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

Details

Stereochemistry ACHIRAL
Molecular Formula 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

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
4002
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
8504
 3.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Phase II
1147
Unknown

Approved Use

Unknown
Primary
Phase II
1147
Unknown

Approved Use

Unknown
Primary
Phase I
438
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
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
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 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
2539 ng/mL
OTHER GOV
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 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
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
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 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
38712 ng × h/mL
OTHER GOV
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 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
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
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 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
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 plasma
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
2%
OTHER GOV
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 plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
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
Health Status: unhealthy
Age Group: 65 - 75 years
Sex: M+F
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
unhealthy, 65 - 75 years
Health Status: unhealthy
Age Group: 65 - 75 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
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
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
Health Status: unhealthy
Age Group: 65 - 75 years
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)
Health Status: unhealthy
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
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
unhealthy, 65 years (range: 27 - 86 years)
Health Status: unhealthy
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
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
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
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
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
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sex: unknown
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
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
Health Status: healthy
Age Group: adult
Sex: M
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
Health Status: unhealthy
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
unhealthy, 27 - 86 years
Health Status: unhealthy
Age Group: 27 - 86 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212327s000lbl.pdf
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
Health Status: unhealthy
Age Group: 65 - 75 years
Sex: M+F
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
unhealthy, 65 - 75 years
Health Status: unhealthy
Age Group: 65 - 75 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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
Health Status: unhealthy
Age Group: 65 - 75 years
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)
Health Status: unhealthy
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
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
unhealthy, 65 years (range: 27 - 86 years)
Health Status: unhealthy
Age Group: 65 years (range: 27 - 86 years)
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212327Orig1s000MultidisciplineR.pdf
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
Health Status: healthy
Age Group: adult
Sex: M
Sources:
https://pubmed.ncbi.nlm.nih.gov/24165976/
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1946

inhibitor
2252
inhibitor
2438
inhibitor
2507
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
P-gp
1741

BCRP
910

MATE1
415

MATE2
267

OCT2
779

OATP1B1
1079

OATP1B3
961

OAT1
725

OAT3
747

OCT1
620

CYP2C19
2057

CYP1A2
2153

CYP2B6
926

CYP2C8
1057
P-gp
2052

CYP2C19
1119

FMO3
77

BCRP
697

OATP1B1
503

OATP1B3
435

BSEP
63

MRP2
252
CYP3A
142
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
2333
 no
CYP2B6
1160
 no
CYP3A
317
 no
OAT1
730
 no
OAT3
749
 no
MATE2
267
 yes [IC50 0.227 uM]
MATE1
416
 yes [IC50 0.352 uM]
OCT2
782
 yes [IC50 0.78 uM]
P-gp
1932
 yes [IC50 10.1 uM]
CYP2C8
1117
 yes [IC50 100.8 uM]
OATP1B1
1095
 yes [IC50 16.4 uM]
CYP2D6
2546
 yes [IC50 20.2 uM]
yes (co-administration study)
Comment: fedratinib increased exposure of metoprolol by 2x
BCRP
985
 yes [IC50 29.9 uM]
CYP3A4
2633
 yes [IC50 3 uM]
yes (co-administration study)
Comment: fedratinib increased exposure of midazolam by 4x
CYP2C9
2497
 yes [IC50 52.2 uM]
OCT1
656
 yes [IC50 6.06 uM]
OATP1B3
970
 yes [IC50 9.51 uM]
CYP2C19
2141
 yes
yes (co-administration study)
Comment: fedratinib increased exposure of omeprazole by 3x
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP2C19
1119
 major
FMO3
77
 major
CYP3A4
1946
 major
yes (co-administration study)
Comment: ketoconazole increased cmax of fedratinib by 4x
BCRP
697
 no
BSEP
63
 no
MRP2
252
 no
OATP1B1
503
 no
OATP1B3
435
 no
P-gp
2052
 yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
2263
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
Aaron Chemicals
AR00GUW0
http://www.aaronchem.com/936091-26-8
abcr GmbH
AB482480
http://www.abcr.com/shop/en/AB482480
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
A11082
https://www.adooq.com/tg-101348.html
Adooq BioScience
TG-101348
http://www.adooq.com/tg-101348.html
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
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
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
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
Boerchem
BC644857
http://www.boerchem.com/?product_41978.html
Chem Scene
CS-0052
http://www.chemscene.com/936091-26-8.html
ChemieTek
CT-TG101
http://www.chemietek.com/tg101348-details.aspx
ChemMol
44022659
http://www.chemmol.com/chemmol/44022659.html
Chemspace
CSSB00015190596
https://chem-space.com/CSSB00015190596
CSNpharm
CSN12405
https://www.csnpharm.com/products/tg-101348.html
DC Chemicals
DC7318
http://www.dcchemicals.com/product_show-TG101348_Fedratinib_.html
Debye Scientific
DA-40258
http://www.debyesci.com/cas_945381-69-1.html
Debye Scientific
DB-079623
http://www.debyesci.com/cas_936091-26-8.html
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
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-0763396
http://www.finetechnology-ind.com/prod/detail/pub/945381-69-1.html
Finetech
FT-0766818
http://www.finetechnology-ind.com/prod/detail/pub/936091-26-8.html
Hairui
HR33073
http://www.hairuichem.com/en/product/936091-26-8.html
Huateng Pharma
F92627
https://en.huatengsci.com/products/intermediates/
iChemical
EBD8909
http://www.ichemical.com/chemicals/cas-936091-26-8
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
PubMed

PubMed

TitleDatePubMed
Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera.
2008 Apr
Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3.
2010 Dec 15
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
Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.
2014 Apr
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

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
Name Type Language
fedratinib [INN]
Preferred Name English
FEDRATINIB
INN   USAN   WHO-DD  
USAN   INN  
Official 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 Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
NCI_THESAURUS C125450
Created by admin on Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
Code System Code Type Description
DAILYMED
6L1XP550I6
Created by admin on Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
PRIMARY
WIKIPEDIA
TG101348
Created by admin on Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
PRIMARY
FDA UNII
6L1XP550I6
Created by admin on Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
PRIMARY
MERCK INDEX
m12160
Created by admin on Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
PRIMARY
USAN
AB-104
Created by admin on Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
PRIMARY
ChEMBL
CHEMBL1287853
Created by admin on Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
PRIMARY
DRUG CENTRAL
5347
Created by admin on Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
PRIMARY
DRUG BANK
DB12500
Created by admin on Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
PRIMARY
INN
9707
Created by admin on Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
PRIMARY
EPA CompTox
DTXSID90239483
Created by admin on Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
PRIMARY
NCI_THESAURUS
C88293
Created by admin on Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
PRIMARY
CAS
936091-26-8
Created by admin on Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
PRIMARY
EVMPD
SUB126288
Created by admin on Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
PRIMARY
LACTMED
Fedratinib
Created by admin on Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
PRIMARY
PUBCHEM
16722836
Created by admin on Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
PRIMARY
RXCUI
2197490
Created by admin on Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
PRIMARY
SMS_ID
100000151872
Created by admin on Mon Mar 31 21:04:26 GMT 2025 , Edited by admin on Mon Mar 31 21:04:26 GMT 2025
PRIMARY
ACTIVE MOIETY
Structure of FEDRATINIB
METABOLITE LESS ACTIVE (PARENT)
Structure of FEDRATINIB metabolite SAR-317981
SALT/SOLVATE (PARENT)
Structure of FEDRATINIB HYDROCHLORIDE
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966