RegulationFast Track (United States), Accelerated Approval (United States), Orphan Drug (United States), Orphan Drug (European Union), Conditional marketing approval (China), Priority Review (China)

Structure/Sequence

Molecular FormulaC34H45BrN4O4

InChIKeyUQRICAQPWZSJNF-UHFFFAOYSA-N

CAS Registry1467052-75-0

Clinical Trials associated with Tazemetostat Hydrobromide

NCT06068881

/ Not yet recruitingPhase 2

A Phase 2, Open-label, Single-Arm Clinical Trial to Investigate the Efficacy and Safety of Oral Tazemetostat for the Treatment of Adult Participants Age 18 and Over With Relapsed/Refractory Follicular Lymphoma Lacking the EZH2 Gain-of-Function (GOF) Mutation

The purpose of this research study is to learn about the effectiveness and safety of the study drug, tazemetostat, in adults with relapsed/refractory follicular lymphoma whose tumours do not have an "EZH2 gain-of-function" genetic mutation. Follicular lymphoma is a blood cancer. It affects white blood cells called lymphocytes. White blood cells normally help to fight infections, but when you have follicular lymphoma, the blood cells can form tumours in your body. 'Relapsed/refractory' follicular lymphoma means the disease has either not improved or is getting worse (progressing) during or after previous treatment.
Tazemetostat already has approval in the United States for the treatment of adult patients with relapsed/refractory follicular lymphoma with or without the "EZH2" mutation who have no satisfactory alternative treatment options.
This study is being conducted to better understand the effectiveness in patients whose tumours do not have an "EZH2 gain-of-function" genetic mutation and who previously received therapies commonly used in the U.S. in your body.
'Relapsed/refractory' follicular lymphoma means the disease has either not improved or is getting worse (progressing) during or after previous treatment.
Tazemetostat already has approval in the United States for the treatment of adult patients with relapsed/refractory follicular lymphoma with or without the "EZH2 gain-of-function" mutation who have no satisfactory alternative treatment options. This study is being conducted to better understand the effectiveness in patients whose tumours do not have an "EZH2" genetic mutation and who previously received therapies commonly used in the U.S.
In this study, all participants will receive the study drug. It will be taken by mouth (orally), as a tablet, twice daily. The sizes and number of tumours according to scan results will be collected as well as results of safety tests (such as physical examinations and laboratory tests).
The study consists of 4 periods:
* Screening period may take up to 4 weeks and require at least 1 visit.
* Treatment period will require 2 visits for each of the first 2 months, followed by 1 visit every month for the remainder of the first 12 months, followed by 1 visit every 3 months (except for women of childbearing potential [WOCBP], who will continue to have a pregnancy testing every month) until unacceptable toxicity, disease progression, or the start of new systemic anticancer therapy, whichever is first.
* Safety follow-up period will last for 1 month after the last dose of tazemetostat, and it will end with 1 visit or telephone call.
* Long-term follow-up period is only for participants who stop taking tazemetostat while their disease continues to respond; this period will last until disease progression, start of new cancer treatment, or death from any cause, whichever is first, and will require a visit every 3 months.
Tazemetostat will be provided to participants who tolerate it for as long as their disease does not progress.
Participants may be transferred to another study or program after about 2 years for continued treatment with tazemetostat or for long-term follow-up. Patients may withdraw consent to participate at any time.

Start Date02 Sep 2025

Sponsor / Collaborator

Epizyme, Inc.

[+1]

NCT06824701

/ Not yet recruitingPhase 1IIT

A Phase 1b Study of Tazemetostat in Combination With Zanubrutinib and Anti-CD20 Monoclonal Antibody in Relapsed or Refractory Indolent B-cell Non-Hodgkin Lymphomas

The purpose of this clinical trial is to learn if the study drug Tazemetostat combined with Zanubrutinib and anti-CD20 monoclonal antibody is safe and effective in treating patients with relapsed or refractory indolent B-cell non-Hodgkin lymphoma.

