Valemetostat Tosilate(Valemetostat Tosilate) - 药物靶点：EZH1 x EZH2_在研适应症：成人T细胞白血病/淋巴瘤，外周T细胞淋巴瘤，B细胞淋巴瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

valemetostat tosilate、valemetostat tosylate、DS-3201

+ [5]

靶点

EZH1 x EZH2

作用方式

抑制剂

作用机制

EZH1抑制剂(Zeste基因增强子同源物1抑制剂)、EZH2抑制剂(组蛋白赖氨酸甲基化酶EZH2抑制剂)

治疗领域

肿瘤免疫系统疾病血液及淋巴系统疾病+ [3]

在研适应症

成人T细胞白血病/淋巴瘤外周T细胞淋巴瘤B细胞淋巴瘤+ [10]

非在研适应症

急性淋巴细胞白血病急性髓性白血病

原研机构

Daiichi Sankyo Co., Ltd.

在研机构

Daiichi Sankyo Co., Ltd.

Daiichi Sankyo Propharma Co., Ltd.

Daiichi Sankyo, Inc.

+ [1]

非在研机构-

权益机构

University of Tokyo

Daiichi Sankyo Co., Ltd.The Lymphoma Study Association

最高研发阶段批准上市

首次获批日期

日本 (2022-09-26),

成人T细胞白血病/淋巴瘤外周T细胞淋巴瘤

最高研发阶段(中国)临床1/2期

特殊审评孤儿药 (美国)、孤儿药 (欧盟)、孤儿药 (日本)

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结构/序列

分子式C33H42ClN3O7S

InChIKeyJSBKGJUYSLVFPF-WJQUPPJOSA-N

CAS号1809336-93-3

关联

21

项与 Valemetostat Tosilate 相关的临床试验

NCT06294548

/ Not yet recruiting临床1/2期IIT

A Phase Ib/II, Dose Escalation and Dose Expansion Study of Valemetostat Tosylate (DS-3201b) With Atezolizumab and Bevacizumab in Advanced Hepatocellular Carcinoma (HCC)

This is a phase Ib/II, dose escalation and dose expansion study of valemetostat (DS-3201) with atezolizumab and bevacizumab in patients advanced Hepatocellular carcinoma (HCC) who did not receive prior systemic therapy for advanced HCC.

开始日期2025-06-30

申办/合作机构

The University of Alabama at Birmingham

NCT05879484

/ Not yet recruiting临床1/2期IIT

A Phase Ib/II Multicenter Study of Front Line Pembrolizumab and Valemetostat in PD-L1 Positive, HPV-Negative Recurrent/Metastatic Squamous Cell Carcinoma (SCC) of the Head and Neck: The PANTHERAS

Background:
Head and neck squamous cell carcinoma (HNSCC) is the 6th most common cancer worldwide. These cancers have different causes, with smoking/tobacco exposure and human papilloma virus infection being the most common. . When HNSCC occurs in people who are not infected with HPV, the cancers are more likely to return after treatment; when this happens, overall survival is only about 10 months, thus better treatments are needed.
Objective:
To test a combination treatment using 2 drugs (valemetostat and pembrolizumab) in people with HNSCC. Phase 1b of the study will determine a recommended dose of the 2 drugs and evaluate how safe the combination is.; this will include patients with HPV-positive and HPV-negative HNSCC, as well as squamous cell NSCLC that have progressed on anti-PD-1/anti-PD-L1 therapies.Phase II will determine how effective the combination is and will focus on patients with HPV-negative HNSCC.
Eligibility:
People aged 18 years and older with HPV-negative HNSCC, sinonasal carcinoma of the head and neck, or squamous non-small cell lung cancer (NSCLC).
Design:
Participants will be screened. They will have a physical exam. They will have blood and urine tests and tests of their heart function. They will have imaging scans. They may have a biopsy: A small sample of tissue will be removed from the tumor.
Treatment will be given in 21-day cycles.
Pembrolizumab is administered through a tube attached to a needle inserted into a vein in the arm. Participants will receive pembrolizumab on the first day of each cycle.
Valemetostat is a tablet taken by mouth. Participants will take the tablet once a day at home. They will record the date and time of each dose in a diary. They will also write down any adverse effects they experience.
Participants may remain in the study up to 2 years.

