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Details

Stereochemistry ACHIRAL
Molecular Formula C28H24FN3O5
Molecular Weight 501.5057
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of Cabozantinib

SMILES

COC1=CC2=NC=CC(OC3=CC=C(NC(=O)C4(CC4)C(=O)NC5=CC=C(F)C=C5)C=C3)=C2C=C1OC

InChI

InChIKey=ONIQOQHATWINJY-UHFFFAOYSA-N
InChI=1S/C28H24FN3O5/c1-35-24-15-21-22(16-25(24)36-2)30-14-11-23(21)37-20-9-7-19(8-10-20)32-27(34)28(12-13-28)26(33)31-18-5-3-17(29)4-6-18/h3-11,14-16H,12-13H2,1-2H3,(H,31,33)(H,32,34)

HIDE SMILES / InChI
Molecular Formula C28H24FN3O5
Molecular Weight 501.5057
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/?term=21606412

Cabozantinib (development code name XL184; marketed under the trade name Cometriq) is an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Cabozantinib strongly binds to and inhibits several RTKs, which are often overexpressed in a variety of cancer cell types, including hepatocyte growth factor receptor (MET), RET (rearranged during transfection), vascular endothelial growth factor receptor types 1 (VEGFR-1), 2 (VEGFR-2), and 3 (VEGFR-3), mast/stem cell growth factor (KIT), FMS-like tyrosine kinase 3 (FLT-3), TIE-2 (TEK tyrosine kinase, endothelial), tropomyosin-related kinase B (TRKB) and AXL. This may result in an inhibition of both tumor growth and angiogenesis, and eventually lead to tumor regression. Cabozantinib was granted orphan drug status by the U.S. Food and Drug Administration (FDA) in January 2011. It is currently undergoing clinical trials for the treatment of prostate, bladder, ovarian, brain, melanoma, breast, non-small cell lung, pancreatic, hepatocellular and kidney cancers.

CNS Activity

CNS Penetrant
2588
Curator's Comment: A short period of cabozantinib treatment, enough to restore the blood-brain barrier, will result in inhibition of distribution of the compound to tumor cells in later stages of treatment

Originator

Approval Year

2012
608
Targets

Targets

Primary TargetPharmacologyConditionPotency
Proto-oncogene tyrosine-protein kinase receptor Ret
7
Target ID: P07949
Gene ID: 5979.0
Gene Symbol: RET
Target Organism: Homo sapiens (Human)
Inhibitor
8504
 5.2 nM [IC50]
Hepatocyte growth factor receptor
56
Target ID: P08581
Gene ID: 4233.0
Gene Symbol: MET
Target Organism: Homo sapiens (Human)
Inhibitor
8504
 1.3 nM [IC50]
Vascular endothelial growth factor receptor 2
112
Target ID: P35968
Gene ID: 3791.0
Gene Symbol: KDR
Target Organism: Homo sapiens (Human)
Inhibitor
8504
 0.035 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
COMETRIQ

Approved Use

COMETRIQ is the (S)-malate salt of cabozantinib. COMETRIQ is a kinase inhibitor indicated for the treatment of patients with progressive, metastatic medullary thyroid cancer

Launch Date

2012
Primary
Approved
8583
CABOMETYX

Approved Use

CABOMETYX is the (S)-malate salt of cabozantinib. CABOMETYX is a kinase inhibitor indicated for the treatment of patients with advanced renal cell carcinoma (RCC).

