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Prostate cancer

Androgen receptor; bromodomain containing 4 (BRD4)

Mouse and cell culture studies suggest BRD4 inhibitors could be more effective than androgen receptor antagonists at treating castration-resistant prostate cancer (CRPC). In a human CRPC cell line, the BRD4 inhibitor JQ1 caused more potent suppression of androgen receptor-mediated gene transcription than the androgen receptor antagonist Xtandi enzalutamide. In a mouse xenograft model of human CRPC, JQ1 caused more potent tumor growth inhibition than Xtandi or vehicle. Next steps include developing a strategy to identify patients that would respond to BET bromodomain inhibitors in prostate and other cancers.
Medivation Inc. and Astellas Pharma Inc. market Xtandi to treat prostate cancer.
The corresponding author is a cofounder of OncoFusion Therapeutics Inc., which is collaborating with Medivation to evaluate OncoFusion's preclinical BET bromodomain inhibitors in undisclosed cancers and other indications.
At least four other companies have BET bromodomain inhibitors in Phase I testing to treat various cancers.
JQ1 is a research reagent (see BETting on OncoFusion, page 1).

SciBX 7(18); doi:10.1038/scibx.2014.525
Published online May 8, 2014

Composition-of-matter patents filed; licensed to Medivation

Asangani, I.A. et al. Nature; published online April 23, 2014;
Contact: Arul M. Chinnaiyan, University of Michigan Medical School, Ann Arbor, Mich.