Drugs / Valemetostat
Valemetostat
also known as
Valemetostat tosylate · DS-3201 · DS-3201b · Valemetostat (DS-3201) · Valemetostat tosilate
Small molecule targets EZH1, EZH2 via inhibition
Trials 16
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 15 trials | ||||||
| Phase 1 | NCT07244341 | Dec 2025 → Jan 2028 expected | castration-resistant prostate carcinoma | Daiichi Sankyo | Recruiting | No outcome recorded |
| Phase 1 | NCT06807632 | Jan 2025 → Jan 2027 expected | small cell lung carcinoma | Memorial Sloan Kettering Cancer Center | Recruiting | No outcome recorded |
| Phase 1 | NCT06244485 | Feb 2024 → Nov 2028 expected | neoplasm | Daiichi Sankyo | Active not recruiting | No outcome recorded |
| Phase 1 | NCT05633979 | Feb 2023 → Dec 2030 expected | breast cancer | M.D. Anderson Cancer Center | Active not recruiting | No outcome recorded |
| Phase 1 | NCT04388852 | Aug 2020 → Dec 2026 expected | castration-resistant prostate carcinoma, clear cell renal carcinoma, metastatic malignant neoplasm, metastatic prostate carcinoma +1 | M.D. Anderson Cancer Center | Active not recruiting | No outcome recorded |
| Phase 1/25 trials | ||||||
| Phase 1/2 | NCT06294548 | Jul 2025 → Jan 2028 expected | hepatocellular carcinoma | University of Alabama at Birmingham | Recruiting | No outcome recorded |
| Phase 1/2 | NCT05879484 | Jul 2025 | head and neck squamous cell carcinoma, nasal cavity and paranasal sinus carcinoma, non-small cell squamous lung carcinoma | National Cancer Institute (NCI) | Withdrawn | No outcome recorded Stop: Enrollment |
| Phase 1/2 | NCT06644768 | Oct 2024 → Mar 2028 expected | non-small cell lung carcinoma | Daiichi Sankyo | Recruiting | No outcome recorded |
| Phase 1/2 | NCT05683171 | May 2023 → Sep 2027 expected | lymphoma | M.D. Anderson Cancer Center | Active not recruiting | No outcome recorded |
| Phase 1/2 | NCT03930953 | May 2019 → Apr 2027 expected | non-Hodgkin lymphoma | Celgene Corporation | Active not recruiting | No outcome recorded |
| Phase 25 trials · 1 met primary | ||||||
| Phase 2 | NCT07303387 | Mar 2026 → Feb 2031 expected | endometrial clear cell adenocarcinoma, ovarian cancer | Gustave Roussy, Cancer Campus, Grand Paris | Recruiting | No outcome recorded |
| Phase 2 | NCT06632977 | Feb 2025 → Apr 2030 expected | castration-resistant prostate carcinoma | Alliance for Clinical Trials in Oncology | Recruiting | No outcome recorded |
| Phase 2 | NCT04842877 | Jun 2021 → Dec 2024 overdue | B-cell non-Hodgkin lymphoma | The Lymphoma Academic Research Organisation | Active not recruiting | No outcome recorded |
| Phase 2 | NCT04703192 | Jun 2021 → May 2023 overdue | adult T-cell leukemia/lymphoma, peripheral T-cell lymphoma, not otherwise specified | Daiichi Sankyo | Active not recruiting | No outcome recorded |
| Phase 2 | NCT04102150 | Nov 2019 → Apr 2021 | adult T-cell leukemia/lymphoma | Daiichi Sankyo | Completed | Met primary |
| Phase not stated1 trial | ||||||
| — | NCT07862465 | — | adult T-cell leukemia/lymphoma, anaplastic large cell lymphoma, peripheral T-cell lymphoma, not otherwise specified | Daiichi Sankyo | Temporarily not available | No outcome recorded |
News releases announcing trial results or a regulatory action · 2
| Date | Issuer | Release |
|---|---|---|
| 2019-04-09 | Daiichi Sankyo | Regulatory Daiichi Sankyo’s EZH1/2 Dual Inhibitor Valemetostat (DS-3201) Receives SAKIGAKE Designation for Treatment of Patients with Relapsed/Refractory Peripheral T-Cell Lymphoma from Japan MHLW daiichisankyo.com ↗
Daiichi Sankyo’s EZH1/2 Dual Inhibitor Valemetostat (DS-3201) Receives SAKIGAKE Designation for Treatment of Patients with Relapsed/Refractory Peripheral T-Cell Lymphoma from Japan MHLW |
| 2017-12-12 | Daiichi Sankyo | Results Daiichi Sankyo Presents Phase 1 Data for EZH1/2 Dual Inhibitor DS-3201 in Patients with Non-Hodgkin Lymphomas at the 59th Annual Meeting of the American Society of Hematology daiichisankyo.com ↗
Preliminary exploratory efficacy results from phase 1 study show an overall response rate of 58.8 percent with single agent DS-3201, an investigational and potential first-in-class EZH1/2 dual inhibitor, in patients with relapsed or refractory non-Hodgkin lymphomas |
All press releases naming this drug 3 releases
Evidence & citations 11 cited values
Every value below carries the sentence it was read from. 19 sources stand behind the page.
| Field | Value | Cited text |
|---|---|---|
| Known as | valemetostat | “Valemetostat tosylate (valemetostat) is a potent, novel, dual inhibitor of EZH2 and EZH1.” PMID 39486433 ↗ Oct 2024 |
| Known as | DS-3201 | “Valemetostat (DS-3201) is an enhancer of zeste homolog 1 and 2 (EZH1/2) dual inhibitor that is actively being investigated in phase I and II trials for hematologic malignancies...” NCT05879484 ↗ |
| Known as | DS-3201b | “A Study of Valemetostat Tosylate (DS-3201b) With Atezolizumab and Bevacizumab in HCC” NCT06294548 ↗ |
| Known as | Valemetostat (DS-3201) | “Valemetostat (DS-3201)” NCT06294548 ↗ |
| Known as | Valemetostat tosilate | ChEMBL registry synonym — accepted as the source's own label CHEMBL4597193 ↗ |
| Known as | Valemetostat tosylate | “This trial will evaluate the safety and efficacy of valemetostat tosylate (DS-3201b) in combination with fixed-dose pembrolizumab versus pembrolizumab alone in participants...” NCT06644768 ↗5“Valemetostat tosylate (DS-3201b) is given continuously at 200 mg once daily (QD).” NCT04842877 ↗ “Drug: Valemetostat Tosylate” NCT04102150 ↗ “Drug: Valemetostat tosylate” NCT06244485 ↗ |
| Action | Inhibit | “a potent enhancer of zeste homolog 2 (EZH2) and EZH1 inhibitor” PMID 36150143 ↗ Mar 2023 |
| Modality | Small molecule | — CHEMBL4597193 ↗ |
| Route | Oral | “Patients received valemetostat 200 mg/day orally until progressive disease or unacceptable toxicity.” PMID 36150143 ↗ Mar 2023 |
| Target | EZH1 | “a potent enhancer of zeste homolog 2 (EZH2) and EZH1 inhibitor” PMID 36150143 ↗ Mar 2023 |
| Target | EZH2 | “a potent enhancer of zeste homolog 2 (EZH2) and EZH1 inhibitor” PMID 36150143 ↗ Mar 2023 |