This week in therapeutics




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Enhancer of zeste homolog 2 (EZH2); embryonic ectoderm development (EED)

In vitro studies suggest inhibiting EZH2-EED interactions could help treat cancer. Chemical synthesis and in vitro testing of stapled peptide analogs of the EED-binding domain of EZH2 identified a lead peptide with nanomolar binding affinity for EED. In a murine leukemia cell line and human breast and prostate cancer cell lines, the peptide inhibited EZH2-EED interactions and decreased proliferation compared with a control peptide. In human lymphoma cell lines harboring EZH2 mutations, the peptide and a small molecule inhibitor of the EZH2 catalytic site decreased proliferation compared with either agent alone. Ongoing work includes optimizing the lead peptide and testing it in a range of cancers.
Epizyme Inc. and Eisai Co. Ltd. have EPZ6438 (E7438), a selective inhibitor of EZH2, in Phase I/II testing to treat lymphoma and non-Hodgkin's lymphoma (NHL).
Constellation Pharmaceuticals Inc., Novartis AG and GlaxoSmithKline plc have EZH2 inhibitors in preclinical development to treat cancer.

SciBX 6(37); doi:10.1038/scibx.2013.1023
Published online Sept. 26, 2013

Patented by the Dana-Farber Cancer Institute; available for licensing or partnering

Kim, W. et al. Nat. Chem. Biol.; published online Aug. 25, 2013;
Contact: Stuart H. Orkin, Boston Children's Hospital, Boston, Mass.
Contact: Loren Walensky,
same affiliation as above