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molibresib (GSK)
- Development stage
- Discontinued
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Molibresib (also known as I-BET or I-BET-762) is an orally bioavailable small molecule inhibitor of the bromodomain and extra-terminal (BET) family of proteins, which includes BRD2, BRD3, BRD4, and BRDT. Developed by GSK, molibresib acts as a synthetic histone mimic that binds to the acetyl-lysine recognition pocket of BET proteins, thereby preventing their interaction with acetylated histones on chromatin. This disruption blocks the recruitment of transcription factors and chromatin remodeling complexes, leading to the downregulation of key oncogenic and pro-inflammatory genes, such as MYC, BCL2, and IL-6. Molibresib has been evaluated in clinical trials for various oncology indications, including NUT midline carcinoma, acute myeloid leukemia, myelodysplastic syndrome, and other advanced solid tumors and hematological malignancies. However, its clinical development has been largely discontinued due to dose-limiting toxicities, particularly thrombocytopenia and gastrointestinal adverse events.
- Other names
- I-BETmolibresib besylate
02
Targets
BRD2 (Bromodomain-containing protein 2)BRD3 (Bromodomain-containing protein 3)BRD4 (Bromodomain-containing protein 4)BRDT (Bromodomain testis-specific protein)
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