Thursday, October 18, 2012
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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,
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