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Details

Stereochemistry ACHIRAL
Molecular Formula C34H44N4O4
Molecular Weight 572.7388
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TAZEMETOSTAT

SMILES

CCN(C1CCOCC1)c2cc(cc(c2C)C(=NCc3c(C)cc(C)nc3O)O)-c4ccc(cc4)CN5CCOCC5

InChI

InChIKey=NSQSAUGJQHDYNO-UHFFFAOYSA-N
InChI=1S/C34H44N4O4/c1-5-38(29-10-14-41-15-11-29)32-20-28(27-8-6-26(7-9-27)22-37-12-16-42-17-13-37)19-30(25(32)4)33(39)35-21-31-23(2)18-24(3)36-34(31)40/h6-9,18-20,29H,5,10-17,21-22H2,1-4H3,(H,35,39)(H,36,40)

HIDE SMILES / InChI
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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
2.5 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
818 ng/mL
800 mg 2 times / day steady-state, oral
dose: 800 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TAZEMETOSTAT unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
4630 ng × h/mL
800 mg 2 times / day steady-state, oral
dose: 800 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TAZEMETOSTAT unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
100 mg 2 times / day steady, oral
Studied dose
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, 38 - 70 years
n = 64
Health Status: unhealthy
Condition: B-cell non-Hodgkin lymphoma or Solid tumour
Age Group: 38 - 70 years
Sex: M+F
Population Size: 64
Sources:
DLT: Neutropenia, Thrombocytopenia...
Dose limiting toxicities:
Neutropenia (grade 4, 1 patient)
Thrombocytopenia (grade 4, 1 patient)
Alanine aminotransferase increased (grade 4)
Aspartate aminotransferase increase (grade 4)
Fatigue (grade 3)
Cardiotoxicity (grade 2)
Nausea (grade 3)
Vomiting (grade 3)
Diarrhoea (grade 3)
Sources:
1600 mg 2 times / day multiple, oral
Highest studied dose
Dose: 1600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1600 mg, 2 times / day
Sources: Page: 89
unhealthy, adult
n = 64
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 64
Sources: Page: 89
DLT: Thrombocytopenia...
Dose limiting toxicities:
Thrombocytopenia (grade 4, 2%)
Sources: Page: 89
1600 mg 2 times / day single, oral
Highest studied dose
Dose: 1600 mg, 2 times / day
Route: oral
Route: single
Dose: 1600 mg, 2 times / day
Sources:
unhealthy, adult
n = 1
Health Status: unhealthy
Condition: B-cell non-Hodgkin lymphoma or Solid tumour
Age Group: adult
Sex: unknown
Population Size: 1
Sources:
DLT: Thrombocytopenia...
Dose limiting toxicities:
Thrombocytopenia (grade 4, 1 patient)
Sources:
