MMSET/NSD2 Inhibitors

MMSET (NSD2 or WHSC1), like EZH2, is a histone methyltransferase. MMSET is found as a recurrent gene fusion with IgH in 20% of multiple myelomas (translocation t(4;14)). MMSET has also been shown to form a complex with BRD4 (see Bromodomain inhibitor program) 

Studies by the founders, under revision in the journal Molecular Cell, suggest that EZH2 functions as an upstream activator of MMSET and that EZH2 and MMSET levels are tightly correlated in most human tumors.


OncoFusion has identified a class of promising lead compounds that achieve on target in vitro and in vivo antitumor activity. The lead compound is closely related to an FDA approved drug and is in advanced pre-clinical testing and optimization.

For partnership opportunities, please contact us.