U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C34H44N4O4.2BrH
Molecular Weight 734.561
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TAZEMETOSTAT DIHYDROBROMIDE

SMILES

Br.Br.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=OVLIOBIPPKJKHT-UHFFFAOYSA-N
InChI=1S/C34H44N4O4.2BrH/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);2*1H

HIDE SMILES / InChI
Molecular Formula BrH
Molecular Weight 80.912
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
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
742
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
 2.5 nM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Phase II
1132
Unknown

Approved Use

Unknown
Primary
Phase II
1132
Unknown

Approved Use

Unknown
Primary
Phase II
1132
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 unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
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 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:
https://pubmed.ncbi.nlm.nih.gov/29650362/
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:
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
Page: 89
unhealthy, adult
n = 64
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 64
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/211723Orig1s000MultidisciplineR.pdf
Page: 89
DLT: Thrombocytopenia...
Dose limiting toxicities:
Thrombocytopenia (grade 4, 2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/211723Orig1s000MultidisciplineR.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/29650362/
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:
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
Page: 6.1
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/29650362/
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:
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
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:
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
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:
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
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:
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
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:
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
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:
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
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:
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
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:
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
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:
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
Page: 89
unhealthy, adult
n = 64
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 64
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/211723Orig1s000MultidisciplineR.pdf
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:
https://pubmed.ncbi.nlm.nih.gov/29650362/
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:
https://pubmed.ncbi.nlm.nih.gov/29650362/
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
Page: 6.1
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: 6.1
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 4
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
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:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
unhealthy, adult
n = 62
Health Status: unhealthy
Condition: epithelioid sarcoma
Age Group: adult
Sex: unknown
Population Size: 62
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/211723s000lbl.pdf
Page: Table 5
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1737

inhibitor
1587
inhibitor
1767

inducer
389
inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP2C8
911

CYP2C19
1478

CYP1A2
1524

CYP2B6
810

MATE1
306

MATE2
263

P-gp
1461

BCRP
699

OATP1B1
788

OATP1B3
706

OCT1
512

OCT2
647

OAT1
599

OAT3
642

BSEP
402
CYP3A
191

P-gp
1537

BCRP
561

OCT2
355

OAT3
339

MATE1
135

OATP1B1
406

OATP1B3
350
CYP3A
129

CYP1A2
701

CYP2B6
547

CYP2C8
168

CYP2C19
293
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
BCRP
773
 no [IC50 >10 uM]
BCRP
773
 no [IC50 >10 uM]
EPZ-6930
5
BSEP
403
 no [IC50 >10 uM]
BSEP
403
 no [IC50 >10 uM]
EPZ-6930
5
OAT1
603
 no [IC50 >10 uM]
OAT1
603
 no [IC50 >10 uM]
EPZ-6930
5
OAT3
644
 no [IC50 >10 uM]
OAT3
644
 no [IC50 >10 uM]
EPZ-6930
5
OATP1B1
803
 no [IC50 >10 uM]
OATP1B1
803
 no [IC50 >10 uM]
EPZ-6930
5
OATP1B3
715
 no [IC50 >10 uM]
OATP1B3
715
 no [IC50 >10 uM]
EPZ-6930
5
OCT1
543
 no [IC50 >10 uM]
OCT1
543
 no [IC50 >10 uM]
EPZ-6930
5
OCT2
648
 no [IC50 >10 uM]
OCT2
648
 no [IC50 >10 uM]
EPZ-6930
5
P-gp
1650
 no [IC50 >10 uM]
P-gp
1650
 no [IC50 >10 uM]
EPZ-6930
5
CYP1A2
1692
 no [IC50 >20 uM]
CYP2B6
1001
 no [IC50 >20 uM]
CYP1A2
1692
 no
EPZ-6930
5
CYP1A2
1692
 no
EPZ006931
5
CYP1A2
1692
 no
EPZ034163
5
CYP2B6
1001
 no
EPZ-6930
5
CYP2B6
1001
 no
EPZ006931
5
CYP2B6
1001
 no
EPZ034163
5
CYP2C19
1553
 no
EPZ-6930
5
CYP2C19
1553
 no
EPZ006931
5
CYP2C19
1553
 no
EPZ034163
5
CYP2C8
965
 no
EPZ-6930
5
CYP2C8
965
 no
EPZ006931
5
CYP2C8
965
 no
EPZ034163
5
CYP2C9
1819
 no
EPZ-6930
5
CYP2C9
1819
 no
EPZ006931
5
CYP2C9
1819
 no
EPZ034163
5
CYP2D6
1891
 no
EPZ-6930
5
CYP2D6
1891
 no
EPZ006931
5
CYP2D6
1891
 no
EPZ034163
5
CYP3A4
1925
 no
EPZ-6930
5
CYP3A4
1925
 no
EPZ006931
5
CYP3A4
1925
 no
EPZ034163
5
CYP1A2
1692
 weak
CYP2B6
1001
 weak
CYP2C19
1553
 weak
CYP2C8
965
 weak
CYP2C9
1819
 weak
CYP2C8
965
 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
263
 yes [IC50 1.89 uM]
MATE2
263
 yes [IC50 12.1 uM]
EPZ-6930
5
CYP2C9
1819
 yes [IC50 15 uM]
MATE1
308
 yes [IC50 2.65 uM]
CYP3A4
1925
 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
308
 yes [IC50 4.79 uM]
EPZ-6930
5
CYP2C19
1553
 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
1891
 yes [IC50 9.16 uM]
CYP3A
298
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP3A4
1737
 major
CYP3A
191
 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
561
 no
MATE1
135
 no
OAT3
339
 no
OATP1B1
406
 no
OATP1B3
350
 no
OCT2
355
 no
P-gp
1537
 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
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
AK Scientific, Inc. (AKSCI)
2399AH
http://www.aksci.com/item_detail.php?cat=2399AH
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
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
BOC Sciences
1403254-99-8
https://www.bocsci.com/epz-6438-cas-1403254-99-8-item-84-462339.html
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
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
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
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
abcr GmbH
AB479418
http://www.abcr.com/shop/en/AB479418
eNovation Chemicals
Y0975468
https://www.enovationchem.com/ProductDetails.asp?ProductID=Y0975468
iChemical
EBD2207002
http://www.ichemical.com/products/1403254-99-8.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
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 Sat Dec 16 07:15:37 GMT 2023
Edited
by admin
on Sat Dec 16 07:15:37 GMT 2023
Record UNII
X536WKK41G
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
TAZEMETOSTAT DIHYDROBROMIDE
Common Name 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)-, HYDROBROMIDE (1:2)
Systematic Name English
EPZ-6438 DIHYDROBROMIDE
Code English
Code System Code Type Description
FDA UNII
X536WKK41G
Created by admin on Sat Dec 16 07:15:37 GMT 2023 , Edited by admin on Sat Dec 16 07:15:37 GMT 2023
PRIMARY
PUBCHEM
91617646
Created by admin on Sat Dec 16 07:15:37 GMT 2023 , Edited by admin on Sat Dec 16 07:15:37 GMT 2023
PRIMARY
CAS
1467052-83-0
Created by admin on Sat Dec 16 07:15:37 GMT 2023 , Edited by admin on Sat Dec 16 07:15:37 GMT 2023
PRIMARY
CAS
1467052-77-2
Created by admin on Sat Dec 16 07:15:37 GMT 2023 , Edited by admin on Sat Dec 16 07:15:37 GMT 2023
NON-SPECIFIC STOICHIOMETRY
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Structure of TAZEMETOSTAT
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