开始日期2025-06-17

申办/合作机构

National Cancer Institute

NCT06632977

/ Recruiting临床2期IIT

PREcision DIagnostics in Prostate Cancer Treatment (PREDICT)

This phase II trial evaluates whether genetic testing in prostate cancer is helpful in deciding which study treatment patients are assigned. Patient cancer tissue samples are obtained from a previous surgery or biopsy procedure and tested for deoxyribonucleic acid (DNA) and ribonucleic acid (RNA) abnormalities or mutations in their cancer. Valemetostat tosylate is in a class of medications called EZH1/EZH2 inhibitors. It blocks proteins called EZH1 and EZH2, which may help slow or stop the spread of tumor cells. Carboplatin is in a class of medications known as platinum-containing compounds. It works in a way similar to the anticancer drug cisplatin, but may be better tolerated than cisplatin. Carboplatin works by killing, stopping or slowing the growth of tumor cells. Cabazitaxel injection is in a class of medications called microtubule inhibitors. It works by slowing or stopping the growth of tumor cells. Abiraterone acetate blocks tissues from making androgens (male hormones), such as testosterone. This may cause the death of tumor cells that need androgens to grow. It is a type of anti-androgen. Enzalutamide is in a class of medications called androgen receptor inhibitors. It works by blocking the effects of androgen (a male reproductive hormone) to stop the growth and spread of tumor cells. Lutetium Lu 177 vipivotide tetraxetan is in a class of medications called radiopharmaceuticals. It works by targeting and delivering radiation directly to tumor cells which damages and kills these cells. Assigning patients to targeted treatment based on genetic testing may help shrink or slow the cancer from growing

开始日期2025-02-06

申办/合作机构

Alliance for Clinical Trials in Oncology

[+1]

100 项与 Valemetostat Tosilate 相关的临床结果

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100 项与 Valemetostat Tosilate 相关的转化医学

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100 项与 Valemetostat Tosilate 相关的专利（医药）

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65

项与 Valemetostat Tosilate 相关的文献（医药）

2025-12-01·FUNCTIONAL & INTEGRATIVE GENOMICS

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

Review

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

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.

2025-12-01·CANCER CHEMOTHERAPY AND PHARMACOLOGY

Pharmacokinetics, metabolism, and excretion of [14C]-valemetostat in healthy male participants, and in vitro plasma protein binding

Article

作者: Siebers, Nicholas ; Inaba, Shinichi ; Craveiro, Thuy Vu ; Ikeda, Tomoko ; Kazui, Miho ; Shimizu, Takako ; Tachibana, Masaya ; Abutarif, Malaz A

INTRODUCTION:

Valemetostat tosylate (valemetostat) is an oral, selective, dual inhibitor of enhancer of zeste homolog (EZH)2 and EZH1. This article reports findings on the mass balance and pharmacokinetics of valemetostat in a phase I study; valemetostat metabolite identification in plasma, urine, and fecal samples; and plasma-protein-binding of valemetostat in vitro.

METHODS:

Eight healthy participants received a single 200-mg oral dose of [¹⁴C]-valemetostat under fasting conditions. Blood, urine, and feces samples were collected to determine total radioactivity and/or unchanged valemetostat, and for metabolite identification. The binding of valemetostat 600-10,000 ng/mL to plasma, 4% human serum albumin (HSA), and 0.1% alpha-1-acid glycoprotein (AAG) was assessed in vitro.

RESULTS:

Mean cumulative recovery of administered radioactivity was 95.3% by 360 h post-dose, with a mean recovery of 15.6% in urine and 79.8% in feces. Valemetostat accounted for the most radioactivity in the excreta, at 10% and 64.9% of the administered dose in the urine and feces, respectively. CALZ-1809a was the most abundant metabolite, present in all biological samples, and accounted for 5.6% of total radioactivity in the feces. Valemetostat was minimally associated with red blood cells, with a blood-to-plasma total radioactivity ratio of 0.54. In vitro, valemetostat was highly plasma-bound (> 94%) at clinically relevant concentrations, with a higher affinity to AAG than to HSA.

