bivemetinib

Bivemetinib (CC-90010) is an orally bioavailable, potent, and reversible small-molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, specifically targeting the bromodomains of BRD2, BRD3, and BRD4. Developed by Celgene (now Bristol Myers Squibb), bivemetinib functions as an epigenetic modulator by competitively binding to the acetyl-lysine recognition site of BET proteins, thereby preventing their interaction with acetylated histones and transcription factors. This inhibition leads to the downregulation of key oncogenic genes, most notably MYC, which is frequently overexpressed in various hematologic and solid malignancies. Bivemetinib has been investigated in clinical trials for the treatment of advanced solid tumors (including glioblastoma), relapsed or refractory diffuse large B-cell lymphoma (DLBCL), and multiple myeloma.

Other names

2-(3-(3,5-dimethyltriazol-4-yl)-5-((S)-oxan-4-yl(phenyl)methyl)pyrido(3,2-b)indol-7-yl)propan-2-ol2-(3-(3,5-dimethyl-4H-1,2,4-triazol-4-yl)-5-((S)-phenyl(tetrahydro-2H-pyran-4-yl)methyl)-5H-pyrido[3,2-b]indol-7-yl)propan-2-ol