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ZEN003694 + abemaciclib
- Development stage
- Unknown
- Lead developer
- Zenith Epigenetics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
ZEN003694 + abemaciclib is an investigational combination therapy being evaluated for the treatment of NUT carcinoma, breast cancer, and other advanced solid tumors. ZEN003694 is a small molecule inhibitor of the bromodomain and extra-terminal (BET) family of epigenetic reader proteins, including BRD2, BRD3, and BRD4. By blocking the binding of BET proteins to acetylated histones, it suppresses the transcription of key oncogenes such as MYC. Abemaciclib is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which prevents the phosphorylation of the retinoblastoma (Rb) protein, thereby inducing cell cycle arrest in the G1 phase. The combination is being studied in National Cancer Institute (NCI)-sponsored clinical trials to determine if the dual inhibition of epigenetic regulation and cell cycle progression can enhance anti-tumor activity and overcome resistance in patients with metastatic or unresectable tumors.
- Brand names
- Verzenio
- Other names
- BET Bromodomain Inhibitor ZEN-3694Abemaciclib
02
Targets
BRD4 (Bromodomain-containing protein 4)CDK6 (Cyclin-dependent kinase 6)BRDT (Bromodomain testis-specific protein)CDK4 (Cyclin-dependent kinase 4)BRD3 (Bromodomain-containing protein 3)BRD2 (Bromodomain-containing protein 2)
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