A2A Receptor Antagonist

EOS100850 - Presently in Phase 1 clinical trials

  • Extracellular adenosine is a major mechanism of 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 EOS1000850, a best-in-class proprietary A2A receptor antagonist which has the highest selectivity for the A2A receptor and has a remarkably tight-binder profile enabling inhibition of suppression of T-cell activation even at the high adenosine levels found in tumors. EOS1000850 has been designed to not cross the blood-brain barrier and demonstrates superior pharmacodynamics for complete target coverage. 
  • EOS1000850 entered clinical phase 1 in January 2019.

A2A Small Molecule Antagonist