Drug intelligence / Profile preview

ZL0742

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

Overview

ZL0742 is a potent and specific small molecule inhibitor of bromodomain-containing protein 4 (BRD4), an epigenetic reader protein involved in the regulation of inflammatory gene expression. Developed for the treatment of inflammatory bowel disease (IBD), including ulcerative colitis and Crohn's disease, ZL0742 is designed to suppress mucosal inflammation and prevent the progression to chronic disease states. To improve therapeutic outcomes and minimize systemic toxicity, ZL0742 has been formulated using nanoparticle-encapsulation technology, specifically employing a PEGylated poly(lactic-co-glycolic acid) (PLGA) matrix. This delivery system facilitates localized mucosal targeting and sustained release within the inflamed intestinal epithelium. Preclinical studies in animal models of dextran sulfate sodium (DSS)-induced and oxazolone-induced colitis have demonstrated that oral administration of nano-encapsulated ZL0742 effectively blocks colonic inflammation at significantly lower doses than systemic administration.

02

Targets

BRD4 (Bromodomain-containing protein 4)

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