Leiden: New therapeutic candidate for treatment strategies in chronic inflammation

Submitted by Leiden University Research and Innovation Services

Adenosine receptors (ARs) of which four subtypes exist (A1, A2A, A2B, A3) are present in the brain, the heart, the kidneys and the lungs and mediate diverse physiological functions including vasodilatation and fluid retention in the periphery, and cognitive and sleep/wake activity in the brain. Adenosine receptor ligands have numerous promising applications and several drug candidates have been clinically evaluated. However the ubiquity of adenosine receptors and the potential side effects impeded the development of adenosine receptor modulators in the past, despite their great therapeutic potential.

Chemists from Leiden University in the Netherlands have synthesized a novel compound proved to be a dual agonist towards both A2A AR and A3 AR. This compound has high affinity and selectivity for both human adenosine A2a and A3 receptors and showed to exert strong anti-inflammatory effects in various pre-clinical animal models of autoimmune disease.

This new agonist opens opportunities for new treatment strategies in conditions of chronic inflammation (arthritis, colitis, multiple sclerosis) either as stand-alone application of the compound or in combination with other drugs.

Key benefits

• High affinity and selectivity for A2A and A3 adenosine receptors
• Potent anti-inflammatory agent

Applications

• Treatments for autoimmune inflammatory diseases such as multiple sclerosis, Crohn's disease, arthritis.