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

Details

Stereochemistry ACHIRAL
Molecular Formula C27H36N6O3S
Molecular Weight 524.678
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of FEDRATINIB

SMILES

CC1=CN=C(NC2=CC=C(OCCN3CCCC3)C=C2)N=C1NC4=CC=CC(=C4)S(=O)(=O)NC(C)(C)C

InChI

InChIKey=JOOXLOJCABQBSG-UHFFFAOYSA-N
InChI=1S/C27H36N6O3S/c1-20-19-28-26(30-21-10-12-23(13-11-21)36-17-16-33-14-5-6-15-33)31-25(20)29-22-8-7-9-24(18-22)37(34,35)32-27(2,3)4/h7-13,18-19,32H,5-6,14-17H2,1-4H3,(H2,28,29,30,31)

HIDE SMILES / InChI
Molecular Formula C27H36N6O3S
Molecular Weight 524.678
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/26181658 | http://adisinsight.springer.com/drugs/800027763

Fedratinib (SAR-302503, TG-101348) is a selective small-molecule inhibitor of Janus kinase-2. Fedratinib demonstrated therapeutic efficacy in a murine model of myeloproliferative disease. Sanofi was developing Fedratinib for the treatment of myeloproliferative diseases and solid tumors. The clinical development of fedratinib was terminated after reports of Wernicke's encephalopathy in myelofibrosis patients.

CNS Activity

CNS Active
3913
Curator's Comment: The clinical development of fedratinib, a Janus kinase (JAK2) inhibitor, was terminated after reports of Wernicke's encephalopathy in myelofibrosis patients.

Originator

Approval Year

2019
334
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
 3.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Phase II
1132
Unknown