CONCLUSION:

Valemetostat was rapidly absorbed into the systemic circulation, mainly excreted via the biliary/fecal route, primarily metabolized by CYP3A enzymes to CALZ-1809a, and highly bound to plasma proteins, with a greater affinity to AAG than HSA in vitro.

2025-06-09·Clinical Epigenetics

EZH1 deficiency promotes ferroptosis resistance by activating NRF2 in sepsis-associated liver injury.

Article

作者: Huang, Junqi ; You, Ying ; Mei, Meihua ; He, Xiaoshun ; Tan, Ningxin

Sepsis-associated acute liver injury (SALI) is a major clinical complication of sepsis due to excessive, unfettered inflammation. In recent years, the role of epigenetic regulatory mechanisms in SALI has been gradually emphasized. Here, we investigated the effects of a Histone-lysine N-methyltransferase EZH1 (Enhancer of zeste homolog 1) inhibition on promoting ferroptosis resistance to activate nuclear factor, erythroid derived 2, like 2 (NRF2) in SALI. We found that EZH1 deficiency improved animal survival in lethal sepsis. EZH1 deficiency mice exhibited alleviated SALI with decreased hepatocellular ferroptosis. EZH1 deficiency attenuated the H3K27me3 modification in the Nfe2l2 promoter, lending to the increased expression and nuclear translocation of NRF2. In the in vitro, LPS-induced ferroptosis model, EZH1 inhibitor DS3201 exhibited an anti-ferroptosis effect, which was reversed NRF2 inhibitor ML385. These findings indicate that EZH1 deficiency or inhibition with DS3201 alleviates ferroptosis in the liver by activating the NRF2, and it is suggested that targeting EZH1 may be a new therapeutic strategy in SALI.

34

项与 Valemetostat Tosilate 相关的新闻（医药）

2025-06-10

·PRNewswire

Foresight Diagnostics and Partners to Present Independent Validation Data for its CLARITY™ MRD Assay at the 2025 European Hematology Association (EHA) Congress and International Conference on Malignant Lymphoma (ICML)

