Therapy Detail

Therapy Name Tazemetostat
Therapy Description

Tazemetostat (EPZ-6438) binds to and inhibits EZH2, resulting in decreased tri-methylation of H3K27, and potentially leading to inhibition of cell proliferation and tumor growth (PMID: 23620515).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Tazemetostat EPZ6438|E-7438|EPZ-6438 EZH2 inhibitor 16 Tazemetostat (EPZ-6438) binds to and inhibits EZH2, resulting in decreased tri-methylation of H3K27, and potentially leading to inhibition of cell proliferation and tumor growth (PMID: 23620515).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
EZH2 Y111D Advanced Solid Tumor resistant Tazemetostat Preclinical - Cell culture Actionable In a preclinical study, over expression of EZH2 Y111D in transformed cells harboring wild-type Ezh2 resulted in resistance to Tazemetostat (EPZ-6438) treatment in culture (PMID: 26360609). 26360609
SMARCB1 negative atypical teratoid rhabdoid tumor predicted - sensitive Tazemetostat Phase I Actionable In a Phase I trial, Tazemetostat (EPZ-6438) was well-tolerated and demonstrated anti-tumor activity in pediatric patients with SMARCB1 (INI)-deficient tumors, including complete or partial responses in patients with epithelioid sarcoma (n=1), chordoma (n=2), and atypical teratoid rhaboid tumor (n=1) (AACR-NCI-EORTC Int Conference on Molecular Targets and Cancer Therapeutics 2017, A175; NCT02601937). detail...
EZH2 Y646H non-Hodgkin lymphoma sensitive Tazemetostat Phase I Actionable In a Phase I trial, Tazemetostat (EPZ-6438) treatment resulted in partial response for more than 16 weeks in a non-Hodgkin lymphoma patient harboring a EZH2 Y646H mutation (ASH 57th Annual Meeting and Exposition, Dec 2015, Abstract #473; NCT01897571). detail...
EZH2 positive follicular lymphoma predicted - sensitive Tazemetostat Phase I Actionable In a Phase I trial, Tazemetostat (EPZ-6438) treatment in non-Hodgkin lymphoma (NHL) patients carrying wild-type EZH2 or an EZH2 Y646H mutation resulted in an objective response rate of 60% (3/5) among patients with follicular lymphoma (ASH 57th Annual Meeting and Exposition, Dec 2015, Abstract #473; NCT01897571). detail...
EZH2 positive non-Hodgkin lymphoma predicted - sensitive Tazemetostat Phase I Actionable In a Phase I trial, Tazemetostat (EPZ-6438) treatment resulted in a total response rate of 60% (9/15) in non-Hodgkin lymphoma patients harboring wild-type EZH2 (n=13/14 tested) or an EZH2 Y646H mutation (n=1/14 tested) (ASH 57th Annual Meeting and Exposition, Dec 2015, Abstract #473; NCT01897571). detail...
EZH2 Y111D SMARCB1 inact mut rhabdoid cancer resistant Tazemetostat Preclinical - Cell culture Actionable In a preclinical study, over expression of EZH2 Y111D in rhabdoid tumor cells harboring an SMARCB1 inactivating mutation resulted in resistance to Tazemetostat (EPZ-6438) treatment in culture (PMID: 26360609). 26360609
Unknown unknown marginal zone B-cell lymphoma not applicable Tazemetostat Phase I Actionable In a Phase I trial, Tazemetostat (EPZ-6438) treatment resulted in a clinical response in a patient with marginal zone B-cell lymphoma (ASH 57th Annual Meeting and Exposition, Dec 2015, Abstract #473; NCT01897571). detail...
KDM6A loss bladder urothelial carcinoma sensitive Tazemetostat Preclinical - Cell culture Actionable In a preclinical study, KDM6A-null urothelial bladder carcinoma cell lines demonstrated sensitivity to Tazemetostat (EPZ-6438), resulting in decreased proliferation in culture (PMID: 28228601). 28228601
EZH2 T678_R679delinsKK acute myeloid leukemia resistant Tazemetostat Preclinical - Cell culture Actionable In a preclinical study, a murine acute myeloid leukemia cell line expressing EZH2 T678_R679delinsKK were resistant to Tazemetostat (EPZ-6438) in culture (PMID: 28231254). 28231254
EZH2 A677G EZH2 Y111D B-cell lymphoma resistant Tazemetostat Preclinical - Cell culture Actionable In a preclinical study, EZH2 Y111D conferred resistance to Tazemetostat (EPZ-6438) when occurring in the same allele as EZH2 A677G in B-cell lymphoma cells in culture (PMID: 26360609). 26360609
SMARCB1 loss rhabdoid cancer sensitive Tazemetostat Preclinical - Cell line xenograft Actionable In a preclinical study, Tazemetostat (EPZ-6438) inhibited growth of SMARCB1-deficient malignant rhabdoid tumor cell lines in culture, and inhibited H3K27 trimethylation and induced tumor regression in a SMARCB1-deleted human malignant rhabdoid tumor cell line xenograft model (PMID: 23620515). 23620515
EZH2 positive diffuse large B-cell lymphoma predicted - sensitive Tazemetostat Phase I Actionable In a Phase I trial, Tazemetostat (EPZ-6438) treatment in non-Hodgkin lymphoma (NHL) patients carrying wild-type EZH2 or an EZH2 Y646H mutation resulted in an objective response rate of 56% (5/9) among patients with diffuse large B-cell lymphoma (ASH 57th Annual Meeting and Exposition, Dec 2015, Abstract #473; NCT01897571). detail...
