tazemetostat 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| enzyme inhibitors | 5380 | 1403254-99-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Tazemetostat is an inhibitor of the methyltransferase, EZH2, and some EZH2 gain-of-function mutations including Y646X and A687V. Tazemetostat also inhibited EZH1 with a half-maximal inhibitory concentration (IC50) of 392 nM, approximately 36 times higher than the IC50 for inhibition of EZH2
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 0.03 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 23, 2020 | FDA | EPIZYME INC | |
| June 23, 2021 | PMDA | EISAI Co., Ltd. |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01XX72 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Other antineoplastic agents |
| FDA MoA | N0000191423 | Multidrug and Toxin Extrusion Transporter 1 Inhibitors |
| FDA EPC | N0000193930 | Methyltransferase Inhibitor |
| FDA MoA | N0000193931 | Methyltransferase Inhibitors |
| FDA MoA | N0000193932 | Multidrug and Toxin Extrusion Transporter 2 K Inhibitors |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Follicular lymphoma | indication | 55150002 | |
| Epithelioid sarcoma | indication | 782827000 | DOID:6193 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 11.8 | acidic |
| pKa2 | 12.91 | acidic |
| pKa3 | 6.92 | Basic |
| pKa4 | 2.4 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 8691507 | Sept. 12, 2031 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA POSITIVE FOR AN ENHANCER OF ZESTE HOMOLOG 2 (EZH2) MUTATION |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 8895245 | Sept. 12, 2031 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA POSITIVE FOR AN ENHANCER OF ZESTE HOMOLOG 2 (EZH2) MUTATION |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 9175331 | Sept. 12, 2031 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA POSITIVE FOR AN ENHANCER OF ZESTE HOMOLOG 2 (EZH2) MUTATION |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 9333217 | Sept. 12, 2031 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA POSITIVE FOR AN ENHANCER OF ZESTE HOMOLOG 2 (EZH2) MUTATION |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 9334527 | Sept. 12, 2031 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA POSITIVE FOR AN ENHANCER OF ZESTE HOMOLOG 2 (EZH2) MUTATION |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 9949999 | Sept. 12, 2031 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA POSITIVE FOR AN ENHANCER OF ZESTE HOMOLOG 2 (EZH2) MUTATION BY INHIBITING EZH2 |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 10155002 | April 13, 2032 | METHOD OF TREATING EPITHELIOID SARCOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 10420775 | April 13, 2032 | METHOD OF TREATING EPITHELIOID SARCOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 10420775 | April 13, 2032 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 10420775 | April 13, 2032 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA POSITIVE FOR AN ENHANCER OF ZESTE HOMOLOG 2 (EZH2) MUTATION |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 11052093 | April 13, 2032 | METHOD OF TREATING EPITHELIOID SARCOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 11052093 | April 13, 2032 | METHOD OF TREATING FOLLICULAR LYMPHOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 8765732 | April 13, 2032 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 8765732 | April 13, 2032 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA POSITIVE FOR AN ENHANCER OF ZESTE HOMOLOG 2 (EZH2) MUTATION |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 9522152 | April 13, 2032 | METHOD OF TREATING A LUNG METASTASIS OF EPITHELIOID SARCOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 9549931 | April 13, 2032 | METHOD OF TREATING EPITHELIOID SARCOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 9549931 | April 13, 2032 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 9549931 | April 13, 2032 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA POSITIVE FOR AN ENHANCER OF ZESTE HOMOLOG 2 (EZH2) MUTATION |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 9855275 | April 13, 2032 | METHOD OF TREATING EPITHELIOID SARCOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 10245269 | April 11, 2033 | METHOD OF TREATING EPITHELIOID SARCOMA BY INHIBITING ENHANCER OF ZESTE HOMOLOG 2 (EZH2) |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 10245269 | April 11, 2033 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA BY INHIBITING EZH2 |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 10245269 | April 11, 2033 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA POSITIVE FOR AN ENHANCER OF ZESTE HOMOLOG 2 (EZH2) MUTATION BY INHIBITING EZH2 |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 11491163 | April 11, 2033 | METHOD OF TREATING LYMPHOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 11491163 | April 11, 2033 | METHOD OF TREATING SARCOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 9394283 | April 11, 2033 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 9394283 | April 11, 2033 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA POSITIVE FOR AN ENHANCER OF ZESTE HOMOLOG 2 (EZH2) MUTATION |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 9872862 | April 11, 2033 | METHOD OF TREATING A LUNG METASTASIS OF EPITHELIOID SARCOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 9688665 | Aug. 22, 2034 | METHOD OF TREATING EPITHELIOID SARCOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 10369155 | Oct. 16, 2035 | METHOD OF TREATING EPITHELIOID SARCOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 10369155 | Oct. 16, 2035 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 10369155 | Oct. 16, 2035 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA POSITIVE FOR AN ENHANCER OF ZESTE HOMOLOG 2 (EZH2) MUTATION |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 9889138 | Oct. 16, 2035 | METHOD OF TREATING EPITHELIOID SARCOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 9889138 | Oct. 16, 2035 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | 9889138 | Oct. 16, 2035 | METHOD OF TREATING RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA POSITIVE FOR AN ENHANCER OF ZESTE HOMOLOG 2 (EZH2) MUTATION |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | June 18, 2023 | TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY (R/R) FOLLICULAR LYMPHOMA (FL) WHO HAVE NO SATISFACTORY ALTERNATIVE TREATMENT OPTIONS |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | June 18, 2023 | TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY (R/R) FOLLICULAR LYMPHOMA (FL) WHOSE TUMORS ARE POSITIVE FOR AN EZH2 MUTATION AS DETECTED BY AN FDA-APPROVED TEST AND WHO HAVE RECEIVED AT LEAST 2 PRIOR SYSTEMIC THERAPIES |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | Jan. 23, 2025 | NEW CHEMICAL ENTITY |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | Jan. 23, 2027 | INDICATED FOR THE TREATMENT OF ADULTS AND PEDIATRIC PATIENTS AGED 16 YEARS AND OLDER WITH METASTATIC OR LOCALLY ADVANCED EPITHELIOID SARCOMA NOT ELIGIBLE FOR COMPLETE RESECTION |
| EQ 200MG BASE | TAZVERIK | EPIZYME INC | N211723 | Jan. 23, 2020 | RX | TABLET | ORAL | June 18, 2027 | INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA WHOSE TUMORS ARE POSITIVE FOR AN EZH2 MUTATION AS DETECTED BY AN FDA-APPROVED TEST AND WHO HAVE RECEIVED AT LEAST 2 PRIOR SYSTEMIC THERAPIES, AND FOR THE TREATMENT OF ADULT PATIENTS WITH RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA WHO HAVE NO SATISFACTORY ALTERNATIVE TREATMENT OPTIONS |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Histone-lysine N-methyltransferase EZH2 | Enzyme | INHIBITOR | IC50 | 7.96 | DRUG LABEL | DRUG LABEL | |||
| Polycomb protein EED | Unclassified | IC50 | 8.70 | CHEMBL | |||||
| Histone-lysine N-methyltransferase EZH1 | Enzyme | INHIBITOR | IC50 | 6.41 | DRUG LABEL | ||||
| Histone-lysine N-methyltransferase EZH2, EC 2.1.1.356 | Unclassified | IC50 | 8.40 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| Q40W93WPE1 | UNII |
| 1467052-75-0 | SECONDARY_CAS_RN |
| C4086895 | UMLSCUI |
| CHEMBL3414621 | ChEMBL_ID |
| 66558664 | PUBCHEM_CID |
| DB12887 | DRUGBANK_ID |
| CHEMBL4594260 | ChEMBL_ID |
| 9963 | INN_ID |
| D11444 | KEGG_DRUG |
| 7011 | IUPHAR_LIGAND_ID |
| 018265 | NDDF |
| 018266 | NDDF |
| 840405005 | SNOMEDCT_US |
| 840407002 | SNOMEDCT_US |
| 879948007 | SNOMEDCT_US |
| 4039121 | VANDF |
| 2274378 | RXNORM |
| 329834 | MMSL |
| 37975 | MMSL |
| d09497 | MMSL |
| C000593333 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| TAZVERIK | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72607-100 | TABLET, FILM COATED | 200 mg | ORAL | NDA | 27 sections |