Thursday, November 8, 2012
Publication and contact
Bromodomain containing 4 (BRD4);
In vitro and rodent studies identified BRD4 inhibitors that
could help treat inflammation. Fragment-based screening, chemical synthesis
and in vitro testing of sulfonamide analogs of quinazolinone
identified a lead compound as a nanomolar inhibitor of BRD4. In a human
monocyte-based inflammation assay, the lead compound blocked lipopolysaccharide
IL-6 production with a low micromolar EC50 value. In normal mice
and rats, the lead compound showed oral bioavailability and good
pharmacokinetics. Future studies could include testing the compound in animal
models of inflammation.
an inhibitor of the bromodomain and extra terminal domain
family of bromodomain-containing proteins including BRD4, is in Phase II
testing to treat diabetes and atherosclerosis and Phase I testing to treat
Alzheimer's disease (AD).
Mitsubishi Tanabe Pharma Corp.
S.A. have OTX015,
a synthetic small molecule inhibitor of BET BRD2,
and BRD4, in Phase I testing to treat cancer.
Published online Nov. 8, 2012
Patent and licensing status
Fish, P. et al. J. Med.
published online Oct. 25, 2012;
Contact: Dafydd R. Owen,
Pfizer Worldwide R&D, Cambridge, Mass.
All contents Copyright © 1993-2015 BioCentury Publications, Inc. ALL RIGHTS RESERVED. All use of this Web Site and its contents is governed by the BioCentury User Agreement
. The contents of this Web Site are protected under U.S. and foreign copyright and intellectual property laws, and no part of this Web Site or its contents may be photocopied, reproduced or retransmitted in any form without the written consent of BioCentury, which may be requested from Reprints/Permissions
. BioCentury®; The Bernstein Report on BioBusiness™; The BioCentury 100™; The Clear Route to ROI™; Because Real Intelligence is Hard to Find™; BCIQ™; and BioPharma's Knowledge Center™; are trademarks of BioCentury Publications, Inc., P.O. Box 1246, San Carlos, CA 94070. SciBX® and SciBX: Science-Business eXchange® are trademarks of Nature America, Inc. that are jointly used by BioCentury Publications, Inc. and Nature America, Inc.
Thanks for purchasing this article.
Please bookmark this url for future reference.
We have also sent you a confirming e-mail with a receipt and this same url for your
close [ X ]