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 20 | 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 |
|---|---|---|---|---|---|---|---|
| RB1 del SMARCB1 loss | rhabdoid cancer | resistant | Tazemetostat | Preclinical - Cell culture | Actionable | In a preclinical study, a SMARCB1-deficient rhabdoid cancer cell line with a deletion of RB1 was resistant to Tazverik (tazemetostat) in culture (PMID: 38315003). | 38315003 |
| 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... |
| SMARCB1 negative | rhabdoid cancer | predicted - sensitive | Tazemetostat | Case Reports/Case Series | Actionable | In a Phase I trial, Tazemetostat (EPZ-6438) demonstrated safety and preliminary efficacy, resulted in a durable complete response lasting over 2.3 years in a patient with SMARCB1-negative malignant rhabdoid tumor (PMID: 29650362; NCT01897571). | 29650362 |
| 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... |
| SMARCA4 negative | rhabdoid cancer | predicted - sensitive | Tazemetostat | Case Reports/Case Series | Actionable | In a Phase I trial, Tazemetostat (EPZ-6438) demonstrated safety and preliminary efficacy, resulted in 1 partial response and 1 durable stable disease in patient with SMARCA4-negative malignant rhabdoid tumor of the ovary (PMID: 29650362; NCT01897571). | 29650362 |
| SMARCB1 negative | epithelioid sarcoma | predicted - sensitive | Tazemetostat | Case Reports/Case Series | Actionable | In a Phase I trial, Tazemetostat (EPZ-6438) demonstrated safety and preliminary efficacy, resulted durable stable disease in 2 patients with SMARCB1-negative epithelioid sarcoma (PMID: 29650362; NCT01897571). | 29650362 |
| 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 | epithelioid sarcoma | predicted - sensitive | Tazemetostat | Phase II | Actionable | In a Phase II trial, Tazverik (tazemetostat) treatment resulted in an objective response rate of 15% (9/62) and a disease control rate of 26% (16/62) in patients with locally advanced or metastatic SMARCB1 (INI1)-negative epithelioid sarcoma, with a median duration of response not reached and a median overall survival of 82.4 weeks (J Clin Oncol 37, no. 15_suppl (May 20, 2019) 11003-11003, NCT02601950). | detail... |
| SMARCB1 negative | Advanced Solid Tumor | predicted - sensitive | Tazemetostat | Phase I | Actionable | In a Phase I trial, Tazemetostat (EPZ-6438) demonstrated safety and preliminary efficacy, resulted in clinical benefit (stable disease or better) in 38% (5/13) of patients with SMARCB1 or SMARCA4-negative advanced solid tumors (PMID: 29650362; NCT01897571). | 29650362 |
| SMARCB1 loss | nasal cavity carcinoma | predicted - sensitive | Tazemetostat | Case Reports/Case Series | Actionable | In a clinical study, Tazverik (tazemetostat) resulted in a clinical benefit in two patients with loss of SMARCB1, including one patient with sinonasal carcinoma and the other patient with sinonasal undifferentiated carcinoma, with stable disease lasting 13 and 8 months, respectively (PMID: 35820243). | 35820243 |
| RB1 I124Rfs*6 RB1 del SMARCB1 loss | epithelioid sarcoma | predicted - resistant | Tazemetostat | Case Reports/Case Series | Actionable | In a clinical case study, a patient with SMARCB1-deficient epithelioid sarcoma progressed on treatment with Tazverik (tazemetostat) and was found to have acquired a hemizygous deletion of RB1 and RB1 I124Rfs*6 (PMID: 38315003). | 38315003 |
| SMARCA4 negative | Advanced Solid Tumor | predicted - sensitive | Tazemetostat | Phase I | Actionable | In a Phase I trial, Tazemetostat (EPZ-6438) demonstrated safety and preliminary efficacy, resulted in clinical benefit (stable disease or better) in 38% (5/13) of patients with SMARCB1 or SMARCA4-negative advanced solid tumors (PMID: 29650362; NCT01897571). | 29650362 |
| 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 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT04241835 | Phase I | Tazemetostat | A Study of Oral Tazemetostat in Subjects With Moderate and Severe Hepatic Impairment With Advanced Malignancies | Recruiting | USA | SVK | POL | FRA | BEL | 0 |
| NCT02860286 | Phase II | Tazemetostat | Study of the EZH2 Inhibitor Tazemetostat in Malignant Mesothelioma | Completed | USA | GBR | FRA | 0 |
| NCT06575686 | Phase II | Tazemetostat Epcoritamab-bysp + Tazemetostat | Epcoritamab and Tazemetostat for the Treatment of Relapsed or Refractory Grade I-IIIa Follicular Lymphoma | Not yet 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 | CAN | AUS | 1 |
| NCT05567679 | Phase I | Tazemetostat | A Study of Tazemetostat (Tazverik) Before Prostatectomy in Men With Prostate Cancer | Withdrawn | USA | 0 |
| NCT05023655 | Phase II | Tazemetostat | Phase II Study of Tazemetostat in Solid Tumors Harboring an ARID1A Mutation | Recruiting | USA | 0 |
| NCT05934838 | Phase I | Tazemetostat | A Feasibility Trial of Tazemetostat Plus CAR T Cell Therapy in B-cell Lymphomas | Recruiting | USA | 0 |
| 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 |
| NCT03348631 | Phase II | Tazemetostat | Tazemetostat in Treating Patients With Recurrent Ovarian, Primary Peritoneal, or Endometrial Cancer | Active, not 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 | NLD | ITA | GBR | FRA | DNK | DEU | CAN | AUS | 0 |
| NCT03217253 | Phase I | Tazemetostat | Tazemetostat in Treating Patients With Metastatic or Unresectable Solid Tumors or B-Cell Lymphomas With Liver Dysfunction | Withdrawn | USA | 0 |
| NCT02875548 | Phase II | Tazemetostat | Tazemetostat Rollover Study (TRuST): An Open-Label Rollover Study | Enrolling by invitation | USA | POL | GBR | FRA | BEL | AUS | 1 |
| NCT05983965 | Phase I | Tazemetostat Acalabrutinib + Tazemetostat | Study of Tazemetostat in Lymphoid Malignancies | 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 |
| 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 Study of Tazemetostat in Adult Participants With Soft Tissue Sarcoma | Completed | USA | ITA | GBR | FRA | DEU | CAN | BEL | AUS | 1 |
| NCT04917042 | Phase II | Tazemetostat | Tazemetostat in Malignant Peripheral Nerve Sheath Tumors | Recruiting | USA | 0 |
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