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: 6.1
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: 6.1
Disc. AE: Mood disorder NOS...
Other AEs: Decreased appetite...
AEs leading to
discontinuation/dose reduction:
Mood disorder NOS (2%)
Other AEs:
Decreased appetite (2%)
Sources: Page: 6.1
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Disc. AE: Mood disorder NOS...
Other AEs: Pain, Fatigue...
AEs leading to
discontinuation/dose reduction:
Mood disorder NOS (2%)
Other AEs:
Pain (all grades, 52%)
Fatigue (all grades, 47%)
Nausea (all grades, 36%)
Vomiting (all grades, 24%)
Constipation (all grades, 21%)
Diarrhea (all grades, 16%)
Abdominal pain (all grades, 13%)
Decreased appetite (all grades, 26%)
Cough (all grades, 18%)
Dyspnea (all grades, 16%)
Hemorrhage (all grades, 18%)
Headache (all grades, 18%)
Anemia (all grades, 16%)
Weight decreased (all grades, 16%)
Pain (grade 3-4, 7%)
Fatigue (grade 3-4, 1.6%)
Abdominal pain (grade 3-4, 1.6%)
Decreased appetite (grade 3-4, 4.8%)
Dyspnea (grade 3-4, 4.8%)
Hemorrhage (grade 3-4, 4.8%)
Anemia (grade 3-4, 13%)
Weight decreased (grade 3-4, 7%)
Sources: Page: Table 4
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Other AEs: Decreased hemoglobin, Lymphocyte count decreased...
Other AEs:
Decreased hemoglobin (all grades, 49%)
Lymphocyte count decreased (all grades, 36%)
White blood cell count decreased (all grades, 19%)
Triglyceride increased (all grades, 36%)
Glucose increased (all grades, 33%)
Sodium decreased (all grades, 30%)
Phosphate decreased (all grades, 28%)
Albumin decreased (all grades, 23%)
Alkaline phosphatase increased (all grades, 23%)
Potassium decreased (all grades, 20%)
Aspartate aminotransferase increased (all grades, 18%)
Calcium decreased (all grades, 16%)
Glucose decreased (all grades, 16%)
Partial thromboplastin time prolonged (all grades, 15%)
Alanine aminotransferase increased (all grades, 14%)
Creatinine increased (all grades, 12%)
Potassium increased (all grades, 12%)
Decreased hemoglobin (grade 3-4, 15%)
Lymphocyte count decreased (grade 3-4, 13%)
Triglyceride increased (grade 3-4, 3.3%)
Glucose increased (grade 3-4, 1.6%)
Sodium decreased (grade 3-4, 1.7%)
Phosphate decreased (grade 3-4, 1.7%)
Alkaline phosphatase increased (grade 3-4, 1.7%)
Potassium decreased (grade 3-4, 1.7%)
Aspartate aminotransferase increased (grade 3-4, 3.5%)
Partial thromboplastin time prolonged (grade 3-4, 5%)
Alanine aminotransferase increased (grade 3-4, 3.4%)
Sources: Page: Table 5
AEs