- Data will be presented as an oral presentation at EHA on Thursday, June 12, 2025, and at ICML on Thursday, June 19, 2025 BOULDER, Colo., June 10, 2025 /PRNewswire/ -- Foresight Diagnostics, a leading developer of ultra-sensitive minimal residual disease (MRD) detection technologies, today announced that validation data demonstrating the prognostic performance of its CLARITY™ MRD assay in patients with newly diagnosed diffuse large B-cell lymphoma (DLBCL) will be featured as encore oral presentations at two upcoming international conferences: the 2025 European Hematology Association (EHA) Congress (June 12–15, in Milan, Italy) and the 18th International Conference on Malignant Lymphoma (ICML) (June 17–21, in Lugano, Switzerland). This multi-center study, conducted in collaboration with Amsterdam University Medical Centers, the Hemato-Oncology Foundation for Adults in the Netherlands (HOVON), and the Netherlands Comprehensive Cancer Organization (IKNL), highlights real-world results using Foresight CLARITY™ MRD on patients who were treated with frontline chemotherapy across over 50 centers in the Netherlands and Belgium. "We're grateful to present our data at major medical meetings this spring, validating our science and the real-world utility of ultra-sensitive ctDNA-MRD technology," said David Kurtz, M.D., Ph.D., Chief Medical Officer of Foresight Diagnostics. "These presentations and the recent incorporation of ctDNA-MRD testing in B-cell lymphoma clinical guidelines give us confidence as we prepare to launch in the clinical market in 2026 and integrate Foresight CLARITY into routine clinical practice." Lead study authors Steven Wang, M.D., and Martine Chamuleau, M.D., Ph.D., Amsterdam UMC, added: "Our findings confirm that ultra-sensitive ctDNA-MRD detection provides meaningful prognostic information beyond standard imaging and clinical factors. We believe this assay can support better risk stratification than imaging alone and inform post-treatment management decisions in DLBCL." Oral presentation details for EHA: Title: Prospective validation of end of treatment ctDNA-MRD by PhasED-Seq in DLBCL patients from a national trial Presenter: Martine Chamuleau, MD, PhD (Amsterdam UMC) Session: Aggressive Non-Hodgkin lymphoma - Clinical (Observational) Time: Thursday, June 12 | 5:00 p.m. – 5:15 p.m. CEST / 11:00 a.m. – 11:15 a.m. ET Room: Brown Hall 3 Abstract number: S240 Oral presentation details for ICML: Title: Prospective validation of end of treatment ctDNA-MRD by PhasED-Seq in DLBCL patients from a national HOVON trial Presenter: Martine Chamuleau, MD, PhD (Amsterdam UMC) Session: Session 6: Liquid biopsy for response assessment Time: Thursday, June 19 | 2:15 p.m. – 2:30 p.m. CEST / 8:15 a.m. – 8:30 a.m. ET Room: Polivalente room, East Campus USI Article number: 041 In addition to the oral presentation, Foresight's technology will be highlighted in other presentations, including: Title: Prognostic Value of Circulating Tumor DNA (ctDNA) Detection by PhasED-Seq After Axicabtagene ciloleucel (Axi-cel) Therapy in Relapsed/Refractory Large B-Cell Lymphoma (LBCL) Meeting: EHA 2025 Sponsor: Kite Pharma Presenter: Jeffrey Gregg, MD (Foresight Diagnostics) Session: Poster Session I | Poster Hall Date/Time: Friday, June 13 | 6:30 p.m. – 7:30 p.m. CEST / 12:30 p.m. – 1:30 p.m. ET Abstract: #PF1002 Title: The Correlation of Mutational Profiles and Valemetostat Efficacy in Patients With R/R PTCL in the Phase 2 VALENTINE-PTCL01 Trial Meeting: ICML 2025 Sponsor: Daiichi Sankyo Presenter: Pier Luigi Zinzani, MD, PhD (University of Bologna) Session: "Focus On" Session Biology and Therapy of T-cell Lymphomas | Room B Date/Time: Saturday, June 14 | 10:05 a.m. – 10:15 a.m. CEST / 4:05 a.m. – 4:15 a.m. ET Article Number: 164 About Foresight Diagnostics Foresight Diagnostics is a privately held cancer diagnostics company and CLIA-registered laboratory. Its liquid biopsy platform, Foresight CLARITY™, is a novel assay that measures minimal residual disease (MRD) with reported detection limits in parts per million. The improved sensitivity of Foresight CLARITY™ has the potential to provide actionable information to physicians and biopharmaceutical companies to enable personalized treatment approaches for patients with solid tumor and hematologic malignancies. For more information, please visit foresight-dx.com and follow us on X, LinkedIn, and Bluesky. SOURCE Foresight Diagnostics, Inc. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

