A2A Receptor Antagonist

  • Extracellular adenosine is a major mechanism to control immune response in acute or chronic inflammation. In the tumor microenvironment, it plays a key role in immunosuppression.
  • Scientific, preclinical and early clinical data have demonstrated that disruption of the adenosine-cancer-immune cell axis through inhibition of the A2A receptor promotes anti-tumor immune responses and leads to tumor regression. iTeos has designed EOS-850, a best-in-class proprietary A2A receptor antagonist which has the highest selectivity for the A2A receptor and has a remarkably tight-binder profile, maintaining potency in the high adenosine concentrations found in the tumor microenvironment. EOS-850 has been designed to not cross the blood-brain barrier and demonstrates superior pharmacodynamics for complete target coverage.
  • EOS-850 completed dose escalation in 1Q2020 and started expansion in monotherapy and in PD-1 or chemo combinations in different indications.
Adenosine pathway