This week in therapeutics




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Enhancer of zeste homolog 2 (EZH2)

Cell culture studies identified a small molecule inhibitor of EZH2 that could help treat EZH2-dependent cancers. Chemical screening and lead optimization identified a competitive small molecule inhibitor that selectively decreased trimethylation of histone H3K27 by wild-type or mutant EZH2. In Pfeiffer lymphoma cells carrying mutant EZH2, the lead compound dose-dependently inhibited growth and H3K27 trimethylation. Next steps include further optimizing lead compounds and testing them in lymphoma models.
Epizyme Inc. has the selective EZH2 inhibitor E7438 in Phase I/II testing to treat lymphomas.
Constellation Pharmaceuticals Inc. has EZH2 inhibitors in discovery to treat cancer.
GlaxoSmithKline plc and Novartis AG also have EZH2 discovery programs.

SciBX 6(47); doi:10.1038/scibx.2013.1341
Published online Dec. 12, 2013

Patent and licensing status undisclosed

Garapaty-Rao, S. et al. Chem. Biol.; published online Oct. 31, 2013;
Contact: Patrick Trojer, Constellation Pharmaceuticals Inc., Cambridge, Mass.