临床2期

2025-05-20

·第一三共中国

第一三共在中国启动Valemetostat Tosylate与DXd ADC联合治疗实体瘤的1b期研究

2025年5月20日，一项valemetostat tosylate与DXd ADC 联合治疗选定实体瘤受试者的1b期研究成功完成中国首例受试者给药！第一三共诚挚感谢研究中心和相关部门所做出的一切努力并期待与各方通力合作，持续推进第一三共早期研发全球化，加速创新药物开发，满足未竟医疗需求！　　　　　关于研究　　　　　　　本研究是一项评价valemetostat tosylate 联合DXd（有效载荷，依喜替康衍生物）ADC（抗体偶联药物）的Ib 期、全球、多中心、开放性的2 部分研究。主方案研究设计包含独立的子方案，这些子方案根据所联合的药物和受试者人群进行定义，包括valemetostat tosylate联合德曲妥珠单抗（T-DXd）治疗无法切除和/或转移性人表皮生长因子2（HER2）低表达乳腺癌受试者，valemetostat tosylate联合T-DXd 治疗晚期或转移性HER2 阳性胃或胃食管交界处腺癌受试者及valemetostat tosylate联合datopotamab deruxtecan（Dato-DXd）治疗局部晚期/无法切除或转移性非鳞状非小细胞肺癌受试者。　　本研究分为两个部分，第1部分剂量递增阶段和第2部分剂量扩展阶段。本研究将同时开始每个子方案的第1 部分剂量递增阶段，以评估valemetostat tosylate联合T-DXd 治疗以及valemetostat tosylate联合Dato-DXd 治疗的安全性，直至确定valemetostat tosylate联合DXd ADC 的扩展期推荐剂量。对于每个子方案的第2 部分剂量扩展阶段，将进一步评价valemetostat tosylate联合DXd ADC 治疗在选定实体瘤中的安全性和有效性。　　表观遗传靶向药物已在多种血液恶性肿瘤中表现出临床活性。考虑到实体瘤的多样性，目前认为癌细胞利用表观遗传调节作用来激活与癌细胞存活相关的细胞通路（耐药性和免疫监视），且表观遗传治疗能够靶向和修饰这些癌症基因组功能，因此极具前景。然而，由于表观遗传学单药治疗实体瘤的疗效较为有限，因此这类药物的临床研究越来越多地集中在与细胞毒化疗、激素疗法和免疫检查点抑制剂的联合治疗方法上1。抗体偶联药物（ADC）已被证实在多种肿瘤类型中的疗效优于标准化疗药物2。因此，第一三共基于初步但具有前景的非临床数据设计了本信号探索研究。　更多研究相关信息，可登陆ClinicalTrials.gov及 http://www.chinadrugtrials.org.cn/index.html 网站查询。关于Valemetostat Tosylate　　Valemetostat tosylate是一种新型特异性小分子EZH1和EZH2双重抑制剂，目前正在开发用作口服抗肿瘤药物，可作为单药治疗或与其他药物联用。　　Valemetostat tosylate已于2022年9月26日在日本获批（EZHARMIA®）用于治疗复发/难治性成人T细胞白血病/淋巴瘤，2024年6月24日在日本获批用于治疗复发/难治性外周T细胞淋巴瘤。在中国，valemetostat tosylate尚未获批任何适应症。其在实体瘤中的安全性和疗效尚在探索中。　　　关于EZH1/EZH2　　　　　增强子zeste同源物1/2（EZH1和EZH2）为组蛋白甲基转移酶，可特异性催化组蛋白H3第二十七位赖氨酸残基K27（H3K27）甲基化，并通过形成多梳蛋白抑制复合物2（PRC2）而发挥甲基转移酶活性。由于H3K27三甲基化（H3K27me3）可表观调节基因表达，进而导致PRC2-EZH2失调，因此其可能会通过抑制肿瘤抑制基因或细胞分化基因而在肿瘤进展中发挥重要作用。　　此外，由于EZH1可部分补偿EZH2的损失，因此对EZH2的单一抑制作用可能不足以抑制肿瘤进展。但阻断EZH2活性可能会互补地诱导EZH1活化，进而有可能重新激活PRC2功能。因此，在阻断PRC2抑制肿瘤进展的功能方面，EZH1和EZH2双重抑制可能比单独抑制EZH2更有效。　　　　关于第一三共　　　　　　第一三共是一家为社会可持续发展做贡献的创新型全球医疗保健公司，致力于发现、开发和提供新的标准疗法，以提高世界各地患者的生活质量。第一三共专注制药行业120余年，凭借其世界一流的科学和技术，为癌症、心血管疾病和其他医疗需求远未得到满足的疾病患者研发新的治疗方法和创新药物。如欲了解更多信息，请访问www.daiichisankyo.com。参考文献：1.Jin N, George T, Otterson G, et al. Advances in epigenetic therapeutics with focus on solid tumors. Clin Epigenet. 2021; 13-83.2.Nasiri H, Valedkarimi Z, Aghebati-Maleki L, et al. Antibody-drug conjugates: promising and efficient tools for targeted cancer therapy. J Cell Physiol. 2018; 233(9):6441-57. doi:10.1002/jcp.26435.

