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

Description

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.

Originator

Approval Year

2020
691
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8504
 2.5 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Phase II
1147
Unknown

Approved Use

Unknown
Primary
Phase II
1147
Unknown

Approved Use

Unknown
Primary
Phase II
1147
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
818 ng/mL
REVIEW
https://patents.google.com/patent/WO2017079757A1
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
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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
REVIEW
https://patents.google.com/patent/WO2017079757A1
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
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/29650362/
unhealthy, 38 - 70 years
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/29650362/
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:
https://pubmed.ncbi.nlm.nih.gov/29650362/
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/211723Orig1s000MultidisciplineR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/211723Orig1s000MultidisciplineR.pdf
DLT: Thrombocytopenia...
Dose limiting toxicities:
Thrombocytopenia (grade 4, 2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/211723Orig1s000MultidisciplineR.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/29650362/
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://pubmed.ncbi.nlm.nih.gov/29650362/
DLT: Thrombocytopenia...
Dose limiting toxicities:
Thrombocytopenia (grade 4, 1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/29650362/
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/29650362/
unhealthy, 38 - 70 years
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/29650362/
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:
https://pubmed.ncbi.nlm.nih.gov/29650362/
unhealthy, 38 - 70 years
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/29650362/
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:
https://pubmed.ncbi.nlm.nih.gov/29650362/
unhealthy, 38 - 70 years
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/29650362/
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:
https://pubmed.ncbi.nlm.nih.gov/29650362/
unhealthy, 38 - 70 years
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/29650362/
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:
https://pubmed.ncbi.nlm.nih.gov/29650362/
unhealthy, 38 - 70 years
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/29650362/
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:
https://pubmed.ncbi.nlm.nih.gov/29650362/
unhealthy, 38 - 70 years
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/29650362/
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:
https://pubmed.ncbi.nlm.nih.gov/29650362/
unhealthy, 38 - 70 years
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/29650362/
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:
https://pubmed.ncbi.nlm.nih.gov/29650362/
unhealthy, 38 - 70 years
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/29650362/
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:
https://pubmed.ncbi.nlm.nih.gov/29650362/
unhealthy, 38 - 70 years
Health Status: unhealthy
Age Group: 38 - 70 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/29650362/
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:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/211723Orig1s000MultidisciplineR.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/211723Orig1s000MultidisciplineR.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/29650362/
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://pubmed.ncbi.nlm.nih.gov/29650362/
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1946

inhibitor
2252
inhibitor
2438

inducer
440
inhibitor
2507
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP2C8
1057