EZH2 Y646F lymphoma sensitive Tazemetostat Preclinical Actionable In a preclinical study, treatment with EPZ-6438 inhibited proliferation and promoted cell death in lymphoma cells expressing EZH2 Y646F (PMID: 24563539). 24563539
EZH2 F120L EZH2 Y111N Advanced Solid Tumor resistant Tazemetostat Preclinical - Cell culture Actionable In a preclinical study, a cancer cell line co-expressing EZH2 F120L and EZH2 Y111N was resistant to Tazemetostat (EPZ-6438) in culture, demonstrating no inhibition of cell proliferation (PMID: 28135235). 28135235
EZH2 Y111D EZH2 Y641F Advanced Solid Tumor decreased response Tazemetostat Preclinical - Cell culture Actionable In a preclinical study, transformed cells over expressing EZH2 carrying simultaneous Y641F and Y111D mutations demonstrated reduced sensitivity to Tazemetostat (EPZ-6438) in culture (PMID: 26360609). 26360609
EZH2 A677G EZH2 Y111D Advanced Solid Tumor resistant Tazemetostat Preclinical - Cell culture Actionable In a preclinical study, transformed cells overexpressing EZH2 and carrying simultaneous A677G and Y111D mutations were resistant to Tazemetostat (EPZ-6438) in culture (PMID: 26360609). 26360609
SMARCB1 negative epithelioid sarcoma predicted - sensitive Tazemetostat Phase I Actionable In a Phase I trial, Tazemetostat (EPZ-6438) was well-tolerated and demonstrated anti-tumor activity in pediatric patients with SMARCB1 (INI)-deficient tumors, including complete or partial responses in patients with epithelioid sarcoma (n=1), chordoma (n=2), and atypical teratoid rhaboid tumor (n=1) (AACR-NCI-EORTC Int Conference on Molecular Targets and Cancer Therapeutics 2017, A175; NCT02601937). detail...
SMARCB1 negative chordoma predicted - sensitive Tazemetostat Phase I Actionable In a Phase I trial, Tazemetostat (EPZ-6438) was well-tolerated and demonstrated anti-tumor activity in pediatric patients with SMARCB1 (INI)-deficient tumors, including complete or partial responses in patients with epithelioid sarcoma (n=1), chordoma (n=2), and atypical teratoid rhaboid tumor (n=1) (AACR-NCI-EORTC Int Conference on Molecular Targets and Cancer Therapeutics 2017, A175; NCT02601937). detail...
Clinical Trial Phase Therapies Title Recruitment Status
NCT02860286 Phase II Tazemetostat Study of the EZH2 Inhibitor Tazemetostat in Malignant Mesothelioma Active, not recruiting
NCT02601937 Phase I Tazemetostat A Phase 1 Study of the EZH2 Inhibitor Tazemetostat in Pediatric Subjects With Relapsed or Refractory INI1-Negative Tumors or Synovial Sarcoma Recruiting
NCT03348631 Phase II Tazemetostat Tazemetostat in Treating Patients With Recurrent Ovarian, Primary Peritoneal, or Endometrial Cancer Not yet recruiting
NCT03213665 Phase II Tazemetostat Pediatric MATCH: Tazemetostat in Treating Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphoma, or Histiocytic Disorders With EZH2, SMARCB1, or SMARCA4 Gene Mutations Suspended
NCT03217253 Phase I Tazemetostat Tazemetostat in Treating Patients With Metastatic or Unresectable Solid Tumors or B-Cell Lymphomas With Liver Dysfunction Recruiting
NCT02875548 Phase II Tazemetostat Tazemetostat Rollover Study (TRuST): An Open-Label Rollover Study Recruiting
NCT03155620 Phase II Tazemetostat Larotrectinib LY3023414 Vemurafenib Olaparib Selumetinib Ensartinib Pediatric MATCH: Targeted Therapy Directed by Genetic Testing in Treating Pediatric Patients With Advanced Refractory Solid Tumors or Lymphomas Recruiting
NCT02601950 Phase II Tazemetostat A Phase II, Multicenter Study of the EZH2 Inhibitor Tazemetostat in Adult Subjects With INI1-Negative Tumors or Relapsed/Refractory Synovial Sarcoma Recruiting