tazemetostat

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Associated Genetic Biomarkers

Associated Diseases

Overview

Generic Name(s):

tazemetostat

Trade Name(s):

Tazverik

NCI Definition [1]:

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.

Biomarker-Directed Therapies

Tazemetostat can be used in the treatment of follicular lymphoma. EZH2, EZH2 A682G, and EZH2 A692V are the most frequent biomarker inclusion criteria for use of tazemetostat [2].

Follicular Lymphoma +

Disease is predicted to be sensitive to tazemetostat: -

Biomarker Criteria:

Sample must match one or more of the following:

EZH2 A682G, EZH2 A692V, EZH2 Y646C, EZH2 Y646F, EZH2 Y646H, EZH2 Y646N, EZH2 Y646S

Clinical Setting(s): Refractory (FDA), Relapse (FDA)

Note: Indicated for adult patients with relapsed or refractory follicular lymphoma whose tumors are positive for an EZH2 mutation and who have received at least 2 prior systemic therapies.

Biomarker Criteria: Sample must match one or more of the following: EZH2 A682G, EZH2 A692V, EZH2 Y646C, EZH2 Y646F, EZH2 Y646H, EZH2 Y646N, EZH2 Y646S	Clinical Setting(s): Refractory (FDA), Relapse (FDA)
	Note: Indicated for adult patients with relapsed or refractory follicular lymphoma whose tumors are positive for an EZH2 mutation and who have received at least 2 prior systemic therapies.

Clinical Trials

View Clinical Trials for tazemetostat

Tazemetostat has been investigated in 21 clinical trials, of which 17 are open and 4 are closed. Of the trials investigating tazemetostat, 5 are phase 1 (4 open), 5 are phase 1/phase 2 (5 open), 9 are phase 2 (6 open), and 2 are phase 3 (2 open).

EZH2 Loss, EZH2 Mutation, and SMARCB1 Loss are the most frequent biomarker inclusion criteria for tazemetostat clinical trials.

Malignant solid tumor, follicular lymphoma, and non-hodgkin lymphoma are the most common diseases being investigated in tazemetostat clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Tazemetostat

Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Tazemetostat

This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating tazemetostat and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:

epz-6438, e7438, tazemetostat, n-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2h-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide, cas 1403254-99-8, histone methyl transferase ezh2 inhibitor e7438, epz6438, Tazverik, n-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(oxan-4-yl)amino)-4-methyl-4'-((morpholin-4-yl)methyl)(1,1'-biphenyl)-3-carboxamide

Drug Categories [2]:

Histone methyltransferase inhibitors

Drug Target(s) [2]:

EZH2

NCIT ID [1]:

C107506

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.

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