CYP2C19
2057

CYP1A2
2153

CYP2B6
926

MATE1
415

MATE2
267

P-gp
1741

BCRP
910

OATP1B1
1079

OATP1B3
961

OCT1
620

OCT2
779

OAT1
725

OAT3
747

BSEP
550
CYP3A
220

P-gp
2052

BCRP
697

OCT2
434

OAT3
391

MATE1
182

OATP1B1
503

OATP1B3
435
CYP3A
142

CYP1A2
832

CYP2B6
669

CYP2C8
198

CYP2C19
329
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
BCRP
985
 no [IC50 >10 uM]
BCRP
985
 no [IC50 >10 uM]
EPZ-6930
5
BSEP
554
 no [IC50 >10 uM]
BSEP
554
 no [IC50 >10 uM]
EPZ-6930
5
OAT1
730
 no [IC50 >10 uM]
OAT1
730
 no [IC50 >10 uM]
EPZ-6930
5
OAT3
749
 no [IC50 >10 uM]
OAT3
749
 no [IC50 >10 uM]
EPZ-6930
5
OATP1B1
1095
 no [IC50 >10 uM]
OATP1B1
1095
 no [IC50 >10 uM]
EPZ-6930
5
OATP1B3
970
 no [IC50 >10 uM]
OATP1B3
970
 no [IC50 >10 uM]
EPZ-6930
5
OCT1
656
 no [IC50 >10 uM]
OCT1
656
 no [IC50 >10 uM]
EPZ-6930
5
OCT2
782
 no [IC50 >10 uM]
OCT2
782
 no [IC50 >10 uM]
EPZ-6930
5
P-gp
1932
 no [IC50 >10 uM]
P-gp
1932
 no [IC50 >10 uM]
EPZ-6930
5
CYP1A2
2333
 no [IC50 >20 uM]
CYP2B6
1160
 no [IC50 >20 uM]
CYP1A2
2333
 no
EPZ-6930
5
CYP1A2
2333
 no
EPZ006931
5
CYP1A2
2333
 no
EPZ034163
5
CYP2B6
1160
 no
EPZ-6930
5
CYP2B6
1160
 no
EPZ006931
5
CYP2B6
1160
 no
EPZ034163
5
CYP2C19
2141
 no
EPZ-6930
5
CYP2C19
2141
 no
EPZ006931
5
CYP2C19
2141
 no
EPZ034163
5
CYP2C8
1117
 no
EPZ-6930
5
CYP2C8
1117
 no
EPZ006931
5
CYP2C8
1117
 no
EPZ034163
5
CYP2C9
2497
 no
EPZ-6930
5
CYP2C9
2497
 no
EPZ006931
5
CYP2C9
2497
 no
EPZ034163
5
CYP2D6
2546
 no
EPZ-6930
5
CYP2D6
2546
 no
EPZ006931
5
CYP2D6
2546
 no
EPZ034163
5
CYP3A4
2633
 no
EPZ-6930
5
CYP3A4
2633
 no
EPZ006931
5
CYP3A4
2633
 no
EPZ034163
5
CYP1A2
2333
 weak
CYP2B6
1160
 weak
CYP2C19
2141
 weak
CYP2C8
1117
 weak
CYP2C9
2497
 weak
CYP2C8
1117
 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
MATE2
267
 yes [IC50 1.89 uM]
MATE2
267
 yes [IC50 12.1 uM]
EPZ-6930
5
CYP2C9
2497
 yes [IC50 15 uM]
MATE1
416
 yes [IC50 2.65 uM]
CYP3A4
2633
 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
MATE1
416
 yes [IC50 4.79 uM]
EPZ-6930
5
CYP2C19
2141
 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
CYP2D6
2546
 yes [IC50 9.16 uM]
CYP3A
317
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP3A4
1946
 major
CYP3A
220
 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
BCRP
697
 no
MATE1
182
 no
OAT3
391
 no
OATP1B1
503
 no
OATP1B3
435
 no
OCT2
434
 no
P-gp
2052
 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

