tazemetostat Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
enzyme inhibitors 5380 1403254-99-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tazemetostat
  • tazemetostat hydrobromide
  • tazverik
  • EPZ-6438
  • EZ438
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
  • Molecular weight: 572.75
  • Formula: C34H44N4O4
  • CLOGP: 3.38
  • LIPINSKI: 1
  • HAC: 8
  • HDO: 2
  • TPSA: 83.14
  • ALOGS: -4.79
  • ROTB: 9

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 23, 2020 FDA EPIZYME INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
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 (View source of the data)

DiseaseRelationSNOMED_IDDOID
Follicular lymphoma indication 55150002
Epithelioid sarcoma indication 782827000 DOID:6193

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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 ALTERNULLTIVE 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 ALTERNULLTIVE TREATMENT OPTIONS

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Histone-lysine N-methyltransferase EZH2 Enzyme INHIBITOR IC50 7.96 DRUG LABEL DRUG LABEL
Histone-lysine N-methyltransferase EZH1 Enzyme INHIBITOR IC50 6.41 DRUG LABEL

External reference:

IDSource
1467052-75-0 SECONDARY_CAS_RN
4039121 VANDF
C3827128 UMLSCUI
CHEMBL3414621 ChEMBL_ID
CHEMBL4594260 ChEMBL_ID
C000593333 MESH_SUPPLEMENTAL_RECORD_UI
D11444 KEGG_DRUG
66558664 PUBCHEM_CID
9963 INN_ID
DB12887 DRUGBANK_ID
Q40W93WPE1 UNII
7011 IUPHAR_LIGAND_ID
2274378 RXNORM
329834 MMSL
37975 MMSL
d09497 MMSL
018265 NDDF
018266 NDDF
840405005 SNOMEDCT_US
840407002 SNOMEDCT_US
879948007 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
TAZVERIK HUMAN PRESCRIPTION DRUG LABEL 1 72607-100 TABLET, FILM COATED 200 mg ORAL NDA 27 sections