Vorinostat
A recent study suggested that vorinostat also possesses some activity against recurrent glioblastoma multiforme, resulting in a median overall survival of 5.7 months (compared to 4–4.4 months in earlier studies). Further brain tumor trials are planned in which vorinostat will be combined with other drugs.
Polycomb Group Proteins and Cancer
One study is investigating the safety and clinical activity of GSK2816126, a histone-lysine N-methyltransferase EZH2 inhibitor with potential antineoplastic activity in subjects with relapsed/refractory diffuse large B cell and transformed follicular lymphoma. Non-Hodgkin lymphoma (NHL) is the seventh most common malignancy. Diffuse large B cell lymphomas are the most common subtype of NHL, constituting about 30 to 40% of adult NHLs. This selective, competitive inhibitor molecule inhibits the activity of EZH2 and prevents the methylation of histone 3 lysine 27. This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased tumor cell proliferation in cancer cells that overexpress this enzyme. EZH2, included in the class of histone methyltransferases (HMTs), is overexpressed or mutated in a variety of cancers and plays a key role in tumor cell proliferation. In Phase I, this study has recruited participants for testing. The treatment regimen includes the administration of GSK2816126 twice weekly by intravenous infusion.