Start Date01 Jun 2025

Sponsor / Collaborator

University of Utah

[+1]

NCT06575686

/ RecruitingPhase 2IIT

A Phase 2 Study of Epcoritamab Plus Tazemetostat for Treatment of Relapsed/Refractory Follicular Lymphoma

This phase II trial tests the safety, side effects and effectiveness of epcoritamab and tazemetostat in treating patients with grade I-IIIa follicular lymphoma that has come back after a period of improvement (relapsed) or that has not responded to previous treatment (refractory). Epcoritamab is a bispecific monoclonal antibody that binds to two different antigens on the surface of cancer cells that may help the body's immune system attack the cancer and may interfere with the ability of the cancer cells to grow and spread. Tazemetostat, a EZH2 inhibitor, may stop the growth of cancer cells by blocking some of the enzymes needed for cell growth. Giving epcoritamab and tazemetostat may be safe, tolerable and/or effective in treating patients with relapsed or refractory grade I-IIIa follicular lymphoma.

Start Date11 Mar 2025

Sponsor / Collaborator

City of Hope National Medical Center

[+1]

100 Clinical Results associated with Tazemetostat Hydrobromide

100 Translational Medicine associated with Tazemetostat Hydrobromide

100 Patents (Medical) associated with Tazemetostat Hydrobromide

462

Literatures (Medical) associated with Tazemetostat Hydrobromide

01 Dec 2025·FUNCTIONAL & INTEGRATIVE GENOMICS

Polycomb repressive complex 2 (PRC2) pathway’s role in cancer cell plasticity and drug resistance

Review

Author: Tabari, Mohammad Amin Khazeei ; Khan, Haroon ; Javan, Alireza ; Larsen, Danaé S ; Rezaee, Aryan ; Heidari, Mohammad Mahdi ; Sanaye, Pantea Majma ; Hadipour, Mahboube ; Daglia, Maria ; Goleij, Pouya

Polycomb Repressive Complex 2 (PRC2) is a central regulator of gene expression via the trimethylation of histone H3 on lysine 27. This epigenetic modification plays a crucial role in maintaining cell identity and controlling differentiation, while its dysregulation is closely linked to cancer progression. PRC2 silences tumor suppressor genes, promoting cell proliferation, metastasis, epithelial-mesenchymal transition, and cancer stem cell plasticity. Enhancement of zeste homolog 2 (EZH2) overexpression or gain-of-function mutations have been observed in several cancers, including lymphoma, breast, and prostate cancers, driving aggressive tumor behavior and drug resistance. In addition to EZH2, other PRC2 components, such as embryonic ectoderm development (EED) and suppressor of zeste 12, are essential for complex stability and function. EED, in particular, enhances EZH2 activity and has emerged as a therapeutic target. Inhibitors like MAK683 and EED226 disrupt EED's ability to maintain PRC2 activity, thereby reducing H3K27me3 levels and reactivating tumor suppressor genes. Valemetostat, a dual inhibitor of both EZH2 and EED, has shown promising results in aggressive cancers like diffuse large B-cell lymphoma and small-cell lung cancer, underlining the therapeutic potential of targeting multiple PRC2 components. PRC2's role extends beyond gene repression, as it contributes to metabolic reprogramming in tumors, regulating glycolysis and lipid synthesis to fuel cancer growth. Furthermore, PRC2 is implicated in chemoresistance, particularly by modulating DNA damage response and immune evasion. Tazemetostat, a selective EZH2 inhibitor, has demonstrated significant clinical efficacy in EZH2-mutant cancers, such as non-Hodgkin lymphomas and epithelioid sarcoma. However, the compensatory function of enhancer of zeste homolog 1 (EZH1) in some cancers requires dual inhibition strategies, as seen with agents like UNC1999 and Tulmimetostat, which target both EZH1 and EZH2. Given PRC2's multifaceted role in cancer biology, its inhibition represents a promising avenue for therapeutic intervention. The continued development of PRC2 inhibitors and exploration of their use in combination with standard chemotherapy or immunotherapy has great potential for improving patient outcomes in cancers driven by PRC2 dysregulation.

01 Aug 2025·BRAIN BEHAVIOR AND IMMUNITY

EZH2-mediated suppression of TIMP1 in spinal GABAergic interneurons drives microglial activation via MMP-9-TLR2/4-NLRP3 signaling in neuropathic pain

Article

Author: Pan, Yinbing ; Wu, Xuefeng ; Wu, Xudong ; Liu, Wentao ; Hu, Fan ; Guo, Haiyue ; Jiang, Chun-Yi ; Yang, Shuo ; Wan, Li

