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Bromodomain containing 4 (BRD4); BRD2; BRD3

Cell culture and mouse studies suggest BET inhibitors of BRD2, BRD3 and BRD4 could help treat diffuse large B cell lymphoma (DLBCL). In a panel of human cell lines, BET-family inhibitors selectively decreased proliferation of DLBCL and Burkitt lymphoma subtypes compared with vehicle. In mouse xenograft models of human DLBCL, BET-family inhibition decreased DLBCL proliferation and bone marrow infiltration and increased median survival compared with vehicle. In cultured DLBCL cells, BET-family inhibition decreased expression of oncogenes and BRD4 was enriched at enhancers associated with oncogenes and transcription factors important for B cell lineage specification. Next steps include elucidating mechanisms of resistance to BET-family inhibitors and developing combination strategies to counter resistance.
At least seven companies have BET bromodomain inhibitors in preclinical through Phase II development for oncology and other indications including inflammatory diseases.

SciBX 7(2); doi:10.1038/scibx.2014.52
Published online Jan. 16, 2014

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Chapuy, B. et al. Cancer Cell; published online Dec. 9, 2013;
Contact: James E. Bradner, Dana-Farber Cancer Institute, Boston, Mass.

Contact: Margaret A. Shipp, same affiliation as above