etrumadenant

Etrumadenant is an orally bioavailable small molecule that acts as a selective dual antagonist of the adenosine A2A receptor (ADORA2A) and A2B receptor (ADORA2B). By blocking these immunomodulatory checkpoint molecules, etrumadenant aims to counteract adenosine-mediated immunosuppression in the tumor microenvironment. Adenosine, often overproduced by tumor cells, suppresses immune cell activity via these receptors on dendritic cells, natural killer cells, macrophages, and T lymphocytes. Etrumadenant inhibits this pathway, thereby enhancing immune cell activation and proliferation to promote anti-tumor responses. The drug is being developed primarily for cancer indications—including metastatic colorectal cancer (mCRC), non-small cell lung cancer (NSCLC), liposarcoma, pancreatic cancer, rectal cancer—and has shown promising results in combination with other therapies such as zimberelimab (anti-PD-1 antibody) and chemotherapy regimens[1][2][4][5][6][7].

Other names

Etruma