AEs

AESignificanceDosePopulation
Cardiotoxicity grade 2
DLT
100 mg 2 times / day steady, oral
Studied dose
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, 38 - 70 years
n = 64
Health Status: unhealthy
Condition: B-cell non-Hodgkin lymphoma or Solid tumour
Age Group: 38 - 70 years
Sex: M+F
Population Size: 64
Sources:
Diarrhoea grade 3
DLT
100 mg 2 times / day steady, oral
Studied dose
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, 38 - 70 years
n = 64
Health Status: unhealthy
Condition: B-cell non-Hodgkin lymphoma or Solid tumour
Age Group: 38 - 70 years
Sex: M+F
Population Size: 64
Sources:
Fatigue grade 3
DLT
100 mg 2 times / day steady, oral
Studied dose
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, 38 - 70 years
n = 64
Health Status: unhealthy
Condition: B-cell non-Hodgkin lymphoma or Solid tumour
Age Group: 38 - 70 years
Sex: M+F
Population Size: 64
Sources:
Nausea grade 3
DLT
100 mg 2 times / day steady, oral
Studied dose
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, 38 - 70 years
n = 64
Health Status: unhealthy
Condition: B-cell non-Hodgkin lymphoma or Solid tumour
Age Group: 38 - 70 years
Sex: M+F
Population Size: 64
Sources:
Vomiting grade 3
DLT
100 mg 2 times / day steady, oral
Studied dose
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, 38 - 70 years
n = 64
Health Status: unhealthy
Condition: B-cell non-Hodgkin lymphoma or Solid tumour
Age Group: 38 - 70 years
Sex: M+F
Population Size: 64
Sources:
Neutropenia grade 4, 1 patient
DLT
100 mg 2 times / day steady, oral
Studied dose
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, 38 - 70 years
n = 64
Health Status: unhealthy
Condition: B-cell non-Hodgkin lymphoma or Solid tumour
Age Group: 38 - 70 years
Sex: M+F
Population Size: 64
Sources:
Thrombocytopenia grade 4, 1 patient
DLT
100 mg 2 times / day steady, oral
Studied dose
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, 38 - 70 years
n = 64
Health Status: unhealthy
Condition: B-cell non-Hodgkin lymphoma or Solid tumour
Age Group: 38 - 70 years
Sex: M+F
Population Size: 64
Sources:
Alanine aminotransferase increased grade 4
DLT
100 mg 2 times / day steady, oral
Studied dose
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, 38 - 70 years
n = 64
Health Status: unhealthy
Condition: B-cell non-Hodgkin lymphoma or Solid tumour
Age Group: 38 - 70 years
Sex: M+F
Population Size: 64
Sources:
Aspartate aminotransferase increase grade 4
DLT
100 mg 2 times / day steady, oral
Studied dose
Dose: 100 mg, 2 times / day
Route: oral
Route: steady
Dose: 100 mg, 2 times / day
Sources:
unhealthy, 38 - 70 years
n = 64
Health Status: unhealthy
Condition: B-cell non-Hodgkin lymphoma or Solid tumour
Age Group: 38 - 70 years
Sex: M+F
Population Size: 64
Sources:
Thrombocytopenia grade 4, 2%
DLT
1600 mg 2 times / day multiple, oral
Highest studied dose
Dose: 1600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 1600 mg, 2 times / day
Sources: Page: 89
unhealthy, adult
n = 64
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 64
Sources: Page: 89
Thrombocytopenia grade 4, 1 patient
DLT
1600 mg 2 times / day single, oral
Highest studied dose
Dose: 1600 mg, 2 times / day
Route: oral
Route: single
Dose: 1600 mg, 2 times / day
Sources:
unhealthy, adult
n = 1
Health Status: unhealthy
Condition: B-cell non-Hodgkin lymphoma or Solid tumour
Age Group: adult
Sex: unknown
Population Size: 1
Sources:
Decreased appetite 2%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: 6.1
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: 6.1
Mood disorder NOS 2%
Disc. AE
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: 6.1
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: 6.1
Mood disorder NOS 2%
Disc. AE
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Abdominal pain all grades, 13%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Anemia all grades, 16%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Diarrhea all grades, 16%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Dyspnea all grades, 16%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Weight decreased all grades, 16%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Cough all grades, 18%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Headache all grades, 18%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Hemorrhage all grades, 18%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Constipation all grades, 21%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Vomiting all grades, 24%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Decreased appetite all grades, 26%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Nausea all grades, 36%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Fatigue all grades, 47%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Pain all grades, 52%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Abdominal pain grade 3-4, 1.6%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Fatigue grade 3-4, 1.6%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Anemia grade 3-4, 13%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Decreased appetite grade 3-4, 4.8%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Dyspnea grade 3-4, 4.8%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Hemorrhage grade 3-4, 4.8%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Pain grade 3-4, 7%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Weight decreased grade 3-4, 7%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 4
