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Details

Stereochemistry ACHIRAL
Molecular Formula C27H36N6O3S
Molecular Weight 524.6803
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of FEDRATINIB

SMILES

Cc1cnc(Nc2ccc(cc2)OCCN3CCCC3)[nH]c1=Nc4cccc(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

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

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

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
3.0 nM [IC50]
Conditions
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1804 ng/mL
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
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
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
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
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
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
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
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%
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%
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%
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: 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: 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: 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: 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: 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: 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: 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: 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: 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:
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:
Disc. AE: Anemia...
AEs leading to
discontinuation/dose reduction:
Anemia (1%)
Sources:
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: 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: Page: 123
Disc. AE: Cardiac disorders...
AEs leading to
discontinuation/dose reduction:
Cardiac disorders (grade 5, 2 patients)
Sources: 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:
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:
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:
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:
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:
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:
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: 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: Page: 123
Disc. AE: Cardiac disorders...
AEs leading to
discontinuation/dose reduction:
Cardiac disorders (grade 5, 2 patients)
Sources: Page: 123
800 mg single, oral
Highest studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources: Page: 20
unhealthy, adult
n = 1
Health Status: unhealthy
Condition: myelofibrosis
Age Group: adult
Sex: unknown
Population Size: 1
Sources: 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: Page: 68
unhealthy, adult
n = 31
Health Status: unhealthy
Condition: myelofibrosis
Age Group: adult
Sex: unknown
Population Size: 31
Sources: Page: 68
680 mg single, oral
MTD
Dose: 680 mg
Route: oral
Route: single
Dose: 680 mg
Sources:
healthy, adult
n = 2
Health Status: healthy
Age Group: adult
Sex: M
Population Size: 2
Sources:
Other AEs: Gastrointestinal disorders...
Other AEs:
Gastrointestinal disorders
Sources:
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:
unhealthy
n = 6
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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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: 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:
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:
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: 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: 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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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:
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: 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: Page: 123
Gastrointestinal disorders
680 mg single, oral
MTD
Dose: 680 mg
Route: oral
Route: single
Dose: 680 mg
Sources:
healthy, adult
n = 2
Health Status: healthy
Age Group: adult
Sex: M
Population Size: 2
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
yes [IC50 0.227 uM]
yes [IC50 0.352 uM]
yes [IC50 0.78 uM]
yes [IC50 10.1 uM]
yes [IC50 100.8 uM]
yes [IC50 16.4 uM]
yes [IC50 20.2 uM]
yes (co-administration study)
Comment: fedratinib increased exposure of metoprolol by 2x
yes [IC50 29.9 uM]
yes [IC50 3 uM]
yes (co-administration study)
Comment: fedratinib increased exposure of midazolam by 4x
yes [IC50 52.2 uM]
yes [IC50 6.06 uM]
yes [IC50 9.51 uM]
yes
yes (co-administration study)
Comment: fedratinib increased exposure of omeprazole by 3x
Drug as victimTox targets

Tox targets

Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera.
2008 Apr
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.
2010 Nov 24
Utilization of human nuclear receptors as an early counter screen for off-target activity: a case study with a compendium of 615 known drugs.
2015 Jun
Patents

Sample Use Guides

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
300 nM Fedratinib (SAR-302503, TG-101348) significantly inhibited JAK2V617F+ progenitor-derived colony formation
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
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 [WHO-DD]
Common Name English
FEDRATINIB [USAN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C129825
Created by admin on Sat Jun 26 10:16:09 UTC 2021 , Edited by admin on Sat Jun 26 10:16:09 UTC 2021
NCI_THESAURUS C125450
Created by admin on Sat Jun 26 10:16:09 UTC 2021 , Edited by admin on Sat Jun 26 10:16:09 UTC 2021
Code System Code Type Description
WIKIPEDIA
TG101348
Created by admin on Sat Jun 26 10:16:09 UTC 2021 , Edited by admin on Sat Jun 26 10:16:09 UTC 2021
PRIMARY
FDA UNII
6L1XP550I6
Created by admin on Sat Jun 26 10:16:09 UTC 2021 , Edited by admin on Sat Jun 26 10:16:09 UTC 2021
PRIMARY
MERCK INDEX
M12160
Created by admin on Sat Jun 26 10:16:09 UTC 2021 , Edited by admin on Sat Jun 26 10:16:09 UTC 2021
PRIMARY
ChEMBL
CHEMBL1287853
Created by admin on Sat Jun 26 10:16:09 UTC 2021 , Edited by admin on Sat Jun 26 10:16:09 UTC 2021
PRIMARY
DRUG CENTRAL
5347
Created by admin on Sat Jun 26 10:16:09 UTC 2021 , Edited by admin on Sat Jun 26 10:16:09 UTC 2021
PRIMARY
DRUG BANK
DB12500
Created by admin on Sat Jun 26 10:16:09 UTC 2021 , Edited by admin on Sat Jun 26 10:16:09 UTC 2021
PRIMARY
INN
9707
Created by admin on Sat Jun 26 10:16:09 UTC 2021 , Edited by admin on Sat Jun 26 10:16:09 UTC 2021
PRIMARY
EPA CompTox
936091-26-8
Created by admin on Sat Jun 26 10:16:09 UTC 2021 , Edited by admin on Sat Jun 26 10:16:09 UTC 2021
PRIMARY
NCI_THESAURUS
C88293
Created by admin on Sat Jun 26 10:16:09 UTC 2021 , Edited by admin on Sat Jun 26 10:16:09 UTC 2021
PRIMARY
CAS
936091-26-8
Created by admin on Sat Jun 26 10:16:09 UTC 2021 , Edited by admin on Sat Jun 26 10:16:09 UTC 2021
PRIMARY
EVMPD
SUB126288
Created by admin on Sat Jun 26 10:16:09 UTC 2021 , Edited by admin on Sat Jun 26 10:16:09 UTC 2021
PRIMARY
LACTMED
Fedratinib
Created by admin on Sat Jun 26 10:16:09 UTC 2021 , Edited by admin on Sat Jun 26 10:16:09 UTC 2021
PRIMARY
PUBCHEM
16722836
Created by admin on Sat Jun 26 10:16:09 UTC 2021 , Edited by admin on Sat Jun 26 10:16:09 UTC 2021
PRIMARY
RXCUI
2197490
Created by admin on Sat Jun 26 10:16:09 UTC 2021 , Edited by admin on Sat Jun 26 10:16:09 UTC 2021
PRIMARY