tazemetostat
Trade name: Tazverik
Small moleculeapprovedOrphan Drug FDA
Approved
Jan 23, 2020
Tazemetostat (EPZ-6438) is a selective inhibitor of histone-lysine N-methyltransferase EZH2. The drug is under clinical development (phase II) for the treatment of Diffuse Large B Cell Lymphoma, Malignant Mesothelioma and Synovial Sarcoma. — NCATS
Clinical trial activity
56 trials · 44 clinical orgs · 1 marketing orgs
Phase 1
31
Phase 2
36
Phase 3
2
Phase 4
0
Earliest trial started Jun 1, 2013 (NCT01897571)
Timeline
2010s
- Jan 1, 2013
Epizyme, Inc. — Earliest Phase 1 Sponsor(trial)
- Jan 1, 2015
Epizyme, Inc. — Earliest Phase 2 Sponsor(trial)
- Jun 15, 2017
Orphan Drug Designation
- Jan 1, 2019
Epizyme, Inc. — Earliest Phase 3 Sponsor(trial)
2020s
- Jan 23, 2020
Epizyme, Inc. — Earliest FDA Approval
- Jan 23, 2020
Epizyme, Inc. — Marketing Organization
- Jan 23, 2020
Epizyme, Inc. — NDA Secondary Org
- Jan 23, 2020
Epizyme, Inc. — NDA Organization
Indications
Studied for
- Carcinoma · Phase 2
- Carcinoma, Hepatocellular · Phase 1
- Carcinoma, Non-Small-Cell Lung · Phase 1/Phase 2
- Carcinoma, Renal Cell · Phase 2
- Carcinoma, Transitional Cell · Phase 1/Phase 2
- Chordoma · Phase 2
- Colorectal Neoplasms · Phase 2
- COVID-19 · Phase 2
- Cytokine Release Syndrome · Phase 2
- Endometrial Neoplasms · Phase 2
- Enteropathy-Associated T-Cell Lymphoma · Phase 2
- Ependymoma · Phase 2
- Glioma · Phase 2
- Hematologic Neoplasms · Phase 1
- Hepatoblastoma · Phase 2
- Histiocytosis, Langerhans-Cell · Phase 2
- Hodgkin Disease · Phase 2
- Hydrolases · Phase 2
- Intestinal Neoplasms · Phase 2
- Kidney Diseases · Phase 2
- Kidney Neoplasms · Phase 1/Phase 2
- Leukemia, Myeloid, Acute · Phase 1
- Liver Diseases · Phase 1
- Lymphoma · Phase 2
- Lymphoma, B-Cell · Phase 2
- Lymphoma, B-Cell, Marginal Zone · Phase 1
- Lymphoma, Follicular · Phase 3
- Lymphoma, Large B-Cell, Diffuse · Phase 2
- Lymphoma, Large-Cell, Immunoblastic · Phase 1/Phase 2
- Lymphoma, Mantle-Cell · Phase 1
- Lymphoma, Non-Hodgkin · Phase 2
- Lymphoma, T-Cell · Phase 2
- Lymphoma, T-Cell, Peripheral · Phase 2
- Medulloblastoma · Phase 2
- Melanoma · Phase 1/Phase 2
- Mesothelioma · Phase 2
- Multiple Myeloma · Phase 1/Phase 2
- Mutation · Phase 2
- Neoplasm Metastasis · Phase 1/Phase 2
- Neoplasms · Phase 2
- Neoplasms, Germ Cell and Embryonal · Phase 2
- Nerve Sheath Neoplasms · Phase 2
- Neuroblastoma · Phase 2
- Neuroectodermal Tumors · Phase 2
- Osteosarcoma · Phase 2
- Ovarian Neoplasms · Phase 2
- Pancreatic Neoplasms · Phase 2
- Prostatic Neoplasms · Early Phase 1
- Prostatic Neoplasms, Castration-Resistant · Phase 1
- Rhabdoid Tumor · Phase 2
- Rhabdomyosarcoma · Phase 2
- Sarcoma · Phase 3
- Sarcoma, Ewing · Phase 2
- Sarcoma, Synovial · Phase 2
- Small Cell Lung Carcinoma · Phase 1
- Squamous Cell Carcinoma of Head and Neck · Phase 1/Phase 2
- Urinary Bladder Neoplasms · Phase 1/Phase 2
- Uterine Neoplasms · Phase 2
- Wilms Tumor · Phase 2
Mechanism of action
- EZH2/SUZ12/EED complexANTAGONIST
EZH2/SUZ12/EED complex antagonist
Histone-lysine N-methyltransferase EZH2 inhibitor
Inhibits some EZH2 mutants including Y646X and A687V and inhibits EZH1 at an IC50 of 392 nM (36 x higher than for EZH2).