TargetModalityActivityMetaboliteClinical evidence
hERG
2263
Sourcing

Sourcing

Vendor/AggregatorIDURL
abcr GmbH
AB479418
http://www.abcr.com/shop/en/AB479418
AbMole Bioscience
M2677
http://www.abmole.com/products/epz-6438.html
Achemtek
0102-012746
http://www.achemtek.com/1403254-99-8
Acorn PharmaTech
ACN-029397
http://www.acornpharmatech.com/
Active Biopharma
ABP001111
http://www.activebiopharma.com/1403254-99-8
Adooq BioScience
A12712
https://www.adooq.com/epz-6438.html
AK Scientific, Inc. (AKSCI)
2399AH
http://www.aksci.com/item_detail.php?cat=2399AH
Ambinter
Amb24059721
http://www.ambinter.com/reference/24059721
Angene
AGN-PC-0WH9N3
http://www.angenechemical.com/productshow/AGN-PC-0WH9N3.html
ApexBio Technology
A8221
http://www.apexbt.com/epz-6438.html
Ark Pharm
AK317596
http://www.arkpharminc.com/products/1403254-99-8.html
Ark Pharma Scientific Limited
A-1248
http://www.arkpharmtech.com/product/33199.html
Aurora Fine Chemicals LLC
K16.667.108
http://online.aurorafinechemicals.com/info?ID=K16.667.108
Axon MedChem
2227
https://www.axonmedchem.com/product/2227
BioChemPartner
BCP07409
http://www.biochempartner.com/1403254-99-8-BCP07409
BioCrick
BCC3634
http://www.biocrick.com/EPZ-6438-BCC3634.html
BioSynth
J-690163
https://www.biosynth.com/en/products/all-products/products/J-690184.html
BioSynth
J-690164
https://www.biosynth.com/en/products/all-products/products/J-690185.html
BOC Sciences
1403254-99-8
https://www.bocsci.com/epz-6438-cas-1403254-99-8-item-84-462339.html
Boerchem
BC600303
http://www.boerchem.com/?product_43138.html
Chem Scene
CS-1758
http://www.chemscene.com/1403254-99-8.html
ChemieTek
CT-EPZ438
http://www.chemietek.com/epz-6438-details.aspx
Chemspace
CSSB00015190551
https://chem-space.com/CSSB00015190551
Clearsynth
CS-T-92516
https://www.clearsynth.com/en/CST92516.html
DC Chemicals
DC7122
http://www.dcchemicals.com/product_show-Tazemetostat_EPZ_6438_.html
Debye Scientific
DA-34776
http://www.debyesci.com/cas_1403254-99-8.html
eNovation Chemicals
Y0975468
https://www.enovationchem.com/ProductDetails.asp?ProductID=Y0975468
Excenen
EX-A509
http://www.excenen.com/searchresultlist.php?id=1403254-99-8
Finetech
FT-0700193
http://www.finetechnology-ind.com/prod/detail/pub/1403254-99-8.html
iChemical
EBD2207002
http://www.ichemical.com/products/1403254-99-8.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
Lab Network
LN01297365
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01297365
Matrix Scientific
147189
https://www.matrixscientific.com/147189.html
MedChem Express
HY-13803
https://www.medchemexpress.com/EPZ-6438.html
Smolecule
S544620
http://www.smolecule.com/products/s544620
Synblock Inc
SB22955
http://www.synblock.com/product/1403254-99-8.html
THE BioTek
bt-283516
https://www.thebiotek.com/product/inhibitors/bt-283516
PubMed

PubMed

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

Patents

08410088
7
08765732
10

Sample Use Guides

In Vivo Use Guide
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
In Vitro Use Guide
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
HISTONE-LYSINE N-METHYLTRANSFERASE EZH2
TARGET -> INHIBITOR
biochemical assay
IC50
Structure of TAZEMETOSTAT HYDROBROMIDE
SALT/SOLVATE -> PARENT
PLASMA PROTEIN FRACTION (HUMAN)
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
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> SUBSTRATE
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
MAJOR
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
Structure of N-((1,2-DIHYDRO-4,6-DIMETHYL-2-OXO-3-PYRIDINYL)METHYL)-4-METHYL-4'-(4-MORPHOLINYLMETHYL)-5-((TETRAHYDRO-2H-PYRAN-4-YL)AMINO)(1,1'-BIPHENYL)-3-CARBOXAMIDE
METABOLITE INACTIVE -> PARENT
MAJOR
Structure of 3-AMINO-N-((4,6-DIMETHYL-2-OXO-1H-PYRIDIN-3-YL)METHYL)-2-METHYL-5-(4-(MORPHOLINOMETHYL)PHENYL)BENZAMIDE
METABOLITE -> PARENT
Structure of N-((1,2-DIHYDRO-4,6-DIMETHYL-2-OXO-3-PYRIDINYL)METHYL)-5-(ETHYLAMINO)-4-METHYL-4'-(4-MORPHOLINYLMETHYL)(1,1'-BIPHENYL)-3-CARBOXAMIDE
METABOLITE -> PARENT
Related Record Type Details
Structure of TAZEMETOSTAT
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

NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966