Approved Use

Unknown
Primary
Phase II
1132
Unknown

Approved Use

Unknown
Primary
Phase I
428
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1804 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
FEDRATINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
2539 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
500 mg 1 times / day steady-state, oral
dose: 500 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
FEDRATINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
1760 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24165976
680 mg single, oral
dose: 680 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
FEDRATINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
26870 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
FEDRATINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
38712 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
500 mg 1 times / day steady-state, oral
dose: 500 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
FEDRATINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
17800 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24165976
680 mg single, oral
dose: 680 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
FEDRATINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
41 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
FEDRATINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
62.1 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/24165976
680 mg single, oral
dose: 680 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
FEDRATINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
8%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
400 mg 1 times / day steady-state, oral
dose: 400 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
FEDRATINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
2%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
500 mg 1 times / day steady-state, oral
dose: 500 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
FEDRATINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
8%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
FEDRATINIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
Disc. AE: Nausea, Cardiac failure...
Other AEs: Diarrhea, Nausea...
AEs leading to
discontinuation/dose reduction:
Nausea (>3)
Cardiac failure (grade 3-4, 3%)
Cardiac failure (grade 5, 1%)
Thrombocytopenia (2%)
Myocardial ischemia (2%)
Diarrhea (2%)
Blood creatinine increased (2%)
Other AEs:
Diarrhea (>3)
Nausea (>3)
Anemia (6%)
Diarrhea (3%)
Vomiting (3%)
Thrombocytopenia (2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
Other AEs: Diarrhea, Nausea...
Other AEs:
Diarrhea (all grades, 66%)
Nausea (all grades, 62%)
Anemia (all grades, 40%)
Vomiting (all grades, 39%)
Asthenia (all grades, 19%)
Muscle spasms (all grades, 12%)
Blood creatinine increased (all grades, 10%)
Pain in extremity (all grades, 10%)
Alanine aminotransferase increased (all grades, 9%)
Headache (all grades, 9%)
Weight increased (all grades, 9%)
Dizziness (all grades, 8%)
Bone pain (all grades, 8%)
Urinary tract infection (all grades, 6%)
Dysuria (all grades, 6%)
Aspartate aminotransferase increased (all grades, 5%)
Diarrhea (grade 3-4, 5%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
Other AEs: Anemia, Vomiting...
Other AEs:
Anemia (grade 3-4, 30%)
Vomiting (grade 3-4, 3.1%)
Asthenia (grade 3-4, 5%)
Blood creatinine increased (grade 3-4, 1%)
Thrombocytopenia (all grades, 47%)
Neutropenia (all grades, 23%)
Lipase increased (all grades, 35%)
Hyponatremia (all grades, 26%)
Amylase increased (all grades, 24%)
Thrombocytopenia (grade 3-4, 12%)
Neutropenia (grade 3-4, 5%)
Lipase increased (grade 3-4, 10%)
Hyponatremia (grade 3-4, 5%)
Amylase increased (grade 3-4, 2.1%)
Cardiac failure (all grades, 5%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Sex: M+F
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Disc. AE: Anemia...
AEs leading to
discontinuation/dose reduction:
Anemia (1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Page: 123
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Sex: M+F
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Page: 123
Disc. AE: Cardiac disorders...
AEs leading to
discontinuation/dose reduction:
Cardiac disorders (grade 5, 2 patients)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Page: 123
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Disc. AE: Thrombocytopenia, Neutropenia...
AEs leading to
discontinuation/dose reduction:
Thrombocytopenia (6%)
Neutropenia (2%)
Vomiting (4%)
Blood creatinine increased (2%)
Diarrhea (2%)
Nausea (2%)
Amylase increased (1%)
Lipase increased (3%)
Fatigue (2%)
Diarrhea (all grades, 8%)
Diarrhea (grade 3-4, 3%)
Nausea (all grades, 6%)
Nausea (grade 3-4, 4%)
Vomiting (all grades, 11%)
Vomiting (grade 3-4, 7%)
Anemia (all grades, 18%)
Anemia (grade 3-4, 14%)
Thrombocytopenia (all grades, 7%)
Thrombocytopenia (grade 3-4, 6%)
Fatigue (all grades, 5%)
Fatigue (grade 3-4, 5%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
400 mg 1 times / day multiple, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 years (range: 27 - 86 years)
n = 96
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Disc. AE: Anemia, Diarrhea...
AEs leading to
discontinuation/dose reduction:
Anemia (2%)
Diarrhea (2%)
Nausea (2%)
Amylase increased (1%)
Lipase increased (1%)
Vomiting (all grades, 10%)
Vomiting (grade 3-4, 3%)
Anemia (all grades, 8%)
Anemia (grade 3-4, 5%)
Thrombocytopenia (all grades, 3%)
Thrombocytopenia (grade 3-4, 2%)
Fatigue (all grades, 3%)
Fatigue (grade 3-4, 3%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
400 mg 1 times / day multiple, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Page: 123
unhealthy, 65 years (range: 27 - 86 years)
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Page: 123
Disc. AE: Cardiac disorders...
AEs leading to
discontinuation/dose reduction:
Cardiac disorders (grade 5, 2 patients)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Page: 123
800 mg single, oral
Highest studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Page: 20
unhealthy, adult
n = 1
Health Status: unhealthy
Condition: myelofibrosis
Age Group: adult
Sex: unknown
Population Size: 1
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Page: 20
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Page: 20
680 mg 1 times / day multiple, oral
MTD
Dose: 680 mg, 1 times / day
Route: oral
Route: multiple
Dose: 680 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Page: 68
unhealthy, adult
n = 31
Health Status: unhealthy
Condition: myelofibrosis
Age Group: adult
Sex: unknown
Population Size: 31
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Page: 68
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Page: 68
680 mg single, oral
MTD
Dose: 680 mg
Route: oral
Route: single
Dose: 680 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/24165976/
healthy, adult
n = 2
Health Status: healthy
Age Group: adult
Sex: M
Population Size: 2
Sources:
https://pubmed.ncbi.nlm.nih.gov/24165976/
Other AEs: Gastrointestinal disorders...
Other AEs:
Gastrointestinal disorders
Sources:
https://pubmed.ncbi.nlm.nih.gov/24165976/
800 mg 1 times / day multiple, oral
Highest studied dose
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy
n = 6
Health Status: unhealthy
Population Size: 6
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
AEs