Effective management of neuropathic pain remains a significant challenge due to the limited understanding of its underlying mechanisms. We found that the FDA-approved enhancer of zeste homolog 2 (EZH2) inhibitor, EPZ6438, can prevent the development of neuropathic pain caused by chronic constriction injury (CCI). Therefore, we utilized EPZ6438 as a probe to investigate the molecular events involved in the early stage of neuropathic pain. RNA-seq analysis reveals that EPZ6438 significantly upregulates Timp1 transcription in the spinal cord of mice. As a specific endogenous inhibitor of MMP-9, tissue inhibitor of metalloproteinase 1 (TIMP1) levels significantly decrease in the cerebrospinal fluid of both neuropathic pain patients and the CCI rat models. Importantly, intrathecal administration of mouse recombinant TIMP1 protein (rmTIMP1) reverses CCI-induced mechanical and thermal hyperalgesia. Mechanistically, substance P released from primary sensory neurons suppresses TIMP1 in spinal GABAergic interneurons by elevating EZH2 expression, which enhances H3K27me3 enrichment at the Timp1 promoter. Blocking spinal NK1R effectively prevents the downregulation of TIMP1 and alleviates CCI-induced hyperalgesia. The imbalance between TIMP1 and MMP-9 leads to NLRP3 activation in spinal microglia and increases IL-1β maturation via TLR2/4 pathway. TIMP1 injection eliminates MMP-9-induced NLRP3 activation and blocks hyperalgesia, suggesting that TIMP1 is a critical gatekeeper in preventing neuroinflammation during neuropathic pain development.

22 May 2025·JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Highly Potent and Selective EZH2 Covalent Inhibitors via Incorporating Basic Amines

Article

Author: Liu, Li ; Liu, Xinqiao ; Fang, Wei ; Zhang, Ying ; Shi, Qiongyu ; Wang, Yuanxiang ; Zhang, Yi ; Huang, Yuting ; Yang, Hong ; Huang, Xun

Targeted covalent inhibition is a promising strategy to address the high dose and acquired drug resistance issues of the first-generation EZH2 noncovalent inhibitors. Recently we have reported a new generation of highly potent EZH2 covalent inhibitors, but further optimization to enhance aqueous solubility is required. Here, we described the systematic optimization of EPZ-6438 by preserving the aqueous groups, resulting in the identification of a highly potent and selective EZH2 covalent inhibitor 13, which displayed nanomolar potency in biochemical and cellular assays. Moreover, SAM competition experiments preliminarily confirmed that 13 was noncompetitive with SAM, leading to the remarkable reduction of the H3K27Me3 marker. In addition, 13 exhibited superior cell growth inhibition in the EZH2 mutant cancer cell lines. The discovery of 13 holds promise for the development of highly potent EZH2 covalent inhibitors.

News (Medical) associated with Tazemetostat Hydrobromide

28 Apr 2025

·www.globenewswire.com

Arvinas Shares New Preclinical Combination Data for the PROTAC BCL6 Degrader, ARV-393, at the 2025 American Association for Cancer Research Annual Meeting

