University of Padua

University Ca' Foscari Venezia

Alessandro Angelini, Laura Cendron, Nicola Frasson, Ylenia Mazzocato

Rheumatoid arthritis, Inhibitors, Bicyclic peptides, Tumour, Urokinase

The human enzyme urokinase – uPA is involved in the degradation of the extracellular matrix, a process associated with metastatic cancer progression or the onset of inflammatory diseases such as rheumatoid arthritis. The bicyclic peptides patented here are able to recognise huPA selectively and block its activity more effectively than other existing inhibitors.

Bicyclic peptides are next-generation therapeutic molecules that display properties similar to monoclonal antibodies (high specificity and affinity for the target protein) and to small molecules (good stability and good tissue penetration). The compounds of the invention are capable of recognising and inhibiting enzymes (huPA) involved in the degradation of the extracellular matrix, thus proving useful in the treatment of pathological conditions, such as primary or metastatic tumour forms and rheumatoid arthritis. These molecules generally have low toxicity and immunogenicity and may be formulated for the therapeutic uses mentioned in pharmaceutical compositions for parenteral administration, possibly in combination with other active ingredients.

• High binding affinity (Ki = 4 nM)
• High target specificity;
• Good tissue penetration;
• High plasma stability;
• High tunability;
• Low toxicity.

• Treatment of cancer, possibly in combination with other active ingredients;
• Treatment of rheumatoid arthritis, possibly in combination with other active ingredients;
• Pharmaceutical compositions for parenteral administration.

Patent entered on 23/08/2022. 

Deadline for expressions of interest: 23/09/2022. 

For information: trasferimento.tecnologia@unipd.it