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ZEN003694 + entinostat
- Development stage
- Unknown
- Lead developer
- Zenith Epigenetics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
ZEN003694 + entinostat is an investigational combination therapy consisting of the BET bromodomain inhibitor ZEN003694 and the histone deacetylase (HDAC) inhibitor entinostat. ZEN003694, developed by Zenith Epigenetics, is a small molecule designed to inhibit the bromodomain and extra-terminal (BET) family of proteins, which are epigenetic readers that often drive oncogenic gene expression in various cancers. Entinostat is a selective Class I HDAC inhibitor that modifies chromatin structure to alter gene expression and inhibit tumor cell proliferation. This combination is currently being evaluated in a Phase Ib/II clinical trial (NCT05053971) sponsored by the National Cancer Institute (NCI) for the treatment of advanced or refractory solid tumors, with a specific expansion cohort for pancreatic cancer and lymphomas. The treatment is administered orally and aims to synergistically target epigenetic regulators to overcome treatment resistance.
- Other names
- entinostatZEN-3694ZEN3694ZEN 3694
02
Targets
HDAC1 (Histone Deacetylase 1)BRDT (Bromodomain testis-specific protein)BRD2 (Bromodomain-containing protein 2)BRD3 (Bromodomain-containing protein 3)BRD4 (Bromodomain-containing protein 4)
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