– ARV-393 demonstrated strong synergistic antitumor activity, including complete regressions, in combination with standard-of-care chemotherapy, biologics, and select investigational oral small molecule inhibitors – – Findings support continued evaluation of ARV-393 combinations in non-Hodgkin lymphoma – NEW HAVEN, Conn., April 28, 2025 (GLOBE NEWSWIRE) -- Arvinas, Inc. (Nasdaq: ARVN), a clinical-stage biotechnology company working to develop a new class of drugs based on targeted protein degradation, today presented data from preclinical combination studies of ARV-393, the company’s investigational PROteolysis TArgeting Chimera (PROTAC) B-cell lymphoma 6 protein (BCL6) degrader. BCL6 is a transcriptional repressor protein and a known driver of B-cell lymphomas. Data demonstrated synergistic antitumor activity, including complete regressions, in combination with standard of care (SOC) chemotherapy, SOC biologics, and investigational oral small molecule inhibitors (SMIs) in high grade B-cell lymphoma (HGBCL) and aggressive diffuse large B-cell lymphoma (DLBCL) models. The results from these preclinical studies were shared in a poster presentation at the 2025 American Association for Cancer Research (AACR) annual meeting in Chicago, Illinois. Key findings from the studies included: ARV-393 in combination with SOC chemotherapy (rituximab, cyclophosphamide, doxorubicin, vincristine, and prednisone [R-CHOP]), induced significantly greater tumor growth inhibition compared with rituximab, CHOP, R-CHOP, or ARV-393 alone, with complete tumor regressions in all mice treated with the ARV-393 and R-CHOP combination.ARV-393 in combination with SOC biologics targeting CD20 (rituximab), CD19 (tafasitamab), or CD79b (polatuzumab vedotin) resulted in tumor regressions and demonstrated significantly stronger tumor growth inhibition compared with each agent alone.In preclinical models, ARV-393 increased CD20 expression, providing additional support for the exploration of combinations with CD20-targeted agents and in the context of low or loss of CD20 expression.ARV-393 in combination with investigational small molecule inhibitors targeting clinically validated oncogenic drivers of lymphoma, such as BTK (acalabrutinib), BCL2 (venetoclax), or EZH2 (tazemetostat), resulted in superior tumor growth inhibition compared with each agent alone, with tumor regressions in all mice treated with the combinations. “Given that combination regimens are the foundation of lymphoma treatment, we are encouraged by the strength of these preclinical combination data, which demonstrate complete tumor regressions in aggressive lymphoma models,” said Noah Berkowitz, M.D., Ph.D., Chief Medical Officer at Arvinas. “We believe these preclinical data demonstrate potential for broad combinability of ARV-393 and provide a compelling rationale for considering combination strategies as we work to bring forward new therapeutic options for lymphoma patients.” A Phase 1 study of ARV-393 is enrolling patients with relapsed/refractory non-Hodgkin lymphoma, including DLBCL (NCT06393738). Additional detail on the ARV-393 data presentation at AACR 2025: Poster Title: ARV-393, a PROteolysis TArgeting Chimera (PROTAC) BCL6 Degrader, Combined With Biologics or Small-Molecule Inhibitors Induces Tumor Regressions in Diffuse Large B-Cell Lymphoma ModelsAbstract: 1655Session Title: Degraders and Glues 2 Session Type: Experimental and Molecular TherapeuticLocation: Poster Section 18Poster Board Number: 15Date: Monday, April 28, 2025Lecture Time: 9:00 a.m. – 12:00 p.m. CT About ARV-393ARV-393 is an investigational, orally bioavailable PROteolysis TArgeting Chimera (PROTAC) designed to degrade B-cell lymphoma 6 protein (BCL6), a transcriptional repressor and major driver of B-cell lymphomas. During B-cell development, tightly controlled BCL6 protein expression regulates >600 genes to facilitate rapid B-cell proliferation and tolerance of somatic hypermutation and gene recombination for antibody generation. Deregulated BCL6 expression is common in B-cell lymphoma and promotes cancer cell survival, proliferation, and genomic instability. PROTAC-mediated degradation has the potential to address the