Therapy Detail

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Therapy Name Tazemetostat
Synonyms
Therapy Description

Tazverik (tazemetostat) 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). Tazverik (tazemetostat) is FDA approved for use in patients aged 16 years and older with metastatic or locally advanced epithelioid sarcoma not eligible for complete resection, and in adult patients with relapsed or refractory follicular lymphoma (R/R FL) harboring an EZH2 mutation after 2 prior therapies, and in patients with R/R FL without treatment options (FDA.gov).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Tazemetostat Tazverik EPZ6438|E-7438|EPZ-6438 EZH2 inhibitor 19 Tazverik (tazemetostat) 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). Tazverik (tazemetostat) is FDA approved for use in patients aged 16 years and older with metastatic or locally advanced epithelioid sarcoma not eligible for complete resection, and in adult patients with relapsed or refractory follicular lymphoma (R/R FL) harboring an EZH2 mutation after 2 prior therapies, and in patients with R/R FL without treatment options (FDA.gov).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
ARID1A inact mut urinary bladder cancer sensitive Tazemetostat Preclinical - Cell culture Actionable In a preclinical study, Tazverik (tazemetostat) inhibited viability of bladder cancer cell lines harboring ARID1A inactivating mutations in culture (PMID: 35852858). 35852858
ATRX fusion neuroblastoma predicted - sensitive Tazemetostat Preclinical - Cell culture Actionable In a preclinical study, treatment with Tazemetostat (EPZ-6438) resulted in reduced proliferation and increased apoptosis of neuroblastoma cell lines harboring in-frame ATRX fusions in culture (PMID: 31631027). 31631027
ARID1A dec exp urinary bladder cancer sensitive Tazemetostat Preclinical - Cell culture Actionable In a preclinical study, Tazverik (tazemetostat) inhibited viability of bladder cancer cell lines with ARID1A knockdown in culture (PMID: 35852858). 35852858

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT04557956 Phase Ib/II Tazemetostat Dabrafenib + Tazemetostat + Trametinib Testing the Addition of the Anti-cancer Drug, Tazemetostat, to the Usual Treatment (Dabrafenib and Trametinib) for Metastatic Melanoma That Has Progressed on the Usual Treatment Recruiting USA 0
NCT03155620 Phase II Tazemetostat Larotrectinib LY3023414 Vemurafenib Palbociclib Olaparib Ulixertinib Erdafitinib Selumetinib Ensartinib Targeted Therapy Directed by Genetic Testing in Treating Pediatric Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphomas, or Histiocytic Disorders (The Pediatric MATCH Screening Trial) Recruiting USA 1
NCT05567679 Phase I Tazemetostat A Study of Tazemetostat (Tazverik) Before Prostatectomy in Men With Prostate Cancer Not yet recruiting USA 0
NCT04917042 Phase II Tazemetostat Tazemetostat in Malignant Peripheral Nerve Sheath Tumors Recruiting USA 0
NCT05467748 Phase Ib/II Tazemetostat EZH2 Inhibitor, Tazemetostat, and PD-1 Blockade for Treatment of Advanced Non-small Cell Lung Cancer Not yet recruiting USA 0
NCT02875548 Phase II Tazemetostat Tazemetostat Rollover Study (TRuST): An Open-Label Rollover Study Active, not recruiting USA | FRA | BEL 4
NCT03217253 Phase I Tazemetostat Tazemetostat in Treating Patients With Metastatic or Unresectable Solid Tumors or B-Cell Lymphomas With Liver Dysfunction Withdrawn USA 0
NCT04241835 Phase I Tazemetostat A Study of Oral Tazemetostat in Subjects With Moderate and Severe Hepatic Impairment With Advanced Malignancies Recruiting USA | FRA | BEL 2
NCT05023655 Phase II Tazemetostat Phase II Study of Tazemetostat in Solid Tumors Harboring an ARID1A Mutation Recruiting USA 0
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 Completed USA | ITA | FRA | DEU | CAN 4
NCT03348631 Phase II Tazemetostat Tazemetostat in Treating Patients With Recurrent Ovarian, Primary Peritoneal, or Endometrial Cancer Active, not recruiting USA 0
NCT03213665 Phase II Tazemetostat Tazemetostat in Treating Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphoma, or Histiocytic Disorders With EZH2, SMARCB1, or SMARCA4 Gene Mutations (A Pediatric MATCH Treatment Trial) Active, not recruiting USA 1
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 Active, not recruiting USA | ITA | FRA | DEU | CAN | BEL 3
NCT02860286 Phase II Tazemetostat Study of the EZH2 Inhibitor Tazemetostat in Malignant Mesothelioma Completed USA | FRA 1


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