Drug · Small Molecule

Tazemetostat

CI-DRUG-00000580Explore in graph →NCIt C107506 CHEMBL3414621 CIViC Approved

Regulatory

Approvals (4)

Each record names the authority, jurisdiction, indication text and status. A drug approved in one jurisdiction for one indication is not 'approved' in general.

openfdaRegulatory4 approval records · authority, jurisdiction and indication text as published.

Jurisdiction · authority	Cancer	Indication	Status	Approval date	Source
US FDA	Epithelioid Sarcoma	Adults and pediatric patients aged 16 years and older with metastatic or locally advanced epithelioid sarcoma not eligible for complete resection.	approved	Jan 23, 2020	openfda
US FDA	Follicular Lymphoma	Adult patients with relapsed or refractory follicular lymphoma whose tumors are positive for an EZH2 mutation as detected by an FDA-approved test and who have received at least 2 prior systemic therapies.	approved	Jan 23, 2020	openfda
US FDA	Follicular Lymphoma	Adult patients with relapsed or refractory follicular lymphoma who have no satisfactory alternative treatment options.	approved	Jan 23, 2020	openfda
US FDA	—	These indications are approved under accelerated approval based on overall response rate and duration of response. Continued approval for these indications may be contingent upon verification and description of clinical benefit in a confirmatory trial(s).

Data updated 16 days agoSource updated unknown

Derived

Development pipeline

Most advanced stage across all cancers, then per top-level cancer reached through trial conditions or approval indications. Approval in any ingested jurisdiction outranks trial phase; counts are interventional studies.

Scope	Stage	Max phase	Active	Recruiting	Phase 3	Trials	Approvals	Jurisdictions	First approval	First trial
All cancers	Approved	Phase 3	19	4	1	49	4	US	Jan 23, 2020	Jun 13, 2013
Non-Hodgkin Lymphoma	Approved	Phase 3	9	2	1	22	2	US	Jan 23, 2020	Jun 13, 2013
Malignant Central Nervous System Neoplasm	Phase2	Phase 2	2	0	0	4	0	—	—	Dec 22, 2015
Malignant Prostate Neoplasm	Phase2	Phase 2	2	1	0	4

Curated evidence

Clinical evidence (24)

CIViC items in which this therapy appears, grouped by cancer context, then molecular profile. 50 items per page.

civicCuratedShowing 1–24 of 24 evidence items · levels, directions and significance as curated at the source; each row links to its CIViC record.

Therapy	Cancer	Type	Level	Direction · significance	Rating (1–5)	Status	Evidence	Source
SMARCB1 Loss4
Tazemetostat	Atypical Teratoid/Rhabdoid Tumor

Clinical trials

Trials with this intervention (52)

Most recently updated first, 50 per page.

clinicaltrialsPublishedShowing 1–50 of 52 studies · status and phase as posted by the registrant; each row links to the study record.

NCT	Title	Status	Phase	Enrollment (n)	Sponsor	Countries	Last update	Source
NCT05627245	Testing the Safety of the Anti-cancer Drugs Tazemetostat and Belinostat in Patients With Lymphomas That Have Resisted Treatment	active not recruiting	Phase 1	48	National Cancer Institute (NCI)NIH	1	Sep 18, 2026	clinicaltrials
NCT06242834	Pembrolizumab and Tazemetostat to Overcome Immune Tolerance Following ASCT or CAR T-cell Therapy in Patients With Aggressive B-Cell Non-Hodgkin's Lymphoma

Molecule

Record

Kind: Small Molecule
Mechanism: Histone-lysine N-methyltransferase EZH2 inhibitor
Targets: 1 gene
UNII: 6P89T5M073
Aliases: CT-EPZ438EPZ-6438EPZ6438A-1623E-7438E7438, E 7438, E-7438, E7438, EPZ 6438, EPZ-6438, EPZ6438, 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, 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, Tazemetostat, TAZEMETOSTAT (EPZ-6438), TAZVERIK

Data updated 21 hours agoSource updated unknown

Identifiers

Codes (0)

Upstream identifiers kept as first-class codes; each links to its registry where a stable public URL exists.

Data not yet available

No cross-reference code recorded yet beyond the record identifiers above.

Regulatory status is jurisdiction-specific and time-bound. Nothing on this page is a treatment recommendation.

