.

Advantages

• Straightforward procedures;
• Manufacturing processes easily industrialized;
• Theranostics suitable for various pathologies.