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OTX-015 is a potent inhibitor of BRD2, BRD3, and BRD4 with IC50 values range from 92 to 112 nM [1].

BRD2, BRD3, and BRD4 belong to BET bromodomain family and play an important role in regulating transcription. BRDs regulate several oncogenes transcription in a variety of cancers and thus have emerged as a promising target [2].

OTX-015 is a selective BRD2, BRD3, and BRD4 inhibitor and inhibits the binding of BRD2, BRD3, and BRD4 to AcH4. Using TR-FRET method and CHO cell lysate harboring BRD2, BRD3, and BRD4 to research the effect of OTX-015, result showed that OTX-015 inhibited BET family binding to AcH4 in a dose-dependent manner and the EC50 values range from 10 to 19 nM. When tested with human tumor cell lines, incubation with OTX-015 for 72 hours inhibited cell proliferation with GI 50 values ranged from 60 to 200 nM [1]. In ALKpos ALCL cell lines, treatment of OTX-015 for 24 h arrested cell proliferation in G1 phase which was more pronounced at 48 h and 72 h, and tested with SUPM2/TS and JB-6 cell lines OTX-015 showed ability to increase cell death rate [3].

In BLAB/c-nu/nu mice model with established Ty82 BRD-NUT midline carcinoma xenografts, oral administration of OTX-015 markedly inhibited tumor growth and reduced tumor volume [1].

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