Creatinine increased all grades, 12%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Potassium increased all grades, 12%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Alanine aminotransferase increased all grades, 14%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Partial thromboplastin time prolonged all grades, 15%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Calcium decreased all grades, 16%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Glucose decreased all grades, 16%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Aspartate aminotransferase increased all grades, 18%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
White blood cell count decreased all grades, 19%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Potassium decreased all grades, 20%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Albumin decreased all grades, 23%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Alkaline phosphatase increased all grades, 23%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Phosphate decreased all grades, 28%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Sodium decreased all grades, 30%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Glucose increased all grades, 33%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Lymphocyte count decreased all grades, 36%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Triglyceride increased all grades, 36%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Decreased hemoglobin all grades, 49%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Glucose increased grade 3-4, 1.6%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Alkaline phosphatase increased grade 3-4, 1.7%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Phosphate decreased grade 3-4, 1.7%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Potassium decreased grade 3-4, 1.7%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Sodium decreased grade 3-4, 1.7%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Lymphocyte count decreased grade 3-4, 13%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Decreased hemoglobin grade 3-4, 15%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Triglyceride increased grade 3-4, 3.3%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Alanine aminotransferase increased grade 3-4, 3.4%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Aspartate aminotransferase increased grade 3-4, 3.5%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
Partial thromboplastin time prolonged grade 3-4, 5%
800 mg 2 times / day multiple, oral
Recommended
Dose: 800 mg, 2 times / day
Route: oral
Route: multiple
Dose: 800 mg, 2 times / day
Sources: Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources: Page: Table 5
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >10 uM]
no [IC50 >20 uM]
no [IC50 >20 uM]
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
weak
weak
weak
weak
weak
yes [IC50 1.27 uM]
yes (co-administration study)
Comment: Coadministration of tazemetostat 800 mg BID with an oral cocktail of repaglinide (a sensitive CYP2C8 substrate) and omeprazole (a sensitive CYP2C19 substrate) in patients increased repaglinide Cmax by 51% and AUClast by 80%; and decreased omeprazole Cmax by 18% and AUClast by 20%
Page: 87.0
yes [IC50 1.89 uM]
yes [IC50 12.1 uM]
yes [IC50 15 uM]
yes [IC50 2.65 uM]
yes [IC50 3.06 uM]
yes (co-administration study)
Comment: Coadministration of tazemetostat 800 mg BID with an oral cocktail of repaglinide (a sensitive CYP2C8 substrate) and omeprazole (a sensitive CYP2C19 substrate) in patients increased repaglinide Cmax by 51% and AUClast by 80%; and decreased omeprazole Cmax by 18% and AUClast by 20%
Page: 87.0
yes [IC50 4.79 uM]
yes [IC50 6.65 uM]
yes (co-administration study)
Comment: In patients with cancer, coadministration of tazemetostat 800 mg BID with single oral doses of repaglinide (0.25 mg, a sensitive CYP2C8 substrate) and omeprazole (20 mg, a sensitive CYP2C19 substrate) increased repaglinide Cmax by 50% and AUCinf by 80%,
Page: 87.0
yes [IC50 9.16 uM]
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
major
yes (co-administration study)
Comment: Coadministration of fluconazole (a moderate CYP3A inhibitor) with tazemetostat 400 mg twice daily increased tazemetostat steady-state AUClast in patients by 3.1-fold and Cmax by 2.3-fold.
Page: 78.0
no
no
no
no
no
no
yes
unlikely
Comment: Therefore, P-gp is expected to play a minor role in regulating tazemetostat absorption and the P-gp-mediated DDI risk at intestinal absorption is low for tazemetostat as a victim drug
Page: 97.0
Tox targets

