Introduction

The invention relates with the use of the compound 1-piperidin propionic acid (1-PPA) for the treatment or prevention of the numerous pathologies known to be related to the overactivation of the protease-activated receptor 2 (PAR2). 1-PPA acts by inhibiting the action of the receptor, producing anti-inflammatory, pain-relieving, antithrombotic effects.

Technical features

The PAR2 receptor has been implicated in a wide range of diseases, including severe inflammatory states such as septic shock, cancer, degenerative diseases and chronic pain, but as of today, there are no known clinically authorised effective PAR2 inhibitors.

The invention concerns the use of 1-PPA compound as a PAR2 inhibitor. In vitro experiments have shown that 1-PPA inhibits even at low dosages the synthesis of new PAR2 molecules (transcriptional control) and its activity (functional control).

In vitro and in vivo studies on PAR2-related disease models show therapeutic and/or protective effects of 1-PPA in septic shock and acute articular damage, on which it acts as an inhibitor of proinflammatory cytokines, reduces pain perception and reduces platelet aggregation. Further tests are ongoing in models of neurodegenerative diseases and acute and chronic kidney damage.

TRL: 3/4 preclinical phase

Possible Applications

• Treatment and/or prevention of PAR2-related diseases;
• Treatment and/or prevention in the context of prothrombotic risk;
• Treatment and/or prevention of severe sepsis and septic shock;
• Treatment and/or prevention of acute and chronic arthritis;
• Treatment and/or prevention of chronic pain.

Advantages

• Potential applicability in a wide range of diseases;
• Efficacy even at low doses;
• Multiple administration possibilities;
• Easy commercial availability of the compound;
• Low toxicity (in vitro and in vivo experiments).