ASKC189

ASKC189 is an investigational, orally bioavailable small molecule antagonist of the Prostaglandin E2 receptor subtype 4 (EP4), developed by Adlai Nortye. The EP4 receptor is a G protein-coupled receptor that mediates the effects of Prostaglandin E2 (PGE2) in the tumor microenvironment, leading to significant immunosuppression. By selectively blocking the EP4 receptor, ASKC189 inhibits PGE2-induced signaling that typically promotes the expansion and activation of regulatory T cells (Tregs) and myeloid-derived suppressor cells (MDSCs), while simultaneously inhibiting the activity of effector T cells and natural killer (NK) cells. This mechanism is intended to reprogram the tumor microenvironment from immunosuppressive to immunostimulatory, thereby enhancing the efficacy of the host's anti-tumor immune response. ASKC189 is currently being evaluated in Phase 1 clinical trials as a treatment for various advanced solid tumors, including colorectal cancer, non-small cell lung cancer, and pancreatic ductal adenocarcinoma, both as a monotherapy and in potential combination with immune checkpoint inhibitors.