Unmet Need: Gastrointestinal (GI) fibrosis, the accumulation of scar tissue in the intestinal wall as a complication in common GI autoimmune diseases such as ulcerative colitis (UC) and Crohn’s disease (CD), leads to intestinal strictures, abdominal pain, and reduced intestinal motility. Current pharmacological and surgical treatment methods have significant limitations and do not prevent fibrosis recurrence. Disclosed herein is a novel use of azole derivatives, such as sulconazole, to prevent or treat fibrotic disease and improve patient outcome.
Advantages disclosed herein:
· Novel use and pharmaceutical composition of sulconazole
· Potent anti-fibrotic activity in vitro
· Effective at low doses, minimizing possible adverse effects
· In vivo anti-fibrotic activity and repression of fibrotic genes
Technology Overview: Researchers at Johns Hopkins University discovered a novel use of sulconazole to prevent and treat fibrotic disease. Briefly, a known compound library screen identified sulconazole as having anti-fibrotic activity. Sulconazole outperformed pulmonary fibrosis drug pirfenidone in vitro, by demonstrating greater potency, at lower concentrations, whilst having minimal impact on cell survival. Similarly, sulconazole more effectively repressed fibrotic gene expression in an in vivo mouse model, validating its potent anti-fibrotic activity.
Stage of Development: Preclinical in vivo data
Publication: Gastroenterology. 2023 May;164(6):937-952.e13. doi:10.1053/j.gastro.2023.01.006. Epub 2023 Jan 16.