Preferred Label : Tazemetostat Hydrobromide;
NCIt synonyms : EPZ-6438 Monohydrobromide; Tazemetostat Monohydrobromide; (1,1'-Biphenyl)-3-carboxamide, N-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(4-morpholinylmethyl)-,
hydrobromide (1:1);
NCIt definition : The hydrobromide salt form of tazemetostat, 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.;
UNII : 6P89T5M073;
InChIKey : UQRICAQPWZSJNF-UHFFFAOYSA-N;
CAS number : 1467052-75-0;
Drug name : TAZVERIK;
NCI Metathesaurus CUI : CL972202;
Origin ID : C166954;
UMLS CUI : C5233973;
Automatic exact mappings (from CISMeF team)
- Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_free_acid_or_base_form
- has_target
- is_component_of_chemotherapy_regimen
- is_salt_form_of