抗体药物偶联物免疫疗法细胞疗法

2025-02-27

·生物世界

Cancer Cell：抑制EZH1/EZH2，增强CAR-T及TCR-T对多种癌症的疗效

撰文丨王聪编辑丨王多鱼排版丨水成文近年来，嵌合抗原受体 T 细胞疗法（CAR-T）和T细胞受体工程化 T 细胞疗法（TCR-T）等过继细胞免疫疗法（ACT）展现了强大的抗肿瘤效果，然而，耐药性是它们临床应用中面临的主要挑战。 2025 年 2 月 20 日，宾夕法尼亚大学的研究人员在 Cancer Cell 期刊发表了题为：EZH1/EZH2 inhibition enhances adoptive T cell immunotherapy against multiple cancer models 的研究论文。该研究揭示了 EZH1/EZH2 抑制剂通过表观遗传重编程，增强过继 T 细胞疗法（CAR-T 和 TCR-T）的抗肿瘤效果。在这项新研究中，研究团队认为，抑制肿瘤驱动基因的甲基转移酶 EZH2 和 EZH1 可以通过将癌细胞重塑为更具免疫原性的状态，从而增强过继细胞免疫疗法（ACT）效果。研究团队发现，在人 B 细胞淋巴瘤中，EZH2 抑制剂（tazemetostat）通过增强抗 CD19 CAR-T 细胞的活化、扩增和肿瘤浸润来提高其疗效。在机制上，tazemetostat 治疗的肿瘤显示出与黏附、B 细胞活化和炎症反应相关的基因上调，并增加了对 CAR-T 细胞的亲和力。此外，tazemetostat 还改善了 CAR-T 细胞和 TCR-T 细胞对多种血液类肿瘤（骨髓瘤、急性髓系白血病）和实体瘤（肉瘤、卵巢癌、前列腺癌）的疗效。研究团队进一步发现，使用 valemetostat 同时抑制 EZH1 和 EZH2，比单一抑制 EZH2 的效果更强，能够进一步增强 CAR-T 在多种癌症中的疗效和持续扩增。该研究的核心发现：抑制 EZH1/2 可增强 CAR-T 和 TCR-T 细胞在多种肿瘤模型中的疗效；抑制 EZH1/2 将癌细胞重塑为更具有免疫原性的状态；抑制肿瘤 EZH1/EZH2 可增强 CAR-T 细胞的活化、扩增和浸润。总的来说，该研究表明，在血液类肿瘤和实体癌的临床前模型中，抑制 EZH1/2，可将肿瘤重编程至更具免疫原性的状态，并优化 T 细胞功能，从而增强 CAR-T 和 TCR-T 细胞疗法的效果。 EZH1/2 抑制剂通过“双管齐下”策略——增强肿瘤免疫原性并优化 T 细胞功能，为过继性细胞疗法提供了强效增效手段，对于 CAR-T 细胞治疗后的复发的血液类肿瘤患者，以及 CAR-T 细胞疗法效果不佳的实体瘤患者，EZH1/2 抑制剂与过继细胞免疫疗法联合，可能是一种有效策略。论文链接： https://www.cell.com/cancer-cell/abstract/S1535-6108(25)00031-5 设置星标，不错过精彩推文开放转载欢迎转发到朋友圈和微信群微信加群为促进前沿研究的传播和交流，我们组建了多个专业交流群，长按下方二维码，即可添加小编微信进群，由于申请人数较多，添加微信时请备注：学校/专业/姓名，如果是PI/教授，还请注明。点在看，传递你的品味

细胞疗法免疫疗法临床结果

100 项与 Valemetostat Tosilate 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11551 D16662	-	-	-

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
成人T细胞白血病/淋巴瘤	日本	Daiichi Sankyo Co., Ltd.	2022-09-26
外周T细胞淋巴瘤	日本	Daiichi Sankyo Co., Ltd.	2022-09-26

