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Brain cancer

Bromodomain containing 4 (BRD4); v-myc myelocytomatosis viral related oncogene neuroblastoma derived (MYCN; NMYC)

Cell profiling and mouse studies suggest inhibiting BET bromodomains could help treat neuroblastomas with MYCN amplification. In a screen of 673 genetically characterized cancer cell lines, MYCN amplification was the most strongly correlated marker for sensitivity to JQ1, a small molecule inhibitor of BRD4 and other BET bromodomains. In three different mouse models for MYCN-amplified neuroblastoma, JQ1 increased survival compared with vehicle. Next steps include looking at the effects of inhibiting BET bromodomains in MYCN-amplified medulloblastoma.
Tensha Therapeutics Inc. has the BET bromodomain inhibitor TEN-010 in preclinical development for cancer.
At least three other companies have BET bromodomain inhibitors in Phase I or preclinical development in cancer (see Bromodomains on the brain, page 1).

SciBX 6(12); doi:10.1038/scibx.2013.282
Published online March 28, 2013

Patent application filed covering JQ1 and derivatives; licensed to Tensha Therapeutics

Puissant, A. et al. Cancer Discov.; published online Feb. 21, 2013;
Contact: Kimberly Stegmaier, Dana-Farber Cancer Institute, Boston, Mass.
Contact: James E. Bradner, same affiliation as above