AEs

AESignificanceDosePopulation
Thrombocytopenia 2%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
Blood creatinine increased 2%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
Diarrhea 2%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
Myocardial ischemia 2%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
Thrombocytopenia 2%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
Diarrhea 3%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
Vomiting 3%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
Anemia 6%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
Diarrhea >3
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
Nausea >3
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
Nausea >3
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
Cardiac failure grade 3-4, 3%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
Cardiac failure grade 5, 1%
Disc. AE
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: 6.1
Blood creatinine increased all grades, 10%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
Pain in extremity all grades, 10%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
Muscle spasms all grades, 12%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
Asthenia all grades, 19%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
Vomiting all grades, 39%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
Anemia all grades, 40%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
Aspartate aminotransferase increased all grades, 5%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
Dysuria all grades, 6%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
Urinary tract infection all grades, 6%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
Nausea all grades, 62%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
Diarrhea all grades, 66%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
Bone pain all grades, 8%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
Dizziness all grades, 8%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
Alanine aminotransferase increased all grades, 9%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
Headache all grades, 9%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
Weight increased all grades, 9%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
Diarrhea grade 3-4, 5%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 3
Neutropenia all grades, 23%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
Amylase increased all grades, 24%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
Hyponatremia all grades, 26%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
Lipase increased all grades, 35%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
Thrombocytopenia all grades, 47%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
Cardiac failure all grades, 5%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
Blood creatinine increased grade 3-4, 1%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
Lipase increased grade 3-4, 10%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
Thrombocytopenia grade 3-4, 12%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
Amylase increased grade 3-4, 2.1%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
Vomiting grade 3-4, 3.1%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
Anemia grade 3-4, 30%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
Asthenia grade 3-4, 5%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
Hyponatremia grade 3-4, 5%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
Neutropenia grade 3-4, 5%
400 mg 1 times / day steady, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: steady
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
unhealthy, 27 - 86 years
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 27 - 86 years
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
Page: Table 4
Anemia 1%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Sex: M+F
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Cardiac disorders grade 5, 2 patients
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Page: 123
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Sex: M+F
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Page: 123
Amylase increased 1%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Blood creatinine increased 2%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Diarrhea 2%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Fatigue 2%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Nausea 2%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Neutropenia 2%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Lipase increased 3%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Vomiting 4%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Thrombocytopenia 6%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Vomiting all grades, 11%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Anemia all grades, 18%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Fatigue all grades, 5%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Nausea all grades, 6%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Thrombocytopenia all grades, 7%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Diarrhea all grades, 8%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Anemia grade 3-4, 14%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Diarrhea grade 3-4, 3%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Nausea grade 3-4, 4%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Fatigue grade 3-4, 5%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Thrombocytopenia grade 3-4, 6%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Vomiting grade 3-4, 7%
Disc. AE
500 mg 1 times / day multiple, oral
Studied dose
Dose: 500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 - 75 years
n = 97
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 - 75 years
Population Size: 97
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Amylase increased 1%
Disc. AE
400 mg 1 times / day multiple, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 years (range: 27 - 86 years)
n = 96
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Lipase increased 1%
Disc. AE
400 mg 1 times / day multiple, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 years (range: 27 - 86 years)
n = 96
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Anemia 2%
Disc. AE
400 mg 1 times / day multiple, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 years (range: 27 - 86 years)
n = 96
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Diarrhea 2%
Disc. AE
400 mg 1 times / day multiple, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 years (range: 27 - 86 years)
n = 96
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Nausea 2%
Disc. AE
400 mg 1 times / day multiple, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 years (range: 27 - 86 years)
n = 96
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Vomiting all grades, 10%
Disc. AE
400 mg 1 times / day multiple, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 years (range: 27 - 86 years)
n = 96
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Fatigue all grades, 3%
Disc. AE
400 mg 1 times / day multiple, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 years (range: 27 - 86 years)
n = 96
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Thrombocytopenia all grades, 3%
Disc. AE
400 mg 1 times / day multiple, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 years (range: 27 - 86 years)
n = 96
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Anemia all grades, 8%
Disc. AE
400 mg 1 times / day multiple, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 years (range: 27 - 86 years)
n = 96
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Thrombocytopenia grade 3-4, 2%
Disc. AE
400 mg 1 times / day multiple, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 years (range: 27 - 86 years)
n = 96
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Fatigue grade 3-4, 3%
Disc. AE
400 mg 1 times / day multiple, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 years (range: 27 - 86 years)
n = 96
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Vomiting grade 3-4, 3%
Disc. AE
400 mg 1 times / day multiple, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 years (range: 27 - 86 years)
n = 96
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Anemia grade 3-4, 5%
Disc. AE
400 mg 1 times / day multiple, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
unhealthy, 65 years (range: 27 - 86 years)
n = 96
Health Status: unhealthy
Condition: intermediate-2 or high-risk myelofibrosis | post-polycythemia vera myelofibrosis | post-essential thrombocythemia myelofibrosis with splenomegaly
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Cardiac disorders grade 5, 2 patients
Disc. AE
400 mg 1 times / day multiple, oral
Recommended
Dose: 400 mg, 1 times / day
Route: oral
Route: multiple
Dose: 400 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Page: 123
unhealthy, 65 years (range: 27 - 86 years)
n = 96
Health Status: unhealthy
Condition: myelofibrosis
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
Population Size: 96
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Page: 123
Gastrointestinal disorders
680 mg single, oral
MTD
Dose: 680 mg
Route: oral
Route: single
Dose: 680 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/24165976/
healthy, adult
n = 2
Health Status: healthy
Age Group: adult
Sex: M
Population Size: 2
Sources:
https://pubmed.ncbi.nlm.nih.gov/24165976/
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1737