historically undruggable nature of BCL6. ARV-393 is currently in a Phase 1 clinical trial in patients with relapsed/refractory non-Hodgkin lymphoma. About ArvinasArvinas (Nasdaq: ARVN) is a clinical-stage biotechnology company dedicated to improving the lives of patients suffering from debilitating and life-threatening diseases. Through its PROteolysis TArgeting Chimera (PROTAC) protein degrader platform, the Company is pioneering the development of protein degradation therapies designed to harness the body’s natural protein disposal system to selectively and efficiently degrade and remove disease-causing proteins. Arvinas is currently progressing multiple investigational drugs through clinical development programs, including vepdegestrant, targeting the estrogen receptor for patients with locally advanced or metastatic ER+/HER2- breast cancer; ARV-393, targeting BCL6 for relapsed/refractory non-Hodgkin Lymphoma; and ARV-102, targeting LRRK2 for neurodegenerative disorders. Arvinas is headquartered in New Haven, Connecticut. For more information about Arvinas, visit www.arvinas.com and connect on LinkedIn and X. Forward-Looking StatementsThis press release contains forward-looking statements within the meaning of The Private Securities Litigation Reform Act of 1995 that involve substantial risks and uncertainties, including statements regarding the potential for Arvinas’ investigational oral PROteolysis TArgeting Chimera (PROTAC) degrader ARV-393 to treat relapsed/refractory non-Hodgkin lymphoma; the preclinical data for ARV-393 demonstrating the potential for broad combinability and supporting continued evaluation of ARV-393 combinations in non-Hodgkin lymphoma associated with B-cell lymphoma 6 protein (“BCL6”) dysfunction; and PROTAC-mediated degradation having the potential to address the historically undruggable nature of BCL6.. All statements, other than statements of historical facts, contained in this press release, including statements regarding Arvinas’ strategy, future operations, future financial position, future revenues, projected costs, prospects, plans and objectives of management, are forward-looking statements. The words “anticipate,” “believe,” “estimate,” “expect,” “intend,” “may,” “might,” “plan,” “predict,” “project,” “target,” “potential,” “will,” “would,” “could,” “should,” “continue,” and similar expressions are intended to identify forward-looking statements, although not all forward-looking statements contain these identifying words. Arvinas may not actually achieve the plans, intentions or expectations disclosed in these forward-looking statements, and you should not place undue reliance on such forward-looking statements. Actual results or events could differ materially from the plans, intentions and expectations disclosed in the forward-looking statements Arvinas makes as a result of various risks and uncertainties, including but not limited to: whether Arvinas will be able to successfully conduct and complete development for its product candidates, including ARV-393, including whether Arvinas initiates and completes clinical trials for its product candidates and receives results from its clinical trials on its expected timelines or at all; Arvinas’ ability to protect its intellectual property portfolio; whether Arvinas’ cash and cash equivalent resources will be sufficient to fund its foreseeable and unforeseeable operating expenses and capital expenditure requirements; and other important factors discussed in the “Risk Factors” section of Arvinas’ Annual Report on Form 10-K for the year ended December 31, 2024 and subsequent other reports on file with the U.S. Securities and Exchange Commission. The forward-looking statements contained in this press release reflect Arvinas’ current views with respect to future events, and Arvinas assumes no obligation to update any forward-looking statements, except as required by applicable law. These forward-looking statements should not be relied upon as representing Arvinas’ views as of any date subsequent to the date of this release. Contacts:Investors:Jeff Boyle+1 (347) 247-5089Jeff.Boyle@arvinas.com Media:Kirsten Owens+1 (203) 584-0307Kirsten.Owens@arvinas.com

