Thursday, May 8, 2014
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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
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).
Published online May 8, 2014
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.
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