YZJ-5053

YZJ-5053 is an orally bioavailable small molecule antagonist targeting both the adenosine A2A receptor (A2AR; ADORA2A) and the adenosine A2B receptor (A2BR; ADORA2B). By blocking these immunomodulatory checkpoint molecules, YZJ-5053 competes with tumor-released adenosine for binding to A2AR and A2BR expressed on various intra-tumoral immune cells, including dendritic cells, natural killer cells, macrophages, and T lymphocytes. This mechanism is designed to counteract the immunosuppressive effects of adenosine in the tumor microenvironment and enhance anti-tumor immune responses. The drug is being developed primarily for advanced solid tumors.