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trotabresib
- Development stage
- Phase 1
- Lead developer
- Bristol Myers Squibb
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Trotabresib is an orally bioavailable, potent, and reversible small molecule inhibitor of the bromodomain and extra-terminal (BET) family of proteins, which includes BRD2, BRD3, BRD4, and BRDT. It preferentially binds to the second bromodomain (BD2) of BET proteins, preventing their interaction with acetylated histones. This disrupts chromatin remodeling and gene expression by inhibiting transcriptional regulators involved in cellular growth and proliferation. The inhibition of BET proteins leads to downregulation of growth-promoting genes in tumor cells with overexpressed BET activity, resulting in antineoplastic effects. Trotabresib is under clinical investigation for various solid tumors and hematologic malignancies[1][2][3][6][9].
- Brand names
- trotabresib
- Other names
- Bet inhibitor cc-90010Trotabresib [USAN]TROTABRESIB [INN]4-[2-(cyclopropylmethoxy)-5-methylsulfonylphenyl]-2-methylisoquinolin-1-one
02
Targets
BRDT (Bromodomain testis-specific protein)BRD2 (Bromodomain-containing protein 2)BRD4 (Bromodomain-containing protein 4)BRD3 (Bromodomain-containing protein 3)
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