Table 1. Clinical bromodomains. At least six companies have compounds that inhibit bromodomains, including the bromodomain containing 2 (BRD2), BRD3 and BRD4 members of the BET bromodomain family, in clinical testing to treat cancer and other diseases.

Source: BCIQ: BioCentury Online Intelligence





Zenith Epigenetics Corp. subsidiary of Resverlogix Corp. (TSX:RVX)


Inhibitor of BRD4 and other members of the BET bromodomain family

Phase II for atherosclerosis and diabetes; Phase I for Alzheimer's disease (AD)

Constellation Pharmaceuticals Inc.


Bromodomain inhibitor

Phase I for lymphoma

GlaxoSmithKline plc (LSE:GSK; NYSE:GSK)

GSK525762 (525762)

Bromodomain inhibitor

Phase I for NUT midline carcinoma (NMC)

Mitsubishi Tanabe Pharma Corp. (Tokyo:4508); Oncoethix S.A.

OTX015 (Y-803)

Synthetic small molecule inhibitor of BRD2, BRD3 and BRD4

Phase I for hematological malignancies

Tensha Therapeutics Inc.


Small molecule inhibitor selective for the BET bromodomain family (BRD2, BRD3, BRD4 and bromodomain testis specific (BRDT))

Phase I for solid tumors