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Publication and contact information


Non-Hodgkin's lymphoma (NHL)

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 trials.
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.
Constellation Pharmaceuticals Inc. has a preclinical program targeting EZH2 in cancer (see EZH2 moves, page 4).

SciBX 5(41); doi:10.1038/scibx.2012.1080
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, Collegeville, Pa.