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
转移性非小细胞肺癌	临床2期	美国	Daiichi Sankyo Co., Ltd.	2024-10-30
转移性非小细胞肺癌	临床2期	中国	Daiichi Sankyo Co., Ltd.	2024-10-30
转移性非小细胞肺癌	临床2期	日本	Daiichi Sankyo Co., Ltd.	2024-10-30
转移性非小细胞肺癌	临床2期	阿根廷	Daiichi Sankyo Co., Ltd.	2024-10-30
转移性非小细胞肺癌	临床2期	巴西	Daiichi Sankyo Co., Ltd.	2024-10-30
鳞状非小细胞肺癌	临床2期	美国	Daiichi Sankyo Co., Ltd.	2024-10-30
鳞状非小细胞肺癌	临床2期	中国	Daiichi Sankyo Co., Ltd.	2024-10-30
鳞状非小细胞肺癌	临床2期	日本	Daiichi Sankyo Co., Ltd.	2024-10-30
鳞状非小细胞肺癌	临床2期	阿根廷	Daiichi Sankyo Co., Ltd.	2024-10-30
鳞状非小细胞肺癌	临床2期	巴西	Daiichi Sankyo Co., Ltd.	2024-10-30

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临床结果

适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


JPRN-jRCT2031190268 (NCCH1904, ASCO2025)	临床1期	实体瘤 INI1-negative	30	Valemetostat tosylate (DS-3201b) 150 mg/1.7 m^2	窪範鏇夢鹽餘選簾夢鏇(鬱淵積襯壓鑰選壓觸糧) = One patient with NB developed acute lymphocytic leukemia as a secondary malignancy 願繭鏇願窪遞艱積壓窪 (網繭艱餘簾顧窪觸廠簾 ) 更多	积极	2025-05-30
JPRN-jRCT2031190268 (NCCH1904, ASCO2025)	临床1期	实体瘤 INI1-negative	30	Valemetostat tosylate (DS-3201b) 200 mg/1.7 m^2		积极	2025-05-30
NCT04703192 (VALENTINE-PTCL01, Pubmed \| Lancet Oncol)	临床2期	外周T细胞淋巴瘤	-	Valemetostat tosylate (valemetostat) 200 mg per day	淵壓襯膚糧膚夢築襯鹽(製鹽製壓艱夢鬱製廠願) = 繭廠鹹糧鑰鹹糧觸築觸廠簾願獵繭鑰築願構壓 (餘餘淵膚窪窪構積鬱鬱, 35 ~ 53)	积极	2024-12-01
NCT04703192 (VALENTINE-PTCL01, CTgov)	临床2期	成人T细胞白血病/淋巴瘤 \| 外周T细胞淋巴瘤 \| 成人T细胞淋巴瘤/难治性白血病	155	Valemetostat Tosylate	齋繭夢築積選獵齋蓋窪 = 顧蓋願蓋膚齋膚窪衊夢鏇夢簾獵艱憲壓範齋壓 (鹽鏇淵簾範製淵壓鑰願, 窪網壓窪淵壓獵艱構製 ~ 簾積獵窪觸遞艱觸鹽窪) 更多	-	2024-07-22
NCT02732275 (DS3201-A-J101, EHA2024) 人工标引	临床1期	非霍奇金淋巴瘤 EZH2 mutation	90	valemetostat tosylate 150-300 mg/d	艱淵鑰製窪鏇蓋夢簾選(憲醖蓋獵鹹夢夢顧衊遞) = 網衊觸鬱築積鹽襯顧鹽範艱繭醖窪繭觸鬱積築 (選餘襯艱觸顧衊淵築憲 ) 更多	积极	2024-05-14
