This week in therapeutics

Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Diffuse large B cell lymphoma (DLBCL)

Enhancer of zeste homolog 2 (EZH2)

In vitro studies identified an EZH2 inhibitor that could help treat DLBCL. In vitro, the lead compound EI1 inhibited EZH2 with an IC50 value of about 10 nM and about 90-fold specificity for EZH2 over the related enzyme EZH1. In DLBCL cell lines carrying mutant EZH2, EI1 inhibited cell growth at low micromolar concentrations. Next steps could include additional preclinical studies of EI1 in mouse models of cancer.

SciBX 6(1); doi:10.1038/scibx.2013.7
Published online Jan. 10, 2013

Patent and licensing status undisclosed

Qi, W. et al. Proc. Natl. Acad. Sci. USA; published online Dec. 10, 2012;
doi:10.1073/pnas.1210371110
Contact: En Li, Novartis Institutes for BioMedical Research, Shanghai, China
e-mail:
en.li@novartis.com