U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
This repository is under review for potential modification in compliance with Administration directives.

Details

Stereochemistry ACHIRAL
Molecular Formula C34H44N4O4
Molecular Weight 572.7376
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TAZEMETOSTAT

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

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

Molecular Formula C34H44N4O4
Molecular Weight 572.7376
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
829 ng/mL
800 mg 2 times / day steady-state, oral
dose: 800 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TAZEMETOSTAT plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
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 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
3340 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 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
3.1 h
800 mg 2 times / day steady-state, oral
dose: 800 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TAZEMETOSTAT plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
12%
800 mg 2 times / day steady-state, oral
dose: 800 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
TAZEMETOSTAT plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
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
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
DLT: Thrombocytopenia...
Dose limiting toxicities:
Thrombocytopenia (grade 4, 2%)
Sources:
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
Health Status: unhealthy
Age Group: adult
Sex: unknown
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
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
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
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
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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:
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
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.
Substance Class Chemical
Created
by admin
on Mon Mar 31 22:45:15 GMT 2025
Edited
by admin
on Mon Mar 31 22:45:15 GMT 2025
Record UNII
Q40W93WPE1
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
EPZ-6438
Preferred Name English
TAZEMETOSTAT
WHO-DD  
USAN   INN  
Official Name English
EPZ6438
Code English
TAZEMETOSTAT [USAN]
Common Name English
E-7438
Code English
tazemetostat [INN]
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
Tazemetostat [WHO-DD]
Common Name English
TAZEMETOSTAT [MI]
Common 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 Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
FDA ORPHAN DRUG 607017
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
FDA ORPHAN DRUG 508415
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
NCI_THESAURUS C274
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
EU-Orphan Drug EU/3/18/2004
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
FDA ORPHAN DRUG 544416
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
FDA ORPHAN DRUG 578417
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
Code System Code Type Description
EVMPD
SUB178719
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
PRIMARY
DRUG BANK
DB12887
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
PRIMARY
FDA UNII
Q40W93WPE1
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
PRIMARY
EPA CompTox
DTXSID201025831
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
PRIMARY
PUBCHEM
66558664
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
PRIMARY
DRUG CENTRAL
5380
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
PRIMARY
CAS
1403254-99-8
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
PRIMARY
WIKIPEDIA
Tazemetostat
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
PRIMARY
USAN
FG-162
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
PRIMARY
MERCK INDEX
m12194
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
PRIMARY
INN
9963
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
PRIMARY
DAILYMED
Q40W93WPE1
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
PRIMARY
NCI_THESAURUS
C107506
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
PRIMARY
SMS_ID
100000164315
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
PRIMARY
RXCUI
2274378
Created by admin on Mon Mar 31 22:45:15 GMT 2025 , Edited by admin on Mon Mar 31 22:45:15 GMT 2025
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
biochemical assay
IC50
SALT/SOLVATE -> PARENT
BINDER->LIGAND
In vitro, tazemetostat is 87.7 to 91.1% bound to human plasma proteins over the concentration range of 1 to 30 ?M.
BINDING
TRANSPORTER -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
MAJOR
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
blood-to-plasma ratio PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC SINGLE ORAL DOSE ADMINISTRATION