inhibitor
1587
inhibitor
1767
inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
P-gp
1461

BCRP
699

MATE1
306

MATE2
263

OCT2
647

OATP1B1
788

OATP1B3
706

OAT1
599

OAT3
642

OCT1
512

CYP2C19
1478

CYP1A2
1524

CYP2B6
810

CYP2C8
911
P-gp
1537

CYP2C19
991

FMO3
67

BCRP
561

OATP1B1
406

OATP1B3
350

BSEP
52

MRP2
205
CYP3A
129
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1692
 no
CYP2B6
1001
 no
CYP3A
298
 no
OAT1
603
 no
OAT3
644
 no
MATE2
263
 yes [IC50 0.227 uM]
MATE1
308
 yes [IC50 0.352 uM]
OCT2
648
 yes [IC50 0.78 uM]
P-gp
1650
 yes [IC50 10.1 uM]
CYP2C8
965
 yes [IC50 100.8 uM]
OATP1B1
803
 yes [IC50 16.4 uM]
CYP2D6
1891
 yes [IC50 20.2 uM]
yes (co-administration study)
Comment: fedratinib increased exposure of metoprolol by 2x
BCRP
773
 yes [IC50 29.9 uM]
CYP3A4
1925
 yes [IC50 3 uM]
yes (co-administration study)
Comment: fedratinib increased exposure of midazolam by 4x
CYP2C9
1819
 yes [IC50 52.2 uM]
OCT1
543
 yes [IC50 6.06 uM]
OATP1B3
715
 yes [IC50 9.51 uM]
CYP2C19
1553
 yes
yes (co-administration study)
Comment: fedratinib increased exposure of omeprazole by 3x
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP2C19
991
 major
FMO3
67
 major
CYP3A4
1737
 major
yes (co-administration study)
Comment: ketoconazole increased cmax of fedratinib by 4x
BCRP
561
 no
BSEP
52
 no
MRP2
205
 no
OATP1B1
406
 no
OATP1B3
350
 no
P-gp
1537
 yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
001 Chemical
DY443054
https://www.001chemical.com/chem/936091-26-8
AA Blocks
AA00GU48
https://www.aablocks.com/goods/Goods/detail?id=AA00GU48
AK Scientific, Inc. (AKSCI)
SYN1104
http://www.aksci.com/item_detail.php?cat=SYN1104
AK Scientific, Inc. (AKSCI)
Y0268
http://www.aksci.com/item_detail.php?cat=Y0268
Aaron Chemicals
AR00GUW0
http://www.aaronchem.com/936091-26-8
AbMole Bioscience
1733
http://www.abmole.com/product.asp?id=1733
AbMole Bioscience
M1733
http://www.abmole.com/products/tg101348.html
Acadechem
ACDX-011122
http://acadechemical.com/product/86010
Aceschem
ACS019922
https://www.aceschem.com/catalog/936091-26-8.html
Achemtek
0101-002350
http://www.achemtek.com/936091-26-8
Active Biopharma
ABP000705
http://www.activebiopharma.com/936091-26-8
Adooq BioScience
TG-101348
http://www.adooq.com/tg-101348.html
Adooq BioScience
A11082
https://www.adooq.com/tg-101348.html
Allbio Pharm Co., Ltd
AD00400
http://www.allbiopharm.com/product/n/AD00400
Alsachim
4373
http://www.alsachim.com/product-C5698-glo.bal-view.html
Ambeed
A345883
https://www.ambeed.com/products/936091-26-8.html
Ambinter
Amb22169887
http://www.ambinter.com/reference/22169887
Angel Pharmatech
AG-10380
http://www.angelpharmatech.com/936091-26-8.html
ApexBio Technology
A4136
http://www.apexbt.com/tg101348-sar302503.html
Ark Pharm
AK-50248
http://www.arkpharminc.com/products/936091-26-8.html
Ark Pharma Scientific Limited
A-0185
http://www.arkpharmtech.com/product/32136.html
Aurora Fine Chemicals LLC
K16.642.248
http://online.aurorafinechemicals.com/info?ID=K16.642.248
