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BAY 1238097
- Development stage
- Discontinued
- Lead developer
- Bayer
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
BAY 1238097 is a small molecule inhibitor of the bromodomain and extraterminal (BET) domain family of proteins, which play a key role in regulating gene transcription. By inhibiting BET proteins, particularly those involved in MYC- or BRD4-driven cancers, the drug was developed as an antineoplastic agent for various malignancies including solid tumors and hematological cancers. The compound was developed by Bayer and entered phase I clinical trials to assess safety, pharmacokinetics, pharmacodynamics, and preliminary efficacy in patients with advanced refractory malignancies. The development program was terminated after dose-limiting toxicities were observed at subtherapeutic exposures and no feasible dosing regimen could be established to balance efficacy with tolerability[1][2][3][6].
- Other names
- BET inhibitor BAY 1238097
02
Targets
BRD3 (Bromodomain-containing protein 3)BRD4 (Bromodomain-containing protein 4)BRD2 (Bromodomain-containing protein 2)BRDT (Bromodomain testis-specific protein)
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