Valemetostat Tosylate

DRUG13 trials

Sponsors

Daiichi Sankyo Inc., Celgene Corp., LYSARC, Institut Gustave Roussy, Daiichi Sankyo Co., Ltd.

Conditions

2-part study of valemetostat in combination with DXd ADCs. The Master Protocol study design contains independent subprotocolsARID1AARID1BAdult T Cell Leukemia/LymphomaAdult T-cell Leukemia/LymphomaAdult patients with histologically/cytologically confirmed progressive metastatic or recurrent solid tumorAdvanced Solid TumorAdvanced or Metastatic Non-Small Cell Lung Cancer

Phase 1

A Study of Valemetostat Tosylate in Combination With DXd ADCs in Subjects With Solid Tumors

RecruitingNCT06244485

Daiichi SankyoAdvanced Solid Tumor

Start: 2024-02-16End: 2028-11-01Target: 210Updated: 2026-02-04

A PHASE I/II, MULTI-CENTER, OPEN-LABEL STUDY TO ASSESS THE SAFETY, PHARMACOKINETICS, AND PRELIMINARY EFFICACY OF AN ORALLY AVAILABLE SMALL MOLECULE, CC-99282, ALONE AND IN COMBINATION WITH ANTI-LYMPHOMA AGENTS IN SUBJECTS WITH RELAPSED OR REFRACTORY NON-HODGKIN LYMPHOMAS (R/R NHL)

RecruitingCTIS2024-515690-10-00

Celgene Corp.Diffuse large B-cell lymphoma, Follicular B-cell non-Hodgkin's lymphoma, Mantle cell lymphoma +2

Start: 2019-05-10Target: 204Updated: 2025-11-12

A Study of Valemetostat Tosylate Plus Pembrolizumab Versus Pembrolizumab Alone in First-Line NSCLC Without Actionable Genomic Alterations

RecruitingNCT06644768

Daiichi SankyoLung Cancer, Non-small Cell Lung Cancer

Start: 2024-10-30End: 2030-04-30Target: 137Updated: 2025-10-09

A phase 1B, multicenter, open-label study of Valemetostat Tosylate in combination with DXd ADCs in subjects with solid tumors(study of Valemetostat Tosylate in combination with DXd ADCs)

SuspendedCTIS2024-516916-93-00

Daiichi Sankyo Inc.2-part study of valemetostat in combination with DXd ADCs. The Master Protocol study design contains independent subprotocols, advanced or metastatic HER2-positive gastric or GEJ adenocarcinoma; for details, as follows: Sub-protocol A: Valemetostat in combination with T-DXd in subjects with previously treated +12

Start: 2025-09-08Target: 45Updated: 2025-09-29

A Multicenter, Randomized, Open-Label, Phase 1b/2 Trial of Valemetostat Tosylate Plus Pembrolizumab vs Pembrolizumab Alone in Participants with Advanced or Metastatic Non-small Cell Lung Cancer whose Tumors Express PD-L1 with Tumor Proportion Score ≥50% Without Actionable Genomic Alterations

Not yet recruitingCTIS2024-519671-26-00

Daiichi Sankyo Inc.Advanced or Metastatic Non-Small Cell Lung Cancer

Target: 21Updated: 2025-12-22

Phase 2

Valemetostat Tosylate (DS-3201b) Phase 2 Study in Relapsed or Refractory Adult T-cell Leukemia/Lymphoma

CompletedNCT04102150

Daiichi Sankyo Co., Ltd.Adult T-cell Leukemia/Lymphoma

Start: 2019-11-21End: 2024-10-27Updated: 2025-02-10

Valemetostat Tosylate (DS-3201b), an Enhancer of Zeste Homolog (EZH) 1/2 Dual Inhibitor, for Relapsed/Refractory Peripheral T-Cell Lymphoma (VALENTINE-PTCL01)

Active, not recruitingNCT04703192

Daiichi SankyoAdult T Cell Leukemia/Lymphoma, Relapsed/Refractory Peripheral T-Cell Lymphoma

Start: 2021-06-03End: 2027-02-19Updated: 2025-12-09

Study of Valemetostat Tosylate as a Single Agent in Patients With Relapse/Refractory B-cell Lymphoma

Active, not recruitingNCT04842877

The Lymphoma Academic Research OrganisationLymphoma, B-Cell

Start: 2021-06-11End: 2026-10-01Target: 141Updated: 2026-02-19

Single-Arm, Phase 2 Study of Valemetostat Tosylate Monotherapy in Subjects with Relapsed/Refractory Peripheral T-Cell Lymphoma

Active, not recruitingCTIS2023-507381-13-00

Daiichi Sankyo Inc.Relapsed/Refractory Peripheral T-Cell Lymphoma

Start: 2021-11-03Target: 46Updated: 2026-01-20

VALYM - A phase II open-label study evaluating valemetostat tosylate as a single agent in patients with relapse/refractory B-cell lymphoma

RecruitingCTIS2024-516181-11-00

LYSARCRELAPSE/REFRACTORY B-CELL LYMPHOMA.

