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Enhancer of zeste homolog 2 (EZH2); SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily b member 1 (SMARCB1; SNF5)

Cell culture and mouse studies identified an EZH2 inhibitor that could help treat SMARCB1 mutant malignant rhabdoid tumors (MRTs). In SMARCB1 mutant MRT cells, the EZH2 inhibitor EPZ-6438 blocked proliferation with nanomolar IC50 values. In mouse xenograft models for SMARCB1 mutant MRT, oral EPZ-6438 for 21 days caused tumor regression without regrowth
32 days after inhibitor cessation. Next steps could include testing the EZH2 inhibitor in additional models for cancer.
Epizyme Inc. and Eisai Co. Ltd. have EPZ-6438 in preclinical testing to treat lymphoma.

SciBX 6(19); doi:10.1038/scibx.2013.463
Published online May 16, 2013

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Knutson, S.K. et al. Proc. Natl. Acad. Sci. USA; published online April 25, 2013;
Contact: Heike Keilhack,
Epizyme Inc., Cambridge, Mass.