ERB041

ERB041 is a highly selective small molecule agonist of the estrogen receptor beta (ERβ), originally developed by Wyeth (now Pfizer). It exhibits significant selectivity for ERβ over the alpha isoform (ERα), often reported as greater than 200-fold. ERB041 has been investigated for its potential anti-inflammatory and tissue-protective effects in various conditions, including rheumatoid arthritis, endometriosis, and inflammatory bowel disease. In the context of ulcerative colitis, ERB041 has been shown to alleviate intestinal inflammation and maintain epithelial barrier integrity by activating ERβ, which subsequently induces autophagy through the HIF-1α and ATG-9a signaling axis. Although it reached Phase 2 clinical trials for rheumatoid arthritis, development for that indication was discontinued after failing to meet primary efficacy endpoints.

Other names

ERB-041ERB041ERB 041