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BI 894999
- Development stage
- Phase 1
- Lead developer
- Boehringer Ingelheim
- Modality
- Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
BI 894999 (also known as amredobresib) is a potent, orally bioavailable small molecule inhibitor targeting the bromodomain and extraterminal domain (BET) family of proteins, including BRD4. BET proteins are epigenetic readers that regulate gene expression by binding to acetylated lysines on histone tails. By inhibiting these interactions, BI 894999 disrupts oncogenic transcriptional programs, particularly in cancers driven by BRD-NUT fusions such as NUT carcinoma. The drug has demonstrated preclinical antitumor activity and has been evaluated in phase I clinical trials for advanced solid tumors and hematological malignancies, including diffuse large B-cell lymphoma (DLBCL), small cell lung cancer (SCLC), colorectal cancer (CRC), metastatic castration-resistant prostate cancer (mCRPC), and NUT carcinoma. While monotherapy efficacy was limited in clinical studies, combination strategies—especially with p300/CBP inhibitors like CCS1477—are being explored due to promising synergistic effects[1][2][3][4][6].
- Other names
- BET inhibitor BI 894999amredobresib
02
Targets
BRD4 (Bromodomain-containing protein 4)
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