Product Description
An inhibitor of the Bromodomain (BRD) and Extra-Terminal domain (BET) family of proteins, with potential antineoplastic activity. Upon administration, the BET inhibitor BAY1238097 binds to the acetylated lysine recognition motifs on the BRD of BET proteins, thereby preventing the interaction between BET proteins and histones. This disrupts chromatin remodeling and prevents the expression of certain growth-promoting genes. This leads to an inhibition of tumor cell growth. BET proteins (BRD2, BRD3, BRD4 and BRDT) are transcriptional regulators that bind to acetylated lysines on the tails of histones H3 and H4, and regulate chromatin structure and function; they play an important role in the modulation of gene expression during development and cellular growth. (Sourced from: https://www.cancer.gov/publications/dictionaries/cancer-drug/def/bet-inhibitor-bay1238097)
Mechanisms of Action: BET Inhibitor
Novel Mechanism: Yes
Modality: Small Molecule
Route of Administration: Oral
FDA Designation: None *
Approval Status: Not Approved
Approved Countries: None
Approved Indications: None
Known Adverse Events: None
Company: Elanco Animal Health
Company Location:
Company CEO:
Additonal Commercial Interests: None
Clinical Description
Countries in Clinic:
Active Clinical Trial Count:
Highest Development Phases
Phase 1: Small Cell Lung Cancer|Acute Myeloid Leukemia|Multiple Myeloma|NUT Carcinoma|Non-Small-Cell Lung Cancer|Melanoma|Lymphoma
Trial |
Phase |
Trial Status |
Disease |
Primary Completion Date |
Probability of Success |
|---|---|---|---|---|---|
| NCT02369029 | P1 |
Terminated |
NUT Carcinoma|Multiple Myeloma|Lymphoma|Small Cell Lung Cancer|Acute Myeloid Leukemia|Melanoma|Non-Small-Cell Lung Cancer |
2016-01-01 |