Launch Date

2016
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
554 ng/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/27139820
140 mg single, oral
dose: 140 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CABOZANTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
58300 ng × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/27139820
140 mg single, oral
dose: 140 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CABOZANTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
112 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/27139820
140 mg single, oral
dose: 140 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CABOZANTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
0.3%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/208692s000lbl.pdf
CABOZANTINIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
250 mg 1 times / day multiple, oral
Highest studied dose
Dose: 250 mg, 1 times / day
Route: oral
Route: multiple
Dose: 250 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Other AEs: Aspartate aminotransferase increased, Palmar-plantar erythrodysesthesia syndrome...
Other AEs:
Aspartate aminotransferase increased (grade 3, 16.7%)
Palmar-plantar erythrodysesthesia syndrome (grade 3, 16.7%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
265 mg 1 times / day multiple, oral
Highest studied dose
Dose: 265 mg, 1 times / day
Route: oral
Route: multiple
Dose: 265 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Other AEs: Mucositis...
Other AEs:
Mucositis (grade 2, 20%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
175 mg 1 times / day multiple, oral
MTD
Dose: 175 mg, 1 times / day
Route: oral
Route: multiple
Dose: 175 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
162.5 mg 1 times / day multiple, oral
Dose: 162.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 162.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Other AEs: Diarrhea, Fatigue...
Other AEs:
Diarrhea (grade 3, 8%)
Fatigue (grade 3, 13%)
Decreased appetite (grade 3, 3%)
Nausea (grade 3, 3%)
Palmar-plantar erythrodysesthesia syndrome (grade 3, 20%)
Aspartate aminotransferase increased (grade 3, 5%)
Alanine aminotransferase increased (grade 3, 5%)
Weight decreased (grade 3, 3%)
Hypertension (grade 3, 5%)
Lipase increased (grade 3, 18%)
Blood amylase increased (grade 3, 8%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
175 mg 1 times / day multiple, oral
Dose: 175 mg, 1 times / day
Route: oral
Route: multiple
Dose: 175 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Other AEs: Pulmonary embolism...
Other AEs:
Pulmonary embolism (grade 4)
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
11.52 mg/kg 1 times / day multiple, oral
Dose: 11.52 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 11.52 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Other AEs: Palmar-plantar erythrodysesthesia syndrome, Aspartate aminotransferase increased...
Other AEs:
Palmar-plantar erythrodysesthesia syndrome (grade 3, 33.3%)
Aspartate aminotransferase increased (grade 3, 33.3%)
Alanine aminotransferase increase (grade 3, 33.3%)
Lipase increased (grade 3, 33.3%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
100 mg 1 times / day multiple, oral
Studied dose
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/28352985/
unhealthy, median age 64.8 years
Health Status: unhealthy
Age Group: median age 64.8 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/28352985/
Disc. AE: Large intestine perforation, Intracranial hemorrhage...
AEs leading to
discontinuation/dose reduction:
Large intestine perforation (7.7%)
Intracranial hemorrhage (7.7%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/28352985/
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Disc. AE: Fatigue, Asthenia...
Other AEs: Fatigue, Asthenia...
AEs leading to
discontinuation/dose reduction:
Fatigue (1.2%)
Asthenia (0.9%)
Death (grade 5, 0.6%)
Diarrhea (0.9%)
Vomiting (0.6%)
Nausea (0.3%)
Constipation (0.3%)
Anal fistula (0.3%)
Dry mouth (0.3%)
Dysphagia (0.3%)
Gastrointestinal perforation (0.3%)
Pancreatitis (0.3%)
Palmar-plantar erythrodysesthesia syndrome (0.3%)
Pain in extremity (0.6%)
Proteinuria (0.9%)
Renal failure (0.3%)
Decreased appetite (1.8%)
Dehydration (0.3%)
Hyperkalemia (0.3%)
Adenocarcinoma (0.3%)
Leiomyoma (0.3%)
Anal abscess (0.3%)
Anorectal cellulitis (0.3%)
Device related infection (0.3%)
AST increased (0.3%)
Weight decreased (0.3%)
Cardiac failure (0.3%)
Ventricular arrhythmia (0.3%)
Hepatitis cholestatic (0.3%)
Muscle spasticity (0.3%)
Pneumothorax (0.3%)
Pulmonary embolism (0.3%)
Asthenia (grade 3, 0.6%)
Anal fistula (grade 3, 0.3%)
Gastrointestinal perforation (grade 3, 0.3%)
Pancreatitis (grade 3, 0.3%)
Pain in extremity (grade 3, 0.3%)
Proteinuria (grade 3, 0.9%)
Renal failure (grade 3, 0.3%)
Decreased appetite (grade 3, 0.9%)
Hyperkalemia (grade 3, 0.3%)
Anal abscess (grade 3, 0.3%)
Anorectal cellulitis (grade 3, 0.3%)
Device related infection (grade 3, 0.3%)
Weight decreased (grade 3, 0.3%)
Hepatitis cholestatic (grade 3, 0.3%)
Pneumothorax (grade 3, 0.3%)
Pulmonary embolism (grade 3, 0.3%)
Diarrhea (16%)
Palmar-plantar erythrodysesthesia syndrome (11%)
Fatigue (10%)
Hypertension (7.6%)
Diarrhea (grade 3, 5.1%)
Palmar-plantar erythrodysesthesia syndrome (grade 3, 4.2%)
Fatigue (grade 3, 3.6%)
Hypertension (grade 3, 6%)
Diarrhea (22%)
Palmar-plantar erythrodysesthesia syndrome (14%)
Fatigue (12%)
Nausea (8.5%)
Decreased appetite (7.6%)
Vomiting (7.6%)
Hypertension (5.1%)
Diarrhea (grade 3, 8.2%)
Palmar-plantar erythrodysesthesia syndrome (grade 3, 7.3%)
Fatigue (grade 3, 4.8%)
Nausea (grade 3, 1.2%)
Decreased appetite (grade 3, 1.2%)
Vomiting (grade 3, 1.2%)
Hypertension (grade 3, 4.5%)
Other AEs:
Fatigue (grade 3, 9.1%)
Asthenia (grade 3, 4.2%)
General physical health deterioration (grade 3, 2.1%)
Diarrhea (grade 3, 11.5%)
Nausea (grade 3, 3.9%)
Abdominal pain (grade 3, 3.6%)
Stomatitis (grade 3, 2.4%)
Vomiting (grade 3, 2.1%)
Palmar-plantar erythrodysesthesia syndrome (grade 3, 8.2%)
Hypertension (grade 3, 14.8%)
Anemia (grade 3, 5.4%)
Dyspnea (grade 3, 3%)
Pleural effusion (grade 3, 2.7%)
Pulmonary embolism (grade 3, 2.4%)
Pneumonia (grade 3, 1.5%)
Hypomagnesemia (grade 3, 4.8%)
Hypokalemia (grade 3, 4.5%)
Hyponatremia (grade 3, 3.9%)
Hypophosphatemia (grade 3, 3.6%)
Decreased appetite (grade 3, 2.7%)
Hypocalcemia (grade 3, 1.8%)
Back pain (grade 3, 2.1%)
Syncope (grade 3, 1.5%)
Proteinuria (grade 3, 2.4%)
Lipase increased (grade 3, 2.7%)
ALT increased (grade 3, 2.4%)
AST increased (grade 3, 1.8%)
Weight decreased (grade 3, 1.8%)
Blood bilirubin increased (grade 3, 1.5%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
200 mg 1 times / day multiple, oral
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
Other AEs: Memory impairment, Mental status changes...
Other AEs:
Memory impairment (grade 3)
Mental status changes (grade 3)
Cognitive disturbance (grade 3)
Weight loss (grade 2)
Blood urea nitrogen increased (grade 1)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
AEs