Phase 1AACRPROTACs

25 Mar 2025

·www.globenewswire.com

HUTCHMED Announces NMPA Conditional Approval for TAZVERIK® (tazemetostat) for the Treatment of Relapsed or Refractory Follicular Lymphoma

— First and only EZH2 inhibitor approved by the NMPA — — HUTCHMED’s fourth product, and its first approval in hematological malignancies — March 21, 2025 -- HUTCHMED (China) Limited (“HUTCHMED”) (Nasdaq/AIM:HCM; HKEX:13) today announces that the New Drug Application (“NDA”) for TAZVERIK® (tazemetostat) has been granted conditional approval in China for the treatment of adult patients with relapsed or refractory (“R/R”) follicular lymphoma (“FL”) with EZH2 mutation who have received at least two prior systemic therapies. This approval follows the priority review status by the National Medical Products Administration (“NMPA”) and marks the first nationwide regulatory approval for TAZVERIK® in China. The conditional approval by the NMPA was supported by results from a multicenter, open-label, Phase II bridging study in China, and clinical studies conducted by Epizyme, Inc. (“Epizyme”), an Ipsen company, outside China. The primary objective of the bridging study is to evaluate the objective response rate (“ORR”) of TAZVERIK® for the treatment of patients with R/R FL whose disease harbor EZH2 mutations. The secondary objectives included duration of response (“DoR”), progression-free survival (PFS), and overall survival (OS) of TAZVERIK® for the treatment of R/R FL patients, as well as to evaluate the safety and pharmacokinetics. Additional details can be found at clinicaltrials.gov, using identifier NCT05467943. “This approval represents a significant advancement in the management of this challenging disease. The majority of FL patients experience multiple relapses over their lifetime, posing substantial treatment difficulties and often leading to poor outcomes,” said Dr Junning Cao of Fudan University Cancer Center and the lead principal investigator of the bridging study. “TAZVERIK® has demonstrated promising efficacy in patients harboring EZH2 mutation in clinical trials. We are eager to provide this transformational epigenetic therapy to patients in China who have long sought new effective treatment options.” “We are thrilled to be able to bring this innovative EZH2 inhibitor to patients in China. This approval highlights our dedication to addressing unmet medical needs not only through our internal pipeline, but also through partnering,” said Dr Michael Shi, Head of R&D and Chief Medical Officer of HUTCHMED. “It also marks our first approval in hematological malignancies, unveiling a new chapter for HUTCHMED as we extend our footprint into this disease area. As we move forward, we are dedicated to making this product available to R/R FL patients as soon as possible and will continue striving to make a meaningful impact on the lives of more patients suffering from devastating diseases.” TAZVERIK® is a first-in-class methyltransferase inhibitor of EZH2 developed by Epizyme. It is approved by the US Food and Drug Administration (“FDA”) for the treatment of certain patients with R/R FL and certain patients with advanced epithelioid sarcoma (“ES”) under the FDA accelerated approval program. It is also approved by the Japan Ministry of Health, Labour and Welfare (MHLW) for certain patients with R/R FL. In 2021, HUTCHMED and Epizyme entered a strategic partnership. HUTCHMED is responsible for the research, development, manufacturing and commercialization of TAZVERIK® in China Mainland, Hong Kong, Macau and Taiwan. Epizyme will be the Marketing Authorization Holder of TAZVERIK® in China. TAZVERIK® was approved for use in the Hainan Boao Lecheng International Medical Tourism Pilot Zone (Hainan Pilot Zone) in May 2022, under the Clinically Urgently Needed Imported Drugs scheme, for the treatment of certain patients with ES and FL consistent with the label as approved by the FDA. TAZVERIK® was approved in Macau in March 2023 and in Hong Kong in May 2024. The ongoing SYMPHONY-1 study will serve as the confirmatory trial to validate the clinical benefits of TAZVERIK®. SYMPHONY-1 is an international, multicenter, randomized, double-blind, active-controlled, 3-stage, biomarker-enriched, confirmatory Phase Ib/III study, which is designed to evaluate the safety and efficacy of TAZVERIK® in combination with rituximab and lenalidomide (R²) in patients with R/R FL after at least one prior line of therapy (NCT04224493). Epizyme is the sponsor of SYMPHONY-1 and HUTCHMED is leading the study in China. FL is the second most common subtype of non-Hodgkin’s lymphoma (“NHL”), making up 20-30% of all NHL. In 2022, there were an estimated 81,000 and 78,000 new cases of NHL in China and the US, respectively.1,2,3 Tazemetostat is a methyltransferase inhibitor indicated in the United States for the treatment of: Adults and pediatric patients aged 16 years and older with metastatic or locally advanced ES not eligible for complete resection. Adult patients with R/R FL whose tumors are positive for an EZH2 mutation as detected by an FDA-approved test and who have received at least two prior systemic therapies. Adult patients with R/R FL who have no satisfactory alternative treatment options. These indications are approved under accelerated approval by the US FDA based on ORR and DoR. Continued approval for these indications may be contingent upon verification and description of clinical benefit in confirmatory trials. The most common (≥20%) adverse reactions in patients with ES are pain, fatigue, nausea, decreased appetite, vomiting and constipation. The most common (≥20%) adverse reactions in patients with FL are fatigue, upper respiratory tract infection, musculoskeletal pain, nausea and abdominal pain. TAZVERIK® is approved in Japan with the indication of relapsed or refractory EZH2 gene mutation-positive FL (only when standard treatment is not applicable). TAZVERIK® is commercialized by Epizyme in the US and by Eisai in Japan. TAZVERIK® is a registered trademark of Epizyme Inc., an Ipsen company. HUTCHMED (Nasdaq/AIM:HCM; HKEX:13) is an innovative, commercial-stage, biopharmaceutical company. It is committed to the discovery and global development and commercialization of targeted therapies and immunotherapies for the treatment of cancer and immunological diseases. Since inception it has focused on bringing drug candidates from in-house discovery to patients around the world, with its first three medicines marketed in China, the first of which is also approved around the world including in the US, Europe and Japan. 1 NCCN Guidelines for Patients: Follicular Lymphoma. https://www.nccn.org/patients/guidelines/content/PDF/nhl-follicular-patient.pdf. Accessed February 17, 2025. 2 SEER Cancer Stat Facts: Follicular Lymphoma. National Cancer Institute. https://seer.cancer.gov/statfacts/html/follicular.html. Accessed February 17, 2025 3 The Global Cancer Observatory (GLOBOCAN), Cancer Today | IARC. https://gco-iarc-who-int.libproxy1.nus.edu.sg/today/en/dataviz/bars?cancers=34. Accessed February 17, 2025. The content above comes from the network. if any infringement, please contact us to modify.