Approval history
- approvedPriority reviewAcceleratedJan 23, 2020
Chemistry & pharmacology
Loading structure…
SMILES
CCN(C1CCOCC1)C2=C(C)C(=CC(=C2)C3=CC=C(CN4CCOCC4)C=C3)C(=O)NCC5=C(C)C=C(C)NC5=O- Mol. weight
- 572.7376 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
First in class
Sources
- WikipediaTazemetostat ↗
- NCATSQ40W93WPE1 ↗
- ChEMBLCHEMBL4594260 ↗
- ChEMBLCHEMBL3414621 ↗
Also known as
- tazemetostat
- tazemetostat
- tazemetostat
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07209163 | Phase 1/Phase 2 (Phase 2) | Oct 31, 2025 | Jiao Tong University |
| NCT06692452 | Phase 2 | Apr 30, 2025 | Harvard University, Ipsen |
| NCT06824701 | Phase 1 | Mar 31, 2025 | Ipsen, University of Utah |
| NCT06575686 | Phase 2 | Nov 23, 2024 | City of Hope National Medical Center, National Cancer Institute (NCI) |
| NCT06242834 | Phase 2 | Sep 30, 2024 | National Cancer Institute (NCI), Northwestern University |
| NCT05983965 | Phase 1 | May 31, 2024 | University of Alabama, Birmingham |
| NCT06068881 | Phase 2 | Dec 13, 2023 | Epizyme, Inc., Ipsen |
| NCT05994235 | Phase 2 | Nov 1, 2023 | Cornell University, Epizyme, Inc., Genentech |
| NCT05934838 | Phase 1 | Oct 4, 2023 | American Society of Clinical Oncology, Cornell University, Epizyme, Inc. |
| NCT05890352 | Phase 2 | Sep 26, 2023 | BeOne Medicines, Incyte, Ipsen, National Cancer Institute (NCI), SWOG Cancer Research Network |
| NCT05551936 | Phase 1/Phase 2 (Phase 2) | May 31, 2023 | Big Ten Cancer Research Consortium, Epizyme, Inc., University of Wisconsin |
| NCT05713110 | Phase 2 | Feb 13, 2023 | Hutchison MediPharma, University of Washington |
| NCT05604417 | Phase 1/Phase 2 (Phase 2) | Jan 31, 2023 | Harvard University, MEI Pharma |
| NCT05467748 | Phase 1/Phase 2 (Phase 2) | Jan 2, 2023 | Department of Veteran Affairs |
| NCT05627232 | Phase 1 | Dec 31, 2022 | Thomas Jefferson University |
| NCT05618366 | Phase 1 | Dec 31, 2022 | Cornell University, Epizyme, Inc., Genentech |
| NCT05407441 | Phase 1/Phase 2 (Phase 2) | Dec 31, 2022 | Bristol-Myers Squibb, Epizyme, Inc., Harvard University |
| NCT05627245 | Phase 1 | Dec 9, 2022 | National Cancer Institute (NCI), Yale University |
| NCT05567679 | Early Phase 1 (Phase 1) | Nov 30, 2022 | Cedars-Sinai Medical Center, Epizyme, Inc. |
| NCT05372354 | Phase 1/Phase 2 (Phase 2) | Oct 31, 2022 | Bristol-Myers Squibb |
Showing 20 of 56 trials
Page 1 / 3
Organizations
Research & Development (44)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Epizyme, Inc. | For profit | 30 | 17 | 4 | 2013 |
| National Cancer Institute (NCI) | Government | 11 | 7 | 2 | 2017 |
| Ipsen | For profit | 5 | 0 | 3 | 2023 |
| Harvard University | Academic/Hospital | 4 | 4 | 2 | 2021 |
| Cornell University | Academic/Hospital | 3 | 3 | 2 | 2022 |
| Bristol-Myers Squibb | For profit | 2 | 1 | 1 | 2022 |
| City of Hope National Medical Center | Academic/Hospital | 2 | 2 | 1 | 2021 |
| Eisai | For profit | 2 | 2 | 2 | 2017 |
| Genentech | For profit | 2 | 0 | 2 | 2022 |
| Hutchison MediPharma | For profit | 2 | 1 | 1 | 2022 |
| Swedish Cancer Institute | Academic/Hospital | 2 | 0 | 1 | 2020 |
| University of Toronto | Academic/Hospital | 2 | 0 | 2 | 2018 |
| University of Washington | Academic/Hospital | 2 | 2 | 1 | 2020 |
| Yale University | Academic/Hospital | 2 | 0 | 2 | 2021 |
| American Society of Clinical Oncology | Academic/Hospital | 1 | 0 | 1 | 2023 |
| AstraZeneca | For profit | 1 | 0 | 1 | 2021 |
| BeOne Medicines | For profit | 1 | 0 | 1 | 2023 |
| Big Ten Cancer Research Consortium | Academic/Hospital | 1 | 1 | 1 | 2023 |
| Cedars-Sinai Medical Center | Academic/Hospital | 1 | 1 | 1 | 2022 |
| Department of Veteran Affairs | Government | 1 | 1 | 1 | 2023 |
44 organizations
Page 1 / 3
Marketing (3)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Epizyme, Inc. | For profit | MKTG | Jan 23, 2020 |
| Epizyme, Inc. | For profit | NDA2 | Jan 23, 2020 |
| Epizyme, Inc. | For profit | NDA | Jan 23, 2020 |