valemetostat
Trade name: Ezharmia
Small moleculeexperimental
Clinical trial activity
18 trials · 10 clinical orgs · 0 marketing orgs
Phase 1
13
Phase 2
10
Phase 3
0
Phase 4
0
Earliest trial started Mar 1, 2016 (NCT02732275)
Timeline
Indications
Studied for
- Breast Neoplasms · Phase 1
- Carcinoma, Hepatocellular · Phase 1/Phase 2
- Carcinoma, Non-Small-Cell Lung · Phase 1/Phase 2
- Carcinoma, Renal Cell · Phase 1
- Carcinoma, Transitional Cell · Phase 1
- Head and Neck Neoplasms · Phase 1/Phase 2
- Leukemia-Lymphoma, Adult T-Cell · Phase 2
- Leukemia, Myeloid, Acute · Phase 1
- Liver Diseases · Phase 1
- Lung Neoplasms · Phase 1/Phase 2
- Lymphoma · Phase 1/Phase 2
- Lymphoma, B-Cell · Phase 2
- Lymphoma, Non-Hodgkin · Phase 1
- Lymphoma, T-Cell · Phase 2
- Neoplasms · Phase 1/Phase 2
- Precursor Cell Lymphoblastic Leukemia-Lymphoma · Phase 1
- Prostatic Neoplasms · Phase 1
- Prostatic Neoplasms, Castration-Resistant · Phase 2
- Small Cell Lung Carcinoma · Phase 1/Phase 2
- Squamous Cell Carcinoma of Head and Neck · Phase 1/Phase 2
Mechanism of action
EZH1 inhibitor
EZH2 inhibitor
Chemistry & pharmacology
Loading structure…
SMILES
Cc1cc(C)c(CNC(=O)c2cc(Cl)c3c(c2C)O[C@@](C)([C@H]2CC[C@H](N(C)C)CC2)O3)c(=O)[nH]1.Cc1ccc(S(=O)(=O)O)cc1- Mol. weight
- 660.23 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL4597193 ↗
- ChEMBLCHEMBL4594405 ↗
Also known as
- ds-3201b
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07303387 | Phase 2 | Feb 28, 2026 | Daiichi Sankyo, Institut Gustave Roussy |
| NCT07244341 | Phase 1 | Nov 20, 2025 | Bayer, Daiichi Sankyo |
| NCT06807632 | Phase 1 | Jan 29, 2025 | Daiichi Sankyo, Memorial Sloan-Kettering Cancer Center |
| NCT06294548 | Phase 1/Phase 2 (Phase 2) | Dec 31, 2024 | University of Alabama, Birmingham |
| NCT06644768 | Phase 1/Phase 2 (Phase 2) | Nov 1, 2024 | Daiichi Sankyo, Merck |
| NCT06632977 | Phase 2 | Oct 13, 2024 | National Cancer Institute (NCI) |
| NCT06244485 | Phase 1 | Feb 16, 2024 | Daiichi Sankyo |
| NCT05879484 | Phase 1/Phase 2 (Phase 2) | Jan 3, 2024 | National Cancer Institute (NCI) |
| NCT05633979 | Phase 1 | May 31, 2023 | Daiichi Sankyo, University of Texas at Houston |
| NCT05683171 | Phase 1/Phase 2 (Phase 2) | May 19, 2023 | Daiichi Sankyo, University of Texas at Houston |
| NCT04842877 | Phase 2 | Jun 11, 2021 | Daiichi Sankyo, The Lymphoma Academic Research Organisation, The Lymphoma Study Association |
| NCT04703192 | Phase 2 | Jun 3, 2021 | Daiichi Sankyo |
| NCT04388852 | Phase 1 | Jul 15, 2020 | National Cancer Institute (NCI), University of Texas at Houston |
| NCT04276662 | Phase 1 | Nov 26, 2019 | Daiichi Sankyo |
| NCT04102150 | Phase 2 | Oct 16, 2019 | Daiichi Sankyo |
| NCT03879798 | Phase 1/Phase 2 (Phase 2) | Mar 15, 2019 | Memorial Sloan-Kettering Cancer Center |
| NCT03110354 | Phase 1 | Mar 28, 2017 | Daiichi Sankyo |
| NCT02732275 | Phase 1 | Mar 1, 2016 | Daiichi Sankyo |
Showing 18 of 18 trials
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Organizations
Research & Development (10)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Daiichi Sankyo | For profit | 13 | 8 | 2 | 2016 |
| National Cancer Institute (NCI) | Government | 3 | 2 | 2 | 2020 |
| University of Texas at Houston | Academic/Hospital | 3 | 3 | 2 | 2020 |
| Memorial Sloan-Kettering Cancer Center | Academic/Hospital | 2 | 2 | 2 | 2019 |
| Bayer | For profit | 1 | 0 | 1 | 2025 |
| Institut Gustave Roussy | Academic/Hospital | 1 | 1 | 1 | 2026 |
| Merck | For profit | 1 | 0 | 1 | 2024 |
| The Lymphoma Academic Research Organisation | Academic/Hospital | 1 | 1 | 1 | 2021 |
| The Lymphoma Study Association | Academic/Hospital | 1 | 0 | 1 | 2021 |
| University of Alabama, Birmingham | Academic/Hospital | 1 | 1 | 1 | 2024 |
10 organizations
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