$HUTCHMED Announces NMPA Conditional Approval for TAZVERIK® (tazemetostat) for the Treatment of Relapsed or Refractory Follicular Lymphoma$

Drug ApprovalPriority ReviewImmunotherapyClinical Result

21 Mar 2025

·www.pharmaceutical-technology.com

China conditionally approves Hutchmed’s Tazverik for follicular lymphoma

The bridging study’s main objective is to assess the objective response rate of the therapy in subjects with R/R FL with EZH2 mutations. Credit: Chay_Tee/Shutterstock. China’s National Medical Products Administration (NMPA) has granted conditional approval for Hutchmed’s Tazverik (tazemetostat) to treat adults with relapsed or refractory (R/R) follicular lymphoma (FL) with enhancer of zeste homolog 2 (EZH2) mutation. The decision is intended for individuals who have undergone a minimum of two previous systemic therapies. This is the first regulatory approval for the therapy in China and comes after it gained NMPA’s priority review status. Hutchmed chief medical officer and research and development (R&D) head Dr Michael Shi stated: “We are thrilled to be able to bring this innovative EZH2 inhibitor to patients in China. This approval highlights our dedication to addressing unmet medical needs not only through our internal pipeline, but also through partnering. “As we move forward, we are dedicated to making this product available to R/R FL patients as soon as possible and will continue striving to make a meaningful impact on the lives of more patients suffering from devastating diseases.” The conditional approval was based on the outcomes from the multicentre, open-label, Phase II bridging study in the country, alongside clinical trials conducted outside the country by Ipsen’s Epizyme, the developer of the therapy. The bridging study’s main objective is to assess the objective response rate (ORR) of the therapy in treating subjects with R/R FL with EZH2 mutations. Secondary objectives are progression-free survival, overall survival and duration of response, along with assessment of the therapy’s pharmacokinetics and safety. Hutchmed and Epizyme entered a strategic collaboration in 2021, with the former taking on the responsibilities for the therapy’s research, development, manufacturing and commercialisation in mainland China, Macau, Taiwan and Hong Kong, while the latter holds marketing authorisation in the country. In January 2025, the NMPA granted acceptance and priority review for the new drug application for Hutchmed’s Orpathys and Tagrisso combo, targeting individuals with locally advanced or metastatic non-small cell lung cancer.

Phase 2Drug ApprovalPriority Review

100 Deals associated with Tazemetostat Hydrobromide

External Link

KEGG	Wiki	ATC	Drug Bank
D11485	Tazemetostat Hydrobromide	L01	DB12887

R&D Status

Approved

10 top approved records.

to view more data

Indication	Country/Location	Organization	Date
Follicular Lymphoma	United States	Epizyme, Inc.	18 Jun 2020
Sarcoma	United States	Epizyme, Inc.	23 Jan 2020

Developing

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Refractory Follicular Lymphoma	Phase 3	United States	Epizyme, Inc.	11 Jun 2020
Refractory Follicular Lymphoma	Phase 3	China	Epizyme, Inc.	11 Jun 2020
Refractory Follicular Lymphoma	Phase 3	Australia	Epizyme, Inc.	11 Jun 2020
Refractory Follicular Lymphoma	Phase 3	Belgium	Epizyme, Inc.	11 Jun 2020
Refractory Follicular Lymphoma	Phase 3	Canada	Epizyme, Inc.	11 Jun 2020
Refractory Follicular Lymphoma	Phase 3	France	Epizyme, Inc.	11 Jun 2020
Refractory Follicular Lymphoma	Phase 3	Germany	Epizyme, Inc.	11 Jun 2020
Refractory Follicular Lymphoma	Phase 3	Hungary	Epizyme, Inc.	11 Jun 2020
Refractory Follicular Lymphoma	Phase 3	Italy	Epizyme, Inc.	11 Jun 2020
Refractory Follicular Lymphoma	Phase 3	Poland	Epizyme, Inc.	11 Jun 2020