Aurum Pharmatech LLC
W-5547
http://www.Aurumpharmatech.com/Product/ProductDetails/W_5547
Axon MedChem
1588
https://www.axonmedchem.com/product/1588
BLD Pharm
BD166858
http://www.bldpharm.com/products/936091-26-8.html
BOC Sciences
936091-26-8
https://www.bocsci.com/fedratinib-cas-936091-26-8-item-100796.html
BioChemPartner
BCP02300
http://www.biochempartner.com/936091-26-8-BCP02300
BioCrick
BCC2190
http://www.biocrick.com/TG101348-SAR302503-BCC2190.html
BioSynth
J-523769
https://www.biosynth.com/en/products/all-products/products/J-523769.html
Boerchem
BC644857
http://www.boerchem.com/?product_41978.html
CSNpharm
CSN12405
https://www.csnpharm.com/products/tg-101348.html
Chem Scene
CS-0052
http://www.chemscene.com/936091-26-8.html
ChemMol
44022659
http://www.chemmol.com/chemmol/44022659.html
ChemieTek
CT-TG101
http://www.chemietek.com/tg101348-details.aspx
Chemspace
CSSB00015190596
https://chem-space.com/CSSB00015190596
DC Chemicals
DC7318
http://www.dcchemicals.com/product_show-TG101348_Fedratinib_.html
Debye Scientific
DB-079623
http://www.debyesci.com/cas_936091-26-8.html
Debye Scientific
DA-40258
http://www.debyesci.com/cas_945381-69-1.html
Excenen
EX-A170
http://www.excenen.com/searchresultlist.php?id=936091-26-8
Finetech
FT-0705969
http://www.finetechnology-ind.com/prod/detail/pub/1374744-69-0.html
Finetech
FT-0766818
http://www.finetechnology-ind.com/prod/detail/pub/936091-26-8.html
Finetech
FT-0763396
http://www.finetechnology-ind.com/prod/detail/pub/945381-69-1.html
Hairui
HR33073
http://www.hairuichem.com/en/product/936091-26-8.html
Huateng Pharma
F92627
https://en.huatengsci.com/products/intermediates/
Lab Network
LN01308311
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01308311
Matrix Scientific
147234
https://www.matrixscientific.com/147234.html
MedChem Express
HY-10409
https://www.medchemexpress.com/TG-101348.html
Molcore
MC443054
https://www.molcore.com/product/936091-26-8
OChem
29958
http://www.ocheminc.com/index.php?act=psearch&pid=091D268
Renno Tech
RS0112
http://www.rennotech.com/product_show.asp?id=35712
Smolecule
S547874
http://www.smolecule.com/products/s547874
Smolecule
S766760
https://www.smolecule.com/products/s766760
Synblock Inc
SB14604
http://www.synblock.com/product/936091-26-8.html
THE BioTek
bt-287151
https://www.thebiotek.com/product/inhibitors/bt-287151
THE BioTek
bt-504588
https://www.thebiotek.com/product/others/bt-504588
VladaChem
VL279311-100MG
https://www.vladachem.com/product.php?products=936091-26-8
Yuhao Chemical
YH65945
http://chemyuhao.com/936091-26-8.html
abcr GmbH
AB482480
http://www.abcr.com/shop/en/AB482480
eNovation Chemicals
D320287
https://www.enovationchem.com/ProductDetails.asp?ProductID=D320287
eNovation Chemicals
K31297
https://www.enovationchem.com/ProductDetails.asp?ProductID=K31297
eNovation Chemicals
Y0973935
https://www.enovationchem.com/ProductDetails.asp?ProductID=Y0973935
iChemical
EBD8909
http://www.ichemical.com/chemicals/cas-936091-26-8
PubMed