AEs

AESignificanceDosePopulation
Aspartate aminotransferase increased grade 3, 16.7%
250 mg 1 times / day multiple, oral
Highest studied dose
Dose: 250 mg, 1 times / day
Route: oral
Route: multiple
Dose: 250 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Palmar-plantar erythrodysesthesia syndrome grade 3, 16.7%
250 mg 1 times / day multiple, oral
Highest studied dose
Dose: 250 mg, 1 times / day
Route: oral
Route: multiple
Dose: 250 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Mucositis grade 2, 20%
265 mg 1 times / day multiple, oral
Highest studied dose
Dose: 265 mg, 1 times / day
Route: oral
Route: multiple
Dose: 265 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Fatigue grade 3, 13%
162.5 mg 1 times / day multiple, oral
Dose: 162.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 162.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Lipase increased grade 3, 18%
162.5 mg 1 times / day multiple, oral
Dose: 162.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 162.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Palmar-plantar erythrodysesthesia syndrome grade 3, 20%
162.5 mg 1 times / day multiple, oral
Dose: 162.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 162.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Decreased appetite grade 3, 3%
162.5 mg 1 times / day multiple, oral
Dose: 162.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 162.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Nausea grade 3, 3%
162.5 mg 1 times / day multiple, oral
Dose: 162.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 162.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Weight decreased grade 3, 3%
162.5 mg 1 times / day multiple, oral
Dose: 162.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 162.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Alanine aminotransferase increased grade 3, 5%
162.5 mg 1 times / day multiple, oral
Dose: 162.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 162.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Aspartate aminotransferase increased grade 3, 5%
162.5 mg 1 times / day multiple, oral
Dose: 162.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 162.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Hypertension grade 3, 5%
162.5 mg 1 times / day multiple, oral
Dose: 162.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 162.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Blood amylase increased grade 3, 8%
162.5 mg 1 times / day multiple, oral
Dose: 162.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 162.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Diarrhea grade 3, 8%
162.5 mg 1 times / day multiple, oral
Dose: 162.5 mg, 1 times / day
Route: oral
Route: multiple
Dose: 162.5 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Pulmonary embolism grade 4
175 mg 1 times / day multiple, oral
Dose: 175 mg, 1 times / day
Route: oral
Route: multiple
Dose: 175 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Alanine aminotransferase increase grade 3, 33.3%
11.52 mg/kg 1 times / day multiple, oral
Dose: 11.52 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 11.52 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Aspartate aminotransferase increased grade 3, 33.3%
11.52 mg/kg 1 times / day multiple, oral
Dose: 11.52 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 11.52 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Lipase increased grade 3, 33.3%
11.52 mg/kg 1 times / day multiple, oral
Dose: 11.52 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 11.52 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Palmar-plantar erythrodysesthesia syndrome grade 3, 33.3%
11.52 mg/kg 1 times / day multiple, oral
Dose: 11.52 mg/kg, 1 times / day
Route: oral
Route: multiple
Dose: 11.52 mg/kg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21606412/
Intracranial hemorrhage 7.7%
Disc. AE
100 mg 1 times / day multiple, oral
Studied dose
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/28352985/
unhealthy, median age 64.8 years
Health Status: unhealthy
Age Group: median age 64.8 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/28352985/
Large intestine perforation 7.7%
Disc. AE
100 mg 1 times / day multiple, oral
Studied dose
Dose: 100 mg, 1 times / day
Route: oral
Route: multiple
Dose: 100 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/28352985/
unhealthy, median age 64.8 years
Health Status: unhealthy
Age Group: median age 64.8 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
https://pubmed.ncbi.nlm.nih.gov/28352985/
AST increased 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Adenocarcinoma 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Anal abscess 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Anal fistula 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Anorectal cellulitis 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Cardiac failure 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Constipation 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Dehydration 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Device related infection 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Dry mouth 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Dysphagia 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Gastrointestinal perforation 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Hepatitis cholestatic 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Hyperkalemia 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Leiomyoma 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Muscle spasticity 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Nausea 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Palmar-plantar erythrodysesthesia syndrome 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Pancreatitis 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Pneumothorax 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Pulmonary embolism 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Renal failure 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Ventricular arrhythmia 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Weight decreased 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Pain in extremity 0.6%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Vomiting 0.6%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Asthenia 0.9%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Diarrhea 