Thursday, October 18, 2012
Publication and contact
Enhancer of zeste homolog 2 (EZH2)
Mouse and in vitro
studies suggest inhibiting EZH2 could help treat NHL characterized by EZH2-activating
mutations. In vitro, EPZ005687 from Epizyme
Inc. and GSK126 from GlaxoSmithKline
plc inhibited wild-type and mutant EZH2 with low
nanomolar Ki values. In most NHL cell lines bearing EZH2-activating
mutations, EPZ005687 and/or GSK126 decreased cell proliferation compared with
vehicle. In a mouse xenograft model of EZH2 mutant NHL, GSK126 led to
tumor regression and increased survival compared with vehicle. Next steps
include additional preclinical studies to prepare for Phase I clinical
GlaxoSmithKline has a preclinical program targeting EZH2 in cancer.
Epizyme and partner Eisai
Co. Ltd. have a preclinical program targeting EZH2 in NHL
and breast cancer.
Pharmaceuticals Inc. has a preclinical program targeting
EZH2 in cancer (see EZH2 moves, page 4).
Published online Oct. 18, 2012
Findings in first study
covered by patents and patent applications; partnered with Eisai
Patent and licensing status undisclosed for findings in second study
Knutson, S.K. et al.
Nat. Chem. Biol.; published online Sept. 30, 2012;
Contact: Kevin W. Kuntz, Epizyme Inc., Cambridge, Mass.
McCabe, M.T. et al. Nature; published online Oct. 10, 2012;
Contact: Caretha L. Creasy, GlaxoSmithKline plc,
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 ]