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASCO2025	Not Applicable	Follicular Lymphoma \| Diffuse Large B-Cell Lymphoma	306	Tazemetostat as monotherapy	yvolnovlps(zvrkzzflva) = pooled value of 84.5% at 12 months fbwlwtxjmi (umlxjtrerl )	Positive	30 May 2025
				Tazemetostat in combination therapy
ASCO2025	Phase 1/2	B-Cell Lymphoma mutant EZH2	241	Tazemetostat 800 mg twice daily	ahuvcxlpak(weuvbvcssu) = tejphljbcu excmxyzium (lsktkxayrc, 29.4 - 69.9) View more	Positive	30 May 2025
NCT02601950 (CTgov)	Phase 2	Typical Teratoid Rhabdoid Tumor \| Chordoma \| Renal Medullary Carcinoma ... View more	267	tazemetostat (Rhabdoid Tumors: Cohort 1)	ljxhhyirpb = ycgkrzhtjc qcncmzywvx (laugwbmegi, yajvbpqtas - xiqikhajxm) View more	-	11 Mar 2025
				tazemetostat (Other INI1-negative: Cohort 3)	ljxhhyirpb = ilrtsmuvcr qcncmzywvx (laugwbmegi, sbmqfrfrky - noiomxhdws) View more
NCT03348631 (CTgov)	Phase 2	Recurrent Ovarian Clear Cell Adenocarcinoma \| Endometrial Endometrioid Adenocarcinoma \| Recurrent ovarian cancer ... View more	62	Tazemetostat (Arm I: Treatment (Tazemetostat) in Endometrial Cancer Patients)	yygttyqiyy = svbbmerinh vltiemhsir (vlattjqvss, tlssfjfpun - dvgrtdonfb) View more	-	06 Mar 2025
				Tazemetostat (Arm II: Treatment (Tazemetostat) Ovarian in Cancer Patients)	yygttyqiyy = ckkjtvwjjn vltiemhsir (vlattjqvss, psasyliiwh - yamdsqeljv) View more
ASH2024	Not Applicable	Follicular Lymphoma	-	Tazemetostat 800mg BID	rbeycsgkoh(tbgxnqxqxj) = leukopenia (n=2), neutropenia (n=1), anemia (n=1), atrial fibrillation (n=1), bone pain (n=1), infection (n=2), and infusion related reaction (n=1) joxwqxxbkl (yvipaytnpl ) View more	-	09 Dec 2024
NCT04179864 (EZH-1101, ESMO2024) Manual	Phase 1/2	Metastatic castration-resistant prostate cancer	81	TAZ 1200 mg BID plus ENZ 160 mg QD	kqtyakmvcv(yktyejhtma) = daoxxmhiwk fcbbqxkxek (drrsowmwvh, 8.5 - NE) View more	Negative	15 Sep 2024
				ENZ 160 mg QD	kqtyakmvcv(yktyejhtma) = qkowkkmgok fcbbqxkxek (drrsowmwvh, 6.6 - NE) View more
NCT04537715 (CTgov)	Phase 1	Renal Medullary Carcinoma \| Follicular Lymphoma \| Rhabdoid Tumor ... View more	42	Tazemetostat (Part 1: Tazemetostat)	snxsmnunhs(aeyruqnfvu) = pxdnyyaext ldtypbezsf (hamoksgbnq, 55.3) View more	-	26 Aug 2024
				Tazemetostat (Part 2: Tazemetostat)	zszqvqbyva(vzqupotjng) = hkrrcivtqx xuhjptsynb (kfmfpbgaxz, 83.2) View more
NCT03854474 (ETCTN 10183, ASCO2024)	Phase 1/2	Advanced Urothelial Carcinoma COMPASS-related proteins KMT2D \| KMT2C \| KDM6A ... View more	-	Tazemetostat 800 mg BID + Pembrolizumab 200 mg	zxooxgmjzh(taacjqiymh) = javyrhjcfh bssddtiuev (urnbcfpxwc ) View more	-	24 May 2024
				Pembrolizumab 200 mg	zxooxgmjzh(taacjqiymh) = urzhhjmmon bssddtiuev (urnbcfpxwc ) View more
NCT05372354 (CA057-003, EHA2024) Manual	Phase 1/2	Multiple Myeloma PRC2 Loss of Function Mutation \| EZH2 Overexpression	10	MEZI+TAZ+DEX 0.3mg	lfvltwrana(bvarpspplt) = kbbqbjtthx ehanpnojhp (dmqmdqitoq ) View more	Positive	14 May 2024
NCT05713110 (EHA2024)	Phase 2	Lymphoma	21	Tazemetostat 800mg BID	kwgksrvcfj(tkynpppztj) = 4 pts, 19.0% nlakmimqtg (ifoemnpidy ) View more	Positive	14 May 2024
				Amdizalisib 30mg QD

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