0.9%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Proteinuria 0.9%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Fatigue 1.2%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Decreased appetite 1.8%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Fatigue 10%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Palmar-plantar erythrodysesthesia syndrome 11%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Fatigue 12%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Palmar-plantar erythrodysesthesia syndrome 14%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Diarrhea 16%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Diarrhea 22%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Hypertension 5.1%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Decreased appetite 7.6%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Hypertension 7.6%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Vomiting 7.6%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Nausea 8.5%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Anal abscess grade 3, 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Anal fistula grade 3, 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Anorectal cellulitis grade 3, 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Device related infection grade 3, 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Gastrointestinal perforation grade 3, 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Hepatitis cholestatic grade 3, 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Hyperkalemia grade 3, 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Pain in extremity grade 3, 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Pancreatitis grade 3, 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Pneumothorax grade 3, 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Pulmonary embolism grade 3, 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Renal failure grade 3, 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Weight decreased grade 3, 0.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Asthenia grade 3, 0.6%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Decreased appetite grade 3, 0.9%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Proteinuria grade 3, 0.9%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Decreased appetite grade 3, 1.2%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Nausea grade 3, 1.2%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Vomiting grade 3, 1.2%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Blood bilirubin increased grade 3, 1.5%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Pneumonia grade 3, 1.5%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Syncope grade 3, 1.5%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
AST increased grade 3, 1.8%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Hypocalcemia grade 3, 1.8%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Weight decreased grade 3, 1.8%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Diarrhea grade 3, 11.5%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Hypertension grade 3, 14.8%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Back pain grade 3, 2.1%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
General physical health deterioration grade 3, 2.1%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Vomiting grade 3, 2.1%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
ALT increased grade 3, 2.4%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Proteinuria grade 3, 2.4%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Pulmonary embolism grade 3, 2.4%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Stomatitis grade 3, 2.4%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Decreased appetite grade 3, 2.7%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Lipase increased grade 3, 2.7%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Pleural effusion grade 3, 2.7%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Dyspnea grade 3, 3%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Abdominal pain grade 3, 3.6%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Hypophosphatemia grade 3, 3.6%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Fatigue grade 3, 3.6%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Hyponatremia grade 3, 3.9%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Nausea grade 3, 3.9%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Asthenia grade 3, 4.2%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Palmar-plantar erythrodysesthesia syndrome grade 3, 4.2%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Hypokalemia grade 3, 4.5%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Hypertension grade 3, 4.5%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Hypomagnesemia grade 3, 4.8%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Fatigue grade 3, 4.8%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Diarrhea grade 3, 5.1%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Anemia grade 3, 5.4%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Hypertension grade 3, 6%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Palmar-plantar erythrodysesthesia syndrome grade 3, 7.3%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Palmar-plantar erythrodysesthesia syndrome grade 3, 8.2%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Diarrhea grade 3, 8.2%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Fatigue grade 3, 9.1%
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Death grade 5, 0.6%
Disc. AE
60 mg 1 times / day multiple, oral
Recommended
Dose: 60 mg, 1 times / day
Route: oral
Route: multiple
Dose: 60 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/208692Orig1s000MedR.pdf
Blood urea nitrogen increased grade 1
200 mg 1 times / day multiple, oral
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
Weight loss grade 2
200 mg 1 times / day multiple, oral
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
Cognitive disturbance grade 3
200 mg 1 times / day multiple, oral
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
Memory impairment grade 3
200 mg 1 times / day multiple, oral
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
Mental status changes grade 3
200 mg 1 times / day multiple, oral
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203756lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1946