PubMed

TitleDatePubMed
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.
2010 Nov 24
Comprehensive analysis of kinase inhibitor selectivity.
2011 Oct 30
Flavanoids induce expression of the suppressor of cytokine signalling 3 (SOCS3) gene and suppress IL-6-activated signal transducer and activator of transcription 3 (STAT3) activation in vascular endothelial cells.
2013 Sep 1
Patents

Patents

20070191405
3
JP2013541595A
3

Sample Use Guides

In Vivo Use Guide
Fedratinib therapy in patients with primary or secondary (post-polycythemia vera or post-essential thrombocythemia) MF: once-daily oral fedratinib, at a dose of 400 mg or 500 mg, or placebo, for at least 6 consecutive 4-week cycles. Fedratinib therapy significantly reduced splenomegaly and symptom burden in patients with MF. These benefits were accompanied by toxic effects in some patients, the most important being encephalopathy of unknown mechanism. Clinical development of fedratinib was subsequently discontinued.
Route of Administration: Oral
In Vitro Use Guide
300 nM Fedratinib (SAR-302503, TG-101348) significantly inhibited JAK2V617F+ progenitor-derived colony formation
Substance Class Chemical
Created
by admin
on Sat Dec 16 01:55:21 GMT 2023
Edited
by admin
on Sat Dec 16 01:55:21 GMT 2023
Record UNII
6L1XP550I6
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
FEDRATINIB
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
fedratinib [INN]
Common Name English
BENZENESULFONAMIDE, N-(1,1-DIMETHYLETHYL)-3-((5-METHYL-2-((4-(2-(1-PYRROLIDINYL)ETHOXY)PHENYL)AMINO)-4-PYRIMIDINYL)AMINO)-
Systematic Name English
FEDRATINIB [MI]
Common Name English
Fedratinib [WHO-DD]
Common Name English
N-TERT-BUTYL-3-((5-METHYL-2-(4-(2-(PYRROLIDIN-1-YL)ETHOXY)ANILINO(PYRIMIDIN-4-YL)AMINO)BENZENESULFONAMIDE
Common Name English
N-TERT-BUTYL-3-(5-METHYL-2-(4-(2-PYRROLIDIN-1-YL-ETHOXY)-PHENYLAMINO)-PYRIMIDIN-4-YLAMINO)-BENZENESULFONAMIDE
Systematic Name English
SAR-302503
Code English
SAR302503
Code English
TG101348
Code English
TG-101348
Code English
FEDRATINIB [USAN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C129825
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
NCI_THESAURUS C125450
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
Code System Code Type Description
DAILYMED
6L1XP550I6
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
PRIMARY
WIKIPEDIA
TG101348
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
PRIMARY
FDA UNII
6L1XP550I6
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
PRIMARY
MERCK INDEX
m12160
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
PRIMARY
USAN
AB-104
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
PRIMARY
ChEMBL
CHEMBL1287853
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
PRIMARY
DRUG CENTRAL
5347
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
PRIMARY
DRUG BANK
DB12500
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
PRIMARY
INN
9707
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
PRIMARY
EPA CompTox
DTXSID90239483
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
PRIMARY
NCI_THESAURUS
C88293
