inupadenant

Inupadenant is an orally bioavailable small molecule immune checkpoint inhibitor that acts as a selective antagonist of the adenosine A2A receptor (ADORA2A). By blocking this receptor on T lymphocytes, it prevents tumor-derived adenosine from suppressing immune cell activity. This leads to enhanced proliferation and activation of T-cells and stimulates a T-cell-mediated anti-tumor immune response. Inupadenant has been investigated primarily for advanced solid tumors and non-small cell lung cancer (NSCLC), both as monotherapy and in combination with chemotherapy. The drug was developed by iTeos Therapeutics but has recently been deprioritized after Phase II trials showed efficacy comparable to existing standard-of-care treatments[1][4][5][6][7][9].

Other names

inupadenant [INN]inupadenant [USAN]A2A Receptor Antagonist EOS100850A-2A Receptor Antagonist EOS100850A 2A Receptor Antagonist EOS100850Thiazolo(5,4-E)(1,2,4)triazolo(1,5-C)pyrimidin-2(3H)-one, 5-amino-3-(2-(4-(2,4-difluoro-5-(2-((S)-methylsulfinyl)ethoxy)phenyl)-1-piperazinyl)ethyl)-8-(2-furanyl)-