inhibitor
2252

inducer
1087
substrate
1193

inhibitor
2438

inducer
440
inhibitor
2507
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP2C8
1057

CYP2C19
2057

P-gp
1741

BCRP
910

BSEP
550

MRP2
499

OAT1
725

OAT3
747

OCT1
620

OATP1B1
1079

OATP1B3
961
MRP2
252

OAT1
395

OCT1
393

OATP1B1
503

OATP1B3
435

MATE1
182

MATE2
98

P-gp
2052
CYP1A1
151

CYP1A2
832

CYP2B6
669

CYP2C8
198

CYP2C19
329
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
BCRP
985
 no
BSEP
554
 no
CYP1A2
2333
 no
CYP2B6
1160
 no
CYP2C19
2141
 no
CYP2C8
1117
 no
CYP2C9
2497
 no
CYP3A4
2633
 no
MRP2
625
 no
OAT1
730
 no
OAT3
749
 no
OATP1B1
1095
 no
OATP1B3
970
 no
OCT1
656
 no
P-gp
1932
 yes [IC50 7 uM]
CYP2D6
2546
 yes [IC50 >20 uM]
CYP2C9
2497
 yes [Ki 10.4 uM]
CYP2C19
2141
 yes [Ki 28.8 uM]
CYP3A4
2633
 yes [Ki 282 uM]
CYP2C8
1117
 yes [Ki 4.6 uM]
CYP1A1
272
 yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
OAT1
395
 no
OATP1B1
503
 no
OATP1B3
435
 no
OCT1
393
 no
P-gp
2052
 no
MATE2
98
 yes [IC50 3.2 uM]
MATE1
182
 yes [IC50 5.94 uM]
MRP2
252
 yes
CYP2C9
1193
 yes
no (co-administration study)
Comment: Inhibition of CYP2C9 had a minimal effect on cabozantinib metabolite formation (i.e., a <20% reduction).
Page: -
CYP3A4
1946
 yes
yes (co-administration study)
Comment: Inhibition of CYP3A4 reduced the formation of the XL184 N-oxide metabolite by >80%.
Page: -
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
2263
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:72317
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:72317
eMolecules
36516753
https://www.emolecules.com/cgi-bin/more?vid=36516753
MolPort
MolPort-021-804-939
https://www.molport.com/shop/molecule-link/MolPort-021-804-939
Selleck Chemicals
XL184
http://www.selleckchem.com/products/XL184.html
ZINC
ZINC000070466416
http://zinc15.docking.org/substances/ZINC000070466416
PubMed

