prinaberel (ERB-041) / Pfizer - LARVOL DELTA

Estrogen receptor β alleviates colitis in intestinal epithelial cells and activates HIF-1a and ATG-9a-mediated autophagy. (PubMed, Exp Cell Res) - "In vivo, ERβ activation by ERB041 alleviated DSS-induced colitis in mice, reducing weight loss, histopathological damage, and inflammatory cytokine levels...Co-IP and dual luciferase assays revealed that ERβ interacted with HIF-1α and modulated ATG-9a-mediated autophagy. These results indicate that ERβ alleviates intestinal inflammation and activates HIF-1a and ATG-9a-mediated autophagy, providing new insights into the therapeutic potential of targeting ERβ in UC and highlighting its role in maintaining intestinal homeostasis."

Journal • Gastroenterology • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Bowel Disease • Ulcerative Colitis • ER • HIF1A

Estrogen receptor β alleviates colitis in intestinal epithelial cells by activating HIF-1α and ATG-9a mediated autophagy (ECCO-IBD 2025) - "ERB041, an ERβ specific agonist, was administered to DSS-induced mice and LPS-induced HT-29 cells...Furthermore, HIF-1α bound to the promoter region of ATG- 9a, and positively regulates its transcription. Conclusion ERβ exerts anti-inflammatory effect by up-regulating HIF-1α and activating ATG-9a mediated autophagy in intestinal epithelial cells, and may be a promising therapeutic target for UC."

Immunology • Inflammatory Bowel Disease • Ulcerative Colitis • ER • HIF1A

Synergistic Anti-Cancer Effects of ERB-041 and Genistein through Estrogen Receptor Suppression-Mediated PI3K/AKT Pathway Downregulation in Canine Mammary Gland Tumor Cells. (PubMed, Int J Mol Sci) - "We also found a synergistic decrease in the expression of ERα, and the expression of proteins involved in the PI3K/AKT pathway, including p-PI3K, phosphatase and tensin homolog (PTEN), AKT, and mechanistic target of rapamycin (mTOR). In conclusion, ERB-041 and genistein exhibited a synergistic anticancer effect on CMTs, suggesting that cotreatment with ERB-041 and genistein is a promising treatment for CMTs."

IO biomarker • Journal • Tumor cell • Breast Cancer • Oncology • ANXA5 • BAX • BCL2 • CASP3 • CCND1 • CDK4 • ER • mTOR • PTEN