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ZEN003694 + capecitabine
- Development stage
- Phase 1
- Lead developer
- Zenith Epigenetics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
ZEN003694 + capecitabine is an investigational combination therapy being evaluated for the treatment of metastatic or unresectable solid tumors, including colorectal cancer. ZEN003694 (ZEN-3694) is an orally bioavailable small molecule inhibitor of the bromodomain and extra-terminal (BET) family of proteins. By binding to the acetyl-lysine binding pockets of BET proteins (such as BRD2, BRD3, and BRD4), ZEN003694 prevents their interaction with acetylated histones, thereby modulating the expression of genes involved in cell cycle progression and apoptosis. Capecitabine is an oral prodrug of 5-fluorouracil (5-FU), an antimetabolite that interferes with DNA synthesis and slows tumor growth. This combination therapy is currently being studied in Phase I clinical trials sponsored by the National Cancer Institute (NCI) to determine safety, tolerability, and the recommended Phase II dose in patients who have progressed on standard therapies.
- Other names
- ZEN-3694 + capecitabine
02
Targets
BRD2 (Bromodomain-containing protein 2)BRD3 (Bromodomain-containing protein 3)TS (Thymidylate synthase)BRD4 (Bromodomain-containing protein 4)
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