PubMed

TitleDatePubMed
Cabozantinib versus Everolimus in Advanced Renal-Cell Carcinoma.
2015-11-05
Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth.
2011-12
Patents

Patents

07579473
4
08067436
5
08178532
5
08476298
5
08497284
4
20070054928
5
20070225307
5
20070244116
5
20090105299
5
20090170896
7
20100209420
7

Sample Use Guides

In Vivo Use Guide
Recommended Dose: 140 mg orally, once daily
Route of Administration: Oral
In Vitro Use Guide
For in vitro assays, 10 mM cabozantinib stock solutions were prepared in dimethyl sulfoxide (DMSO) and diluted in the appropriate media.
Substance Class Chemical
Created
by admin
on Mon Mar 31 19:45:47 GMT 2025
Edited
by admin
on Mon Mar 31 19:45:47 GMT 2025
Record UNII
1C39JW444G
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
Cabozantinib [INN]
Preferred Name English
Cabozantinib
DASH   INN   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
1,1-Cyclopropanedicarboxamide, N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N?-(4-fluorophenyl)-
Systematic Name English
Cabozantinib [WHO-DD]
Common Name English
BMS-907351 free base
Code English
XL-184 FREE BASE
Code English
Cabozantinib [VANDF]
Common Name English
Cabozantinib [MI]
Common Name English
N-(4-((6,7-Dimethoxy-4-quinolinyl)oxy)phenyl)-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide
Systematic Name English
1,1-Cyclopropanedicarboxamide, N?-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N-(4-fluorophenyl)-
Systematic Name English
Cabozantinib [USAN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C1967
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
NCI_THESAURUS C1742
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
FDA ORPHAN DRUG 297109
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
NCI_THESAURUS C129825
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
LIVERTOX NBK548279
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
NDF-RT N0000175605
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
EMA ASSESSMENT REPORTS COMETRIQ (AUTHORIZED: THYROID NEOPLASMS)
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
WHO-ATC L01XE26
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
NCI_THESAURUS C93259
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
FDA ORPHAN DRUG 552916
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
Code System Code Type Description
WIKIPEDIA
Cabozantinib
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
PRIMARY
MERCK INDEX
m11686
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
PRIMARY
USAN
WW-154
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
PRIMARY
DAILYMED
1C39JW444G
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
PRIMARY
DRUG BANK
DB08875
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
PRIMARY
EVMPD
SUB93452
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
PRIMARY
IUPHAR
5887
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
PRIMARY
INN
9297
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
PRIMARY
ChEMBL
CHEMBL2105717
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
PRIMARY
RXCUI
1363268
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
PRIMARY RxNorm
DRUG CENTRAL
4715
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
PRIMARY
NCI_THESAURUS
C52200
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
PRIMARY
FDA UNII
1C39JW444G
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
PRIMARY
PUBCHEM
25102847
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
