Birabresib (OTX015, MK 8628) is a potent BET bromodomain inhibitor that inhibits the binding of BRD2, BRD3 and BRD4 to AcH4. OTX-015 shows inhibition of BRD2, BRD3 and BRD4 with IC50 values in the range of 92 – 112 nM. OTX 015 exhibits sub-micromolar antiproliferative effects in vitro against multiple solid tumor types and leukemias, downregulates c-Myc expression and induces cell cycle arrest and apoptosis. The EC50 ranges from 10 to 19 nM for BRD2, BRD3 and BRD4 in cell-free assays. Birabresib inhibits the expression of nuclear receptor-binding SET domain protein 3 (NSD3) target genes.
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