Tazemetostat

Tazemetostat (EPZ-6438) is an experimental cancer drug that acts as a potent selective EZH2 inhibitor.

Tazemetostat

Clinical data
Other names	EPZ-6438
Legal status
Legal status	Investigational
Identifiers
IUPAC name N-[(4,6-Dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide
CAS Number	1403254-99-8
PubChem CID	66558664
UNII	Q40W93WPE1
KEGG	D11444
Chemical and physical data
Formula	C34H44N4O4
Molar mass	572.750 g·mol−1
3D model (JSmol)	Interactive image
SMILES CCN(C1CCOCC1)C2=CC(=CC(=C2C)C(=O)NCC3=C(C=C(NC3=O)C)C)C4=CC=C(C=C4)CN5CCOCC5

According to the NCI Drug Dictionary, "tazemetostat is an orally available, small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone methyl transferase EZH2, with potential antineoplastic activity. Upon oral administration, tazemetostat selectively inhibits the activity of both wild-type and mutated forms of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 lysine 27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased tumor cell proliferation in EZH2 mutated cancer cells. EZH2, which belongs to the class of histone methyltransferases (HMTs), is overexpressed or mutated in a variety of cancer cells and plays a key role in tumor cell proliferation."[1]