PRIMARY
LACTMED
Cabozantinib
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
PRIMARY
CAS
849217-68-1
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
PRIMARY
EPA CompTox
DTXSID10233968
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
PRIMARY
SMS_ID
100000141570
Created by admin on Mon Mar 31 19:45:47 GMT 2025 , Edited by admin on Mon Mar 31 19:45:47 GMT 2025
PRIMARY
Related Record Type Details
BDNF/NT-3 GROWTH FACTORS RECEPTOR
TARGET -> INHIBITOR
MRP-2
TRANSPORTER -> SUBSTRATE
MATE-2
TRANSPORTER -> INHIBITOR
IC50
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
MAJOR
VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 1
TARGET -> INHIBITOR
ANGIOPOIETIN-1 RECEPTOR
TARGET -> INHIBITOR
VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2
TARGET -> INHIBITOR
IC50
MULTIDRUG AND TOXIN EXTRUSION PROTEIN 1
TRANSPORTER -> INHIBITOR
IC50
PROTO-ONCOGENE TYROSINE-PROTEIN KINASE RECEPTOR RET V804M
TARGET -> INHIBITOR RESISTANT
IC50
PROTO-ONCOGENE TYROSINE-PROTEIN KINASE RECEPTOR RET M918T
TARGET -> INHIBITOR
IC50
Structure of Cabozantinib Fumarate
SALT/SOLVATE -> PARENT
PROTO-ONCOGENE TYROSINE-PROTEIN KINASE RECEPTOR RET V804L
TARGET -> INHIBITOR RESISTANT
IC50
Structure of Cabozantinib S-malate
SALT/SOLVATE -> PARENT
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
CYTOCHROME P450 1A1
METABOLIC ENZYME -> INDUCER
Inducer of CYP1A1 mRNA; however, the clinical relevance of this finding is unknown. Cabozantinib does not induce CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19 or CYP3A4.
VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 3
TARGET -> INHIBITOR
Structure of Cabozantinib Hydrochloride
SALT/SOLVATE -> PARENT
Related Record Type Details
Structure of METHYL 1-(((4-((6,7-DIMETHOXY-4-QUINOLINYL)OXY)PHENYL)AMINO)CARBONYL)CYCLOPROPANECARBOXYLATE
METABOLITE -> PARENT
PLASMA
Structure of N-(4-((6,7-Dimethoxy-1-oxido-4-quinolinyl)oxy)phenyl)-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide
METABOLITE -> PARENT
MAJOR
PLASMA
Structure of 1-(((4-((6,7-Dimethoxy-4-quinolinyl)oxy)phenyl)amino)carbonyl)cyclopropanecarboxylic acid
METABOLITE -> PARENT
MAJOR
URINE
Structure of N-(4-((6,7-DIMETHOXY-4-QUINOLINYL)OXY)PHENYL)-N'-(4-FLUORO-2-(SULFOOXY)PHENYL)-1,1-CYCLOPROPANEDICARBOXAMIDE
METABOLITE -> PARENT
MAJOR
PLASMA
Structure of DEQUINOLINYL CABOZANTINIB SULFATE
METABOLITE -> PARENT
MAJOR
URINE
Structure of 1-(((4-((7-METHOXY-6-(SULFOOXY)-4-QUINOLINYL)OXY)PHENYL)AMINO)CARBONYL)CYCLOPROPANECARBOXYLIC ACID
METABOLITE -> PARENT
MAJOR
PLASMA
Structure of N-(4-((6,7-DIMETHOXY-4-QUINOLINYL)OXY)PHENYL)-N'-(4-FLUORO-2-HYDROXYPHENYL)-1,1-CYCLOPROPANEDICARBOXAMIDE
METABOLITE -> PARENT
MAJOR
FECAL
Structure of N-(4-FLUOROPHENYL)-N'-(4-((6-HYDROXY-7-METHOXY-4-QUINOLINYL)OXY)PHENYL)-1,1-CYCLOPROPANEDICARBOXAMIDE
METABOLITE -> PARENT
MAJOR
FECAL
Structure of N-(4-((6,7-DIMETHOXY-4-QUINOLINYL)OXY)PHENYL)-N'-(4-FLUORO-3-(SULFOOXY)PHENYL)-1,1-CYCLOPROPANEDICARBOXAMIDE
METABOLITE -> PARENT
FECAL
Structure of 4-(((1-(((4-FLUOROPHENYL)AMINO)CARBONYL)CYCLOPROPYL)CARBONYL)AMINO)PHENYL .BETA.-D-GLUCOPYRANOSIDURONIC ACID
METABOLITE -> PARENT
MAJOR
URINE
Structure of N-(4-((6,7-DIMETHOXY-4-QUINOLINYL)OXY)PHENYL)-N'-(4-FLUORO-3-HYDROXYPHENYL)-1,1-CYCLOPROPANEDICARBOXAMIDE
METABOLITE -> PARENT
FECAL
Related Record Type Details
Structure of Cabozantinib
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC ORAL ADMINISTRATION

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