NCT02732275 (DS3201-A-J101, EHA2024) 人工标引	临床1期	非霍奇金淋巴瘤 EZH2 mutation	90	valemetostat (ATLL)	鑰淵獵觸廠膚範製遞糧(醖鹽窪淵製窪窪衊構製) = 糧構繭製糧淵壓糧製積夢壓廠築簾獵顧夢範願 (醖製觸築齋製遞網餘繭, 1.4 ~ 38.7) 更多	积极	2024-05-14
NCT04703192 (VALENTINE-PTCL01, EHA2024) 人工标引	临床2期	外周T细胞淋巴瘤	119	Valemetostat tosylate 200 mg/day (pts with 1 prior LOT)	構廠製淵簾齋鑰壓獵網(築願顧製積餘鏇糧築餘) = 鑰獵鹽簾選範艱網夢蓋餘糧蓋窪繭醖衊願糧網 (夢遞膚觸範夢積壓襯製, 35.5 ~ 69.6)	积极	2024-05-14
NCT04703192 (VALENTINE-PTCL01, EHA2024) 人工标引	临床2期	外周T细胞淋巴瘤	119	Valemetostat tosylate 200 mg/day (pts with 2 prior LOT)	構廠製淵簾齋鑰壓獵網(築願顧製積餘鏇糧築餘) = 鬱糧鹽艱糧鏇鹹願衊夢餘糧蓋窪繭醖衊願糧網 (夢遞膚觸範夢積壓襯製, 28.3 ~ 65.7)	积极	2024-05-14
NCT03110354 (CTgov)	临床1期	急性髓性白血病 \| 急性淋巴细胞白血病	28	DS-3201b (DS-3201b 150 mg)	選窪獵製製構衊淵選襯 = 鏇鬱構艱觸遞構鹽窪獵鏇選襯蓋願衊顧選製憲 (鑰鬱餘艱廠鑰簾蓋膚鏇, 遞齋範鑰齋構蓋廠窪觸 ~ 網糧衊鏇願蓋壓壓獵構) 更多	-	2024-01-30
NCT03110354 (CTgov)	临床1期	急性髓性白血病 \| 急性淋巴细胞白血病	28	DS-3201b (DS-3201b 250 mg)	選窪獵製製構衊淵選襯 = 鬱夢遞壓築鏇齋鬱齋築鏇選襯蓋願衊顧選製憲 (鑰鬱餘艱廠鑰簾蓋膚鏇, 網獵選膚醖積壓鹽膚壓 ~ 糧衊膚醖壓鏇築淵廠憲) 更多	-	2024-01-30
ASH2023	临床1期	难治性B细胞淋巴瘤	19	Valemetostat	鹹鏇廠蓋鬱糧鹽醖醖鏇(遞遞積窪願顧淵夢簾鬱) = The most common TEAEs (any grade) were decreased platelet count (64%), dysgeusia (50%), anemia (43%), decreased neutrophil count (34%), and alopecia (33%) 願淵夢壓餘願憲製廠製 (淵觸醖膚齋築衊範製鹽 ) 更多	-	2023-12-09
ASH2023	临床1期	外周T细胞淋巴瘤	71	Valemetostat	廠夢製蓋糧壓鹽淵鬱積(築淵繭壓積壓願範糧願) = 範選齋窪襯窪齋遞襯餘鏇夢夢構繭鑰膚醖鹹憲 (願範鑰獵積網構觸獵積 ) 更多	-	2023-12-09
NCT04703192 \| NCT04102150 (VALENTINE-PTCL01, ASH2023)	临床2期	外周T细胞淋巴瘤	133	Valemetostat 200 mg/day	壓糧遞構蓋簾醖餘鑰憲(繭簾獵淵選鏇壓廠糧範) = 觸觸遞鹹範糧糧蓋餘壓築淵選憲醖鑰網製衊築 (簾艱鏇築淵壓鹹遞糧衊, 34.6 ~ 53.1) 更多	-	2023-12-09
NCT04102150 (VALENTINE-PTCL01, Pubmed) 人工标引	临床2期	成人T细胞白血病/淋巴瘤	25	Valemetostat Tosilate	襯積製夢選選壓廠範夢(窪網顧膚獵築醖淵餘網) = 糧網齋範淵築遞顧夢積顧糧鏇製鏇範鬱鑰選鏇 (鏇鏇築願繭構淵蓋齋鬱, 30.5 ~ 65.9) 更多	积极	2022-09-23