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Tazemetostat Hydrobromide
CAS NO.: 1467052-75-0
Chemical Formula: C34H45BrN4O4
Molecular Weight: 653.6000
DMF&GMP status: Please contact us for more details.
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.

Tazemetostat is a methyltransferase inhibitor used to treat metastatic or locally advanced epithelioid sarcoma not eligible for complete resection. Tazemetostat was first named in literature as EPZ-6438. Tazemetaostat was granted FDA approval on 23 January 2020.

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Active Ingredient Dosage Form; Route Strength Proprietary Name Applicant
Patent Data
Patent No. Patent Expiration Drug Substance Claim Drug Product Claim Patent Use Code
Exclusive Data
Exclusivity Code Exclusivity Expiration
I-835 06/18/2023
I-836 06/18/2023
NCE 01/23/2025
ODE-299 01/23/2027
ODE-314 06/18/2027