Tox targets

Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2.
2013 May 7
Patents

Sample Use Guides

Malignant Mesothelioma, Synovial Sarcoma: patients receive 800 mg of oral tazemetostat two times daily. Diffuse Large B Cell Lymphoma: patients receive 200, 400, 600 or 800 mg of the drug twice a day in combination with rituximab (IV, 375 mg/m2, day 1),pPrednisolone (PO, 40 mg/m2 in the morning, day 1 to day 5), doxorubicine (IV, 50 mg/m2, day 1), cyclophosphamide (IV, 750 mg/m2, day 1), vincristine (IV, 1.4 mg/m2, day 1): 8 cycles, every 21 days.
Route of Administration: Oral
Treatment of WSU-DLCL2 with 1uM tazemetostat for 4 days resulted in a concentration-dependent reduction in global H3K27Me3 levels with an IC50 value of 9 nmol/L. Treatment of WSU-DLCL2 cells with 200 nM tazemetostat; KARPAS-422 with 100 nM; SU-DHL-6 with 200 nM; and Pfeiffer with 0.5 nM inhibited cell proliferation with IC50 values of 0.0086, 0.0018, 0.0047 and 0.00049 uM, respectively.
Name Type Language
TAZEMETOSTAT
WHO-DD  
USAN   INN  
Official Name English
TAZEMETOSTAT [USAN]
Common Name English
E-7438
Code English
EPZ-6438
Code English
TAZEMETOSTAT [INN]
Common Name English
TAZEMETOSTAT [WHO-DD]
Common Name English
N-((4,6-DIMETHYL-2-OXO-1,2-DIHYDROPYRIDIN-3-YL)METHYL)-5-(ETHYL(OXAN-4-YL)AMINO)-4-METHYL-4'-((MORPHOLIN-4-YL)METHYL)(1,1'-BIPHENYL)-3-CARBOXAMIDE
Systematic Name English
E7438
Code English
(1,1'-BIPHENYL)-3-CARBOXAMIDE, N-((1,2-DIHYDRO-4,6-DIMETHYL-2-OXO-3-PYRIDINYL)METHYL)-5-(ETHYL(TETRAHYDRO-2H-PYRAN-4-YL)AMINO)-4-METHYL-4'-(4-MORPHOLINYLMETHYL)-
Systematic Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 637118
Created by admin on Sat Jun 26 07:08:24 UTC 2021 , Edited by admin on Sat Jun 26 07:08:24 UTC 2021
FDA ORPHAN DRUG 508415
Created by admin on Sat Jun 26 07:08:24 UTC 2021 , Edited by admin on Sat Jun 26 07:08:24 UTC 2021
NCI_THESAURUS C274
Created by admin on Sat Jun 26 07:08:24 UTC 2021 , Edited by admin on Sat Jun 26 07:08:24 UTC 2021
EU-Orphan Drug EU/3/18/2004
Created by admin on Sat Jun 26 07:08:24 UTC 2021 , Edited by admin on Sat Jun 26 07:08:24 UTC 2021
FDA ORPHAN DRUG 544416
Created by admin on Sat Jun 26 07:08:24 UTC 2021 , Edited by admin on Sat Jun 26 07:08:24 UTC 2021
FDA ORPHAN DRUG 578417
Created by admin on Sat Jun 26 07:08:24 UTC 2021 , Edited by admin on Sat Jun 26 07:08:24 UTC 2021
FDA ORPHAN DRUG 607017
Created by admin on Sat Jun 26 07:08:24 UTC 2021 , Edited by admin on Sat Jun 26 07:08:24 UTC 2021
Code System Code Type Description
EVMPD
SUB178719
Created by admin on Sat Jun 26 07:08:24 UTC 2021 , Edited by admin on Sat Jun 26 07:08:24 UTC 2021
PRIMARY
DRUG BANK
DB12887
Created by admin on Sat Jun 26 07:08:24 UTC 2021 , Edited by admin on Sat Jun 26 07:08:24 UTC 2021
PRIMARY
FDA UNII
Q40W93WPE1
Created by admin on Sat Jun 26 07:08:24 UTC 2021 , Edited by admin on Sat Jun 26 07:08:24 UTC 2021
PRIMARY
PUBCHEM
66558664
Created by admin on Sat Jun 26 07:08:24 UTC 2021 , Edited by admin on Sat Jun 26 07:08:24 UTC 2021
PRIMARY
DRUG CENTRAL
5380
Created by admin on Sat Jun 26 07:08:24 UTC 2021 , Edited by admin on Sat Jun 26 07:08:24 UTC 2021
PRIMARY
CAS
1403254-99-8
Created by admin on Sat Jun 26 07:08:24 UTC 2021 , Edited by admin on Sat Jun 26 07:08:24 UTC 2021
PRIMARY
INN
9963
Created by admin on Sat Jun 26 07:08:24 UTC 2021 , Edited by admin on Sat Jun 26 07:08:24 UTC 2021
PRIMARY
NCI_THESAURUS
C107506
Created by admin on Sat Jun 26 07:08:24 UTC 2021 , Edited by admin on Sat Jun 26 07:08:24 UTC 2021
PRIMARY
RXCUI
2274378
Created by admin on Sat Jun 26 07:08:24 UTC 2021 , Edited by admin on Sat Jun 26 07:08:24 UTC 2021
PRIMARY