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birabresib
- Development stage
- Phase 1
- Lead developer
- Merck
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Birabresib is an experimental small molecule inhibitor targeting the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins BRD2, BRD3, and BRD4. It binds to the acetylated lysine recognition motifs on these bromodomains preventing their interaction with acetylated histone peptides. This disrupts chromatin remodeling and gene expression regulation of growth-promoting genes such as c-Myc-dependent targets leading to inhibition of tumor cell proliferation. Birabresib is under clinical investigation primarily for various cancers including nuclear protein in testis midline carcinoma (NMC), triple negative breast cancer (TNBC), non-small cell lung cancer (NSCLC), castration-resistant prostate cancer (CRPC), leukemia and glioblastoma. The drug was initially developed by Mitsubishi Tanabe Pharma Corporation and later licensed by OncoEthix; it is currently in development by Merck & Co.[1][2][5][9]
- Other names
- 2-[(6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thienol[3,2,-f]-[1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl]-N-(4-hydroxyphenyl)-acetamide
02
Targets
BRD2 (Bromodomain-containing protein 2)BRD3 (Bromodomain-containing protein 3)BRD4 (Bromodomain-containing protein 4)
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