mivebresib

Mivebresib is an orally administered small molecule inhibitor of the bromodomain and extra-terminal (BET) family of proteins, including BRD2, BRD3, and BRD4. It binds to the acetyl–lysine binding site of these proteins with high affinity (Ki for BRD2/BRD4/T: 1–2.2 nM; Ki for BRD3: ~12 nM), thereby preventing their interaction with acetylated histones. This disrupts chromatin remodeling and transcriptional regulation of genes involved in cancer cell growth and survival. The drug has demonstrated antineoplastic activity in preclinical models across a range of hematologic malignancies and solid tumors by inducing G1 cell-cycle arrest or apoptosis in cancer cells. Developed by AbbVie as a new molecular entity, mivebresib has been evaluated in phase 1/2 clinical trials as monotherapy or in combination (notably with venetoclax) for relapsed/refractory acute myeloid leukemia (AML), advanced solid tumors including uveal melanoma, prostate cancer, breast cancer, pancreatic cancer, head & neck cancers, non-small-cell lung cancers and myelofibrosis[1][5][7][8].

Other names

1445993-26-9Mivebresib [INN]Mivebresib [USAN]N-(4-(2,4-difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamideMFCD30377200MFCD-30377200MFCD 30377200