Start: 2021-06-10Target: 140Updated: 2025-12-15

Targeted Treatment for Metastatic Prostate Cancer, The PREDICT Trial

RecruitingNCT06632977

Alliance for Clinical Trials in OncologyCastration-Resistant Prostate Carcinoma, Stage IVB Prostate Cancer AJCC v8

Start: 2025-02-06End: 2034-10-11Target: 474Updated: 2026-03-04

An open label phase II platform modular study exploring the efficacy and safety of the Valemetostat (EZH1/2 inhibitor) in patients with selected solid tumors (EZHiSWITCH)

Not yet recruitingCTIS2024-519788-16-00

Institut Gustave RoussyAdult patients with histologically/cytologically confirmed progressive metastatic or recurrent solid tumor, ARID1A, ARID1B +7

Target: 600Updated: 2025-12-09

Efficacy and Safety of the Valemetostat in Patients With Selected Solid Tumors.

Not yet recruitingNCT07303387

Gustave Roussy, Cancer Campus, Grand ParisClear Cell Endometrial Carcinoma, Ovarian Cancer, Solid Tumor Malignancies

Start: 2026-02-28End: 2032-02-28Target: 900Updated: 2025-12-24

Related Papers

Clinical Utility of Transcriptomic Signatures to Identify Androgen Receptor and Neuroendocrine Signaling in Prostate Cancer.

2026-03-05

Valemetostat monotherapy in patients with relapsed or refractory B-cell lymphoma: Final results of the Phase 2 valym study from the lysa

Blood2025-11-03

Abstract P3-08-24: Valemetostat and Trastuzumab Deruxtecan in Patients With HER2-Low, Previously Treated, Unresectable or Metastatic Breast Cancer

Clinical Cancer Research2025-06-13

Precision diagnostics in prostate cancer treatment (PREDICT): A phase 2 multi-arm biomarker based study (Alliance A032102).

Journal of Clinical Oncology2025-05-28

Abstract 3790: Preclinical assessment of valemetostat, a dual inhibitor of EZH2 and EZH1, combined with trastuzumab deruxtecan and datopotamab deruxtecan for multiple solid tumors

Cancer Research2025-04-21

Valemetostat and trastuzumab deruxtecan (T-DXd) in previously treated advanced or metastatic human epidermal growth factor receptor 2 (HER2)-positive gastric cancer or gastro-esophageal junction (GEJ) adenocarcinoma.

Journal of Clinical Oncology2025-01-27

Prediction of Clinical Response By Phased Variants in Circulating Tumor DNA (ctDNA) in the VALENTINE-PTCL01 Trial of Patients with Relapsed or Refractory (R/R) Peripheral T-Cell Lymphoma (PTCL)

Blood2024-11-051 citations

Valemetostat Monotherapy in Patients with Relapsed or Refractory Large B-Cell Lymphoma: Primary Results of the Phase 2 Valym Study from the Lysa

Blood2024-11-05

Valemetostat for patients with relapsed or refractory peripheral T-cell lymphoma (VALENTINE-PTCL01): a multicentre, open-label, single-arm, phase 2 study.

2024-10-2933 citations

A phase 1b, multicenter, open-label study of valemetostat in combination with DXd antibody drug conjugates (ADCs), trastuzumab deruxtecan (T-DXd) or datopotamab deruxtecan (Dato-DXd), in patients with solid tumors.

Journal of Clinical Oncology2024-06-017 citations

Efficacy and Safety of Valemetostat Monotherapy in Patients with Relapsed or Refractory Peripheral T-Cell Lymphomas: Primary Results of the Phase 2 VALENTINE-PTCL01 Study

Blood2023-11-0217 citations

Valemetostat for Relapsed or Refractory B-Cell Lymphomas: Primary Results from a Phase 1 Trial

Blood2023-11-024 citations

Highly Sensitive Detection Method Reveals Significant Anti-Tumor Activity of Valemetostat in Patients with Relapsed/Refractory Adult T Cell Leukemia

Blood2022-11-15

An open-label, single-arm phase 2 trial of valemetostat for relapsed or refractory adult T-cell leukemia/lymphoma

Blood2022-09-23146 citations

A Global Phase 2 Study of Valemetostat Tosylate (Valemetostat) in Patients with Relapsed or Refractory (R/R) Peripheral T-Cell Lymphoma (PTCL), Including R/R Adult T-Cell Leukemia/Lymphoma (ATL) - Valentine-PTCL01

Blood2021-11-0521 citations

Pivotal Phase 2 Study of the EZH1 and EZH2 Inhibitor Valemetostat Tosylate (DS-3201b) in Patients with Relapsed or Refractory Adult T-Cell Leukemia/Lymphoma

Blood2021-11-056 citations

EZH1/2 Dual Inhibitor Valemetostat Tosylate (DS-3201b) Acts Differently from EZH2 Selective Inhibitor on Epigenetic Landscape to Exert Greater Anti-Tumor Effect Against Diffuse Large B-Cell Lymphoma

Blood2021-11-051 citations