EZH2 Y646F3
Tazemetostat	B-Cell Malignant NeoplasmCURATED_BROADER	Predictive	D	Supports Sensitivity Response	4	submitted	EID10999 In this preclinical study, EZH2 inhibitor, EPZ-6438, was tested for its antitumoral efficacy and potency using WSU-DLCL2 lymphoma cell line and mice harboring Y646F mutation. In-vitro cell treatment s… (full text at CIViC) PMID 24563539 · Knutson et al., 2014 · Open in CIViC	civic
〃	Non-Hodgkin Lymphoma	Predictive	D	Supports Sensitivity Response	4	submitted	EID11000 In this preclinical study, authors aimed to study the effect of combining glucocorticoid receptor agonists with the EZP-6438 inhibitor in NHL. WSU-DLCL2 lymphoma cells harboring the Y646F mutation we… (full text at CIViC) PMID 25493630 · Knutson et al., 2014 · Open in CIViC	civic
〃	Non-Hodgkin Lymphoma	Predictive	D	Supports Sensitivity Response	3	submitted	EID11048 To study EZH2 blocking outcome on TADs, authors used EPZ6438 in NHL cell line, OCI-Ly19-EZH2 carrying the Y646F mutation. EZH2 inhibition efficiently depleted H3K27me3 in lymphoma cells and exhibited … (full text at CIViC) PMID 30692681 · Donaldson-Collier et al., 2019 · Open in CIViC	civic

EZH2 Y646F3

Tazemetostat

B-Cell Malignant NeoplasmCURATED_BROADER

Predictive

Supports Sensitivity Response

submitted

EID10999

In this preclinical study, EZH2 inhibitor, EPZ-6438, was tested for its antitumoral efficacy and potency using WSU-DLCL2 lymphoma cell line and mice harboring Y646F mutation. In-vitro cell treatment s… (full text at CIViC)

PMID 24563539 · Knutson et al., 2014 · Open in CIViC

EZH2 A682G + EZH2 A692V + EZH2 Y646C + EZH2 Y646F + EZH2 Y646H + EZH2 Y646N + EZH2 Y646S3
Tazemetostat	B-Cell Non-Hodgkin Lymphoma	Predictive	A	Supports Sensitivity Response	2	accepted	EID11220 In a multicentre, open-label, phase 1 trial, tazemetostat was evaluated in 64 adult patients (≥18 years) with relapsed or refractory B-cell non-Hodgkin lymphoma (n=21) or advanced solid tumours (n=43)… (full text at CIViC) PMID 29650362 · Italiano et al., 2018 · Open in CIViC	civic
〃	Diffuse Large B-Cell LymphomaCURATED_BROADER	Predictive	B	Supports Sensitivity Response	3	accepted	EID11110 This phase II study evaluated the efficacy and safety of the EZH2 inhibitor tazemetostat in Japanese adults with relapsed or refractory B-cell non-Hodgkin lymphoma harboring EZH2-activating mutations … (full text at CIViC) PMID 34159682 · Izutsu et al., 2021 · Open in CIViC	civic
〃	Follicular Lymphoma	Predictive	B	Supports Sensitivity Response	4	accepted	EID11109 In this study, Koji Izutsu et al. conducted a multicenter, open-label phase II clinical trial to evaluate the efficacy and safety of the EZH2 inhibitor tazemetostat in Japanese patients with relapsed … (full text at CIViC) PMID 34159682 · Izutsu et al., 2021 · Open in CIViC	civic

SMARCB1 Underexpression2
Tazemetostat	Malignant NeoplasmALIAS	Predictive	C	Supports Sensitivity Response	3	rejected	EID6374 Tazemetostat showed a favourable safety profile and antitumour activity in patients with refractory B-cell non-Hodgkin lymphoma and advanced solid tumours, including epithelioid sarcoma. One SMARCA4 n… (full text at CIViC) PMID 29650362 · Italiano et al., 2018 · Open in CIViC	civic
〃	Synovial Sarcoma	Predictive	D	Supports Sensitivity Response	2	accepted	EID1739 Treatment with tazemetostat , a small-molecule inhibitor of EZH2, results in concentration-dependent cell growth inhibition and cell death specifically in SS18-SSX-positive, SMARCB1-deficient synovial… (full text at CIViC) PMID 27391784 · Kawano et al., 2016 · Open in CIViC	civic