BAY-218 (AHR antagonist 1) is a novel, selective, and potent AhR small molecule inhibitor. BAY-218 inhibits AhR nuclear translocation, dioxin response element (DRE)-luciferase reporter expression, and AhR-regulated target gene expression induced by both exogenous and endogenous AhR ligands[1].
In vitro, BAY-218 (0.1, 0.3 and 1μM; 18h) is able to reverse the inhibitory effect of kynurenic acid (KA) on the production of tumor necrosis factor alpha (TNFα) by lipopolysaccharide (LPS)-stimulated human primary monocytes[2].
In vivo, BAY-218 (30mg/kg; twice daily; p.o.) enhanced the therapeutic effect of anti-PD-L1 antibody in the CT26 mouse tumor model[2].
References:
[1] Gutcher I, Kober C, Roese L, et al. Abstract 1288: Blocking tumor-associated immune suppression with BAY-218, a novel, selective aryl hydrocarbon receptor (AhR) inhibitor[J].Experimental and Molecular Therapeutics, 2019.
[2] Schmees N, Gutcher I, Irlbacher H, et al. 3-oxo-2,6-diphenyl-2,3-dihydropyridazine-4-carboxamides: US201716303539[P]. US11040035B2[2025-10-07].
BAY-218 (AHR antagonist 1)是一种新型的、选择性的、强效的AhR小分子抑制剂。BAY-218能够抑制AhR核转位、二噁英反应元件（DRE）-荧光素酶报告基因表达，以及由外源性和内源性AhR配体诱导的AhR调节靶基因表达[1]。
在体外实验中，BAY-218（0.1, 0.3和1μM; 18小时）能够逆转犬尿氨酸（KA）对脂多糖（LPS）刺激的人原代单核细胞产生肿瘤坏死因子α（TNFα）的抑制作用[2]。
在体内实验中，BAY-218（30mg/kg; 每日两次; 口服）在CT26小鼠肿瘤模型中增强了抗PD-L1抗体的治疗效果[2]。