According to the NCI website, tazemetostat hydrobromide is 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. Check for active clinical trials using this agent. (NCI Thesaurus)
Indikationen/Anwendungsmöglichkeiten gemäss FDA:
- Epithelioid sarcoma that is locally advanced or has metastasized (spread to other parts of the body). It is used in adults and in children aged 16 years or older whose disease cannot be removed by surgery.
This use is approved under FDA’s Accelerated Approval Program. As a condition of approval, confirmatory trial(s) must show that tazemetostat hydrobromide provides a clinical benefit in these patients.
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