tazemetostat

a histone methyltransferase EZH2 inhibitor with antineoplastic activity

Also Known As:

(1,1'-biphenyl)-3-carboxamide, N-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-5-(ethyl(tetrahydro-2h-pyran-4-yl)amino)-4-methyl-4'-(4-morpholinylmethyl)-, hydrobromide (1:2); (1,1'-biphenyl)-3-carboxamide, N-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-5-(ethyl(tetrahydro-2h-pyran-4-yl)amino)-4-methyl-4'-(4-morpholinylmethyl)-, hydrochloride (1:1); E 7438; E-7438 hydrobromide; E7438; EPZ-6438; EPZ-6438 dihydrobromide; EPZ-6438 monohydrobromide; EPZ-6438 monohydrochloride; EPZ-6438 trihydrochloride; EZ-438; EZ438; 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(oxan-4-yl)amino)-4-methyl-4'-((morpholin-4-yl)methyl)(1,1'-biphenyl)-3-carboxamide monohydrobromide; Tazverik; tazemetostat dihydrobromide; tazemetostat hydrobromide; tazemetostat hydrochloride; tazemetostat monohydrobromide; tazemetostat monohydrochloride; tazemetostat trihydrochloride

Networked: 110 relevant articles (16 outcomes, 24 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Experts

1.	Keilhack, Heike: 6 articles (01/2018 - 04/2014)
2.	Copeland, Robert A: 5 articles (01/2018 - 04/2014)
3.	Agarwal, Shefali: 4 articles (01/2022 - 11/2020)
4.	Nishikori, Momoko: 4 articles (01/2022 - 01/2021)
5.	Ribrag, Vincent: 4 articles (01/2022 - 01/2018)
6.	Yang, Jay: 4 articles (01/2022 - 11/2020)
7.	Salles, Gilles: 4 articles (06/2021 - 01/2020)
8.	Knutson, Sarah K: 4 articles (11/2017 - 04/2014)
9.	Fennell, Dean A: 3 articles (01/2022 - 01/2018)
10.	Morschhauser, Franck: 3 articles (01/2022 - 01/2020)

Related Diseases

1.	Neoplasms (Cancer) 01/01/2017 - "Tazemetostat induced significant reduction of H3K27me3 levels in the majority of tumors compared with controls. " 11/08/2023 - "Although tazemetostat did not meet its primary efficacy endpoint in this population of refractory pediatric tumors (objective response rate = 5%, 90% CI = 1% to 20%), 25% of patients with multiple histologic diagnoses experienced prolonged stable disease of 6 months and over (range = 9-26 cycles), suggesting a potential effect of tazemetostat on disease stabilization." 11/08/2023 - "Patients whose tumors harbored EZH2 mutations or loss of SMARCB1 or SMARCA4 by immunohistochemistry were treated with EZH2 inhibitor tazemetostat. " 11/08/2023 - "Tazemetostat for tumors harboring SMARCB1/SMARCA4 or EZH2 alterations: results from NCI-COG pediatric MATCH APEC1621C." 01/01/2023 - "Intriguingly, the W113C mutation leads to tazemetostat resistance in both H3K27 methylation and tumor proliferation. "
2.	Follicular Lymphoma (Lymphoma, Small Cleaved Cell, Follicular) 01/01/2022 - "In the tazemetostat E7438-G000-101 trial of relapsed/refractory (R/R) follicular lymphoma (FL), apparent superior efficacy was suggested for mutant-type (MT) EZH2 versus wild-type (WT) status. " 01/01/2018 - "A recently reported clinical trial indicates that the EZH2 inhibitor tazemetostat is effective against relapsed or refractory follicular lymphoma. " 11/01/2020 - "Tazemetostat is a novel treatment for patients with follicular lymphoma. " 01/01/2018 - "Positive Results for Tazemetostat in Follicular Lymphoma." 01/01/2022 - "Tazemetostat in relapsed/refractory follicular lymphoma: a propensity score-matched analysis of E7438-G000-101 trial outcomes."
3.	Lymphoma (Lymphomas) 03/01/2021 - "We carried out a phase I study of tazemetostat in Japanese patients with relapsed or refractory B-cell non-Hodgkin-type lymphoma (B-NHL) to evaluate its tolerability, safety, pharmacokinetics, and preliminary antitumor activity. " 02/01/2022 - "Tazemetostat monotherapy showed clinically meaningful and durable responses with a favorable toxicity profile, especially in EZH2 mutant lymphoma. " 01/01/2022 - "Tazemetostat also induces lymphoma cells to secrete CCL17/TARC and enhances T-cell migration. " 01/01/2022 - "Tazemetostat restores the expressions of MHC and CD58 in lymphoma cells and synergistically enhances the immune reactions of T and natural killer cells against lymphoma cells. " 01/01/2021 - "Recently tazemetostat hit the market after FDA-approval for the treatment of lymphoma. "
4.	Chordoma 03/14/2022 - "Dramatic In Vivo Efficacy of the EZH2-Inhibitor Tazemetostat in PBRM1-Mutated Human Chordoma Xenograft." 03/14/2022 - "The first demonstration of a high antitumor activity of tazemetostat in a PDX model harboring a PBRM1 variant supports further evaluation for EZH2-inhibitors in this subgroup of chordomas." 01/01/2019 - "We sought to determine the mechanism of an exceptional response in a patient diagnosed with a SMARCB1/INI1-negative chordoma treated with tazemetostat, an EZH2 inhibitor, and followed by radiotherapy.Patient" 01/01/2018 - "In a phase I trial of the EZH2 inhibitor tazemetostat, children with INI1-deficient tumors-including relapsed or refractory malignant rhabdoid tumors, atypical teratoid rhabdoid tumors, epithelioid sarcomas, and poorly differentiated chordomas-responded well to treatment, with some experiencing durable responses."
5.	Sarcoma (Soft Tissue Sarcoma) 03/01/2022 - "Tazemetostat was first approved for patients 16 years and older with metastatic or locally advanced epithelioid sarcoma not eligible for complete resection based on the results of an international open-label phase II basket trial. " 11/01/2020 - "In this study, we report the clinical activity and safety of tazemetostat, an oral selective EZH2 inhibitor, in patients with epithelioid sarcoma. " 11/01/2020 - "Tazemetostat in advanced epithelioid sarcoma with loss of INI1/SMARCB1: an international, open-label, phase 2 basket study." 02/06/2023 - "Based on functional antagonism between BAF/SWI/SNF and PRC2 in SMARCB1 -deficient sarcomas, we and colleagues recently completed the clinical trial of the EZH2 inhibitor tazemetostat, leading to its FDA approval. " 01/01/2023 - "Here, we examined the mechanistic effects of Tazemetostat (EPZ6438), an Food and Drug Administration approved Ezh2 inhibitor for epithelioid sarcoma treatment, because this drug could potentially be repurposed to stimulate osteogenesis for clinical indications. "

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Related Therapies and Procedures

1.	Therapeutics
2.	Immunotherapy
3.	Drug Therapy (Chemotherapy)
4.	Radiotherapy