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
PRIMARY
CAS
936091-26-8
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
PRIMARY
EVMPD
SUB126288
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
PRIMARY
LACTMED
Fedratinib
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
PRIMARY
PUBCHEM
16722836
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
PRIMARY
RXCUI
2197490
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
PRIMARY
SMS_ID
100000151872
Created by admin on Sat Dec 16 01:55:21 GMT 2023 , Edited by admin on Sat Dec 16 01:55:21 GMT 2023
PRIMARY
Related Record Type Details
Structure of FEDRATINIB
EXCRETED UNCHANGED
AMOUNT EXCRETED
FECAL
CYTOCHROME P450 2C19
METABOLIC ENZYME -> SUBSTRATE
Metabolized by CYP3A4 (0 to 70%), CYP2C19 (0‐20%), and FMO3 (0‐33%) in vitro.
RECEPTOR-TYPE TYROSINE-PROTEIN KINASE FLT3
TARGET -> INHIBITOR
INHIBITOR
IC50
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
Structure of FEDRATINIB
EXCRETED UNCHANGED
AMOUNT EXCRETED
URINE
RECEPTOR-TYPE TYROSINE-PROTEIN KINASE FLT3 D835Y
TARGET -> INHIBITOR
Structure of FEDRATINIB HYDROCHLORIDE
SALT/SOLVATE -> PARENT
OCT-2
TRANSPORTER -> INHIBITOR
IC50
TYROSINE-PROTEIN KINASE JAK2
TARGET -> INHIBITOR
Structure of FEDRATINIB
CUMULATIVE EXCRETION
Only 82% of radioactivity recovered
URINE
PROTO-ONCOGENE TYROSINE-PROTEIN KINASE RECEPTOR RET
TARGET -> INHIBITOR
INHIBITOR
IC50
MULTIDRUG AND TOXIN EXTRUSION PROTEIN 1
TRANSPORTER -> INHIBITOR
IC50
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
Metabolized by CYP3A4 (0 to 70%), CYP2C19 (0‐20%), and FMO3 (0‐33%) in vitro.
TYROSINE-PROTEIN KINASE JAK2 V617F MUTANT
TARGET -> INHIBITOR
IC50
Structure of FEDRATINIB
CUMULATIVE EXCRETION
Only 82% of radioactivity recovered
FECAL
Structure of FEDRATINIB DIHYDROCHLORIDE ANHYDROUS
SALT/SOLVATE -> PARENT
THIAMINE TRANSPORTER 2
TRANSPORTER -> INHIBITOR
Patients being treated with fedratinib developed Wernicke?s encephalopathy (WE) (Sanofi, 2013), a neurological disorder linked to thiamine deficiency (Cook et al., 1998).
IC50
MATE-2
TRANSPORTER -> INHIBITOR
IC50
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> SUBSTRATE
FETAL HEPATIC FLAVIN-CONTAINING MONOOXYGENASE 3 (HUMAN)
METABOLIC ENZYME -> SUBSTRATE
Metabolized by CYP3A4 (0 to 70%), CYP2C19 (0‐20%), and FMO3 (0‐33%) in vitro.
TYROSINE-PROTEIN KINASE JAK1
TARGET -> INHIBITOR
NON-RECEPTOR TYROSINE-PROTEIN KINASE TYK2
TARGET -> INHIBITOR
IC50
TYROSINE-PROTEIN KINASE JAK3
TARGET -> INHIBITOR
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> INHIBITOR
IC50
ATP-BINDING CASSETTE SUB-FAMILY G MEMBER 2
TRANSPORTER -> INHIBITOR
IC50
Related Record Type Details
Structure of FEDRATINIB metabolite SAR318031
METABOLITE -> PARENT
Structure of FEDRATINIB metabolite SAR-317981
METABOLITE LESS ACTIVE -> PARENT
2 fold less active than parent. accounting for ~ 9% of the radioactivity AUC.
MAJOR
PLASMA
Related Record Type Details
Structure of FEDRATINIB
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Blood to Plasma Ratio PHARMACOKINETIC
Tmax PHARMACOKINETIC STEADY-STATE

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