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2-(3-(3,5-dimethyltriazol-4-yl)-5-((S)-oxan-4-yl(phenyl)methyl)pyrido[3,2-b]indol-7-yl)propan-2-ol

Development stage: Phase 2
Lead developer: Bristol Myers Squibb
Modality: Small Molecules
Administration: Oral

Overview

2-(3-(3,5-dimethyltriazol-4-yl)-5-((S)-oxan-4-yl(phenyl)methyl)pyrido[3,2-b]indol-7-yl)propan-2-ol is a potent, small-molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, including BRD2, BRD3, and BRD4. Developed by Bristol Myers Squibb, this compound (often identified by the code name BMS-986158, although some medicinal chemistry literature specifies the isoxazole analog for that code) is being investigated for the treatment of myelofibrosis and other hematologic malignancies. By binding to the bromodomains of BET proteins, it prevents their interaction with acetylated histones, thereby modulating the expression of key oncogenes such as MYC and BCL2. In clinical trials, it is often evaluated as a monotherapy or in combination with JAK inhibitors like ruxolitinib to overcome resistance and improve therapeutic outcomes in patients with myelofibrosis.

Other names: BET inhibitor BMS-986158ezobresib(S)-2-(3-(1,4-dimethyl-1H-1,2,3-triazol-5-yl)-5-(phenyl(tetrahydro-2H-pyran-4-yl)methyl)-5H-pyrido[3,2-b]indol-7-yl)propan-2-ol

Targets

BRDT (Bromodomain testis-specific protein)BRD4 (Bromodomain-containing protein 4)BRD3 (Bromodomain-containing protein 3)BRD2 (Bromodomain-containing protein 2)

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