Table 1.

Summary of EZH2 inhibitors that have been tested for anti-myeloma activity.

EZH2 Inhibitor	Anti-MM Activity	Treatment Type	Reference
UNC1999	In vitro and in vivo	Single agent treatment or in combination with Bortezomib	[102,112,113]
GSK343	In vitro	Single agent treatment	[58,102,107]
GSK126	In vitro and in vivo	Single agent treatment or in combination with Bortezomib and Panobinostat	[107,114,115]
EPZ-7438	In vitro and in vivo	Single agent treatment or in combination with Lenalidomide, Pomalidomide, Bortezomib and Panobinostat	[115–117]
EPZ005687	In vitro	Single agent treatment	[88]
OR-S1 and OR-S2	In vitro	Single agent treatment	[118]
GSK2816126	Phase I clinical trial (NCT02082977)–Terminated	Single agent treatment	[119]