AhR agonists suggested as potential therapeutic agents built on evidence from cell culture or animal studies
| Name of Agonist or Antagonist | Disease Involved | Cell/Animal Studies | Human Trials | Reference |
|---|---|---|---|---|
| E/Z-2-Benzylindene-5,6-dimethoxy-3,3-dimethylindan-1-one | UVB-induced skin damage (cancer, skin aging) | Cells | 10 volunteers | Tigges et al., 2014 |
| 6-Methyl-1,3,8-trichlorodibenzofuran (a so-called selective AhR modulator) | Breast cancer, prostate cancer, metastasis, lung cancer | Cells | No | Fritz et al., 2009; Zhang et al., 2012 |
| Tranilast | Breast cancer | Cells, animals | No | Prud'homme et al., 2010 |
| Leflunomide | Melanoma | Cells | No | |
| 6,2′,4′-Trimethoxyflavone and GNF351 | Head and neck cancer | Cells | No | DiNatale et al., 2012 |
| Sulindac, leflunomide, 4-hydroxytamoxifen, mexiletine, and omeprazole | Cancer, bone preservation | Cells | No | Jin et al., 2012 |
| VAF347 | Inflammation, transplant acceptance, IL-22 induction | Cells, animals | Hauben et al., 2008; Lawrence et al., 2008; Baba et al., 2012 | |
| Aminoflavone | Breast cancer, renal cancer | Phase II | Loaiza-Pérez et al., 2004; Callero et al., 2012 | |
| ITE | Autoimmunity | Animals | No | Yeste et al., 2012 |
| FICZ | Irritable bowel disease | Human cells, animals | No | Monteleone et al., 2011 |
| Kynurenine inhibitor | Glioblastoma | Human cells | No | Opitz et al., 2011 |
| FICZ, kynurenine, and 3,3′-diindolylmethane | NK cell antitumor activity | Cells, animals | No | Shin et al., 2013 |
| StemRegenin 1 | Expansion of hematopoietic stem cells | Cells | No | Boitano et al., 2010 |
| Coal tar | AD | Skin cultures | van den Bogaard et al., 2013 |