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ZEN003694 + binimetinib
- Development stage
- Unknown
- Lead developer
- Zenith Epigenetics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
ZEN003694 + binimetinib is an investigational combination therapy being developed for the treatment of advanced or metastatic solid tumors, specifically those harboring RAS pathway alterations and triple-negative breast cancer (TNBC). ZEN003694 is an oral small molecule inhibitor of the bromodomain and extra-terminal (BET) family of proteins (including BRD2, BRD3, and BRD4), which are epigenetic readers that regulate the transcription of genes involved in cell growth and survival. Binimetinib is an oral, potent, and selective inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1/2), key components of the MAPK/ERK signaling pathway. Preclinical evidence suggests that BET inhibition can sensitize tumors to MEK inhibitors and overcome acquired resistance by suppressing the upregulation of alternative signaling pathways. This combination is currently being evaluated in Phase 1/2 clinical trials sponsored by the National Cancer Institute (NCI) in collaboration with Zenith Epigenetics and Pfizer.
- Brand names
- Mektovi
- Other names
- BET Bromodomain Inhibitor ZEN-3694
02
Targets
BRD4 (Bromodomain-containing protein 4)MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)BRDT (Bromodomain testis-specific protein)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)BRD2 (Bromodomain-containing protein 2)BRD3 (Bromodomain-containing protein 3)
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