BAY-218

BAY-218 (also known as BAY-2335218) is a potent and selective small-molecule antagonist of the aryl hydrocarbon receptor (AhR), originally developed by Bayer AG. By inhibiting AhR, the compound prevents its nuclear translocation and the subsequent expression of AhR-regulated target genes, such as those induced by dioxin response elements (DRE). In the tumor microenvironment, AhR activity often contributes to immune suppression; BAY-218 counteracts this by stimulating pro-inflammatory monocyte and T-cell responses, thereby driving anti-tumor immunity and reducing tumor growth. Preclinical studies have demonstrated that BAY-218 has an IC50 of 39.9 nM in U87 glioblastoma cells and shows monotherapeutic efficacy comparable to immune checkpoint inhibitors. Furthermore, its therapeutic effect is enhanced when used in combination with anti-PD-L1 antibodies, making it a promising candidate for the treatment of various cancers and conditions characterized by dysregulated immune responses.

Other names

AHR antagonist 1