Drug intelligence / Profile preview

ZL0591

Development stage
Preclinical
Lead developer
The University of Texas Medical Branch at Galveston
Modality
Small Molecules, Nanoparticles → Drug Delivery Systems
Administration
Oral
01

Overview

ZL0591 is a potent and specific small molecule inhibitor of bromodomain-containing protein 4 (BRD4), an epigenetic reader protein that plays a critical role in regulating the expression of inflammatory genes. Developed by researchers at the University of Texas Medical Branch (UTMB), ZL0591 is being investigated as a therapeutic candidate for inflammatory bowel disease (IBD), including ulcerative colitis and Crohn's disease. To overcome challenges associated with systemic administration, such as limited mucosal delivery and potential side effects, ZL0591 has been formulated into nanoparticle-encapsulated delivery systems using PEGylated poly(lactic-co-glycolic acid) (PLGA). Preclinical studies in animal models of dextran sulfate sodium (DSS)-induced and oxazolone-induced colitis have demonstrated that oral administration of nano-encapsulated ZL0591 effectively blocks colonic inflammation at significantly lower doses than systemic administration, suggesting a favorable therapeutic and safety profile for mucosal targeting.

02

Targets

BRD2 (Bromodomain-containing protein 2)BRD3 (Bromodomain-containing protein 3)BRD4 (Bromodomain-containing protein 4)BRDT (Bromodomain testis-specific protein)

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