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Details

Stereochemistry ACHIRAL
Molecular Formula C28H24FN3O5
Molecular Weight 501.5067
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CABOZANTINIB

SMILES

COc1cc2c(cc1OC)nccc2Oc3ccc(cc3)NC(=O)C4(CC4)C(=O)Nc5ccc(cc5)F

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 501.5067
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment:: 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

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

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P07949
Gene ID: 5979
Gene Symbol: RET
Target Organism: Homo sapiens (Human)
5.20000000000000018 nM [IC50]
Target ID: P08581
Gene ID: 4233
Gene Symbol: MET
Target Organism: Homo sapiens (Human)
1.30000000000000004 nM [IC50]
Target ID: P35968
Gene ID: 3791
Gene Symbol: KDR
Target Organism: Homo sapiens (Human)
0.0350000000000000033 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Secondary
COMETRIQ

Approved Use

Indicated for the treatment of patients with progressive, metastatic medullary thyroid cancer (MTC)

Launch Date

1354147200000
Primary
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

1354060800000
Primary
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

1461456000000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
554 ng/mL
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
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
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%
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
Other AEs: Mucositis...
Other AEs:
Mucositis (grade 2, 20%)
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
175 mg 1 times / day multiple, oral
Dose: 175 mg, 1 times / day
Route: oral
Route: multiple
Dose: 175 mg, 1 times / day
Sources:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
Other AEs: Pulmonary embolism...
Other AEs:
Pulmonary embolism (grade 4)
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
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:
unhealthy, median age 64.8 years
Disc. AE: Large intestine perforation, Intracranial hemorrhage...
AEs leading to
discontinuation/dose reduction:
Large intestine perforation (7.7%)
Intracranial hemorrhage (7.7%)
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
200 mg 1 times / day multiple, oral
Dose: 200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 200 mg, 1 times / day
Sources:
unhealthy
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:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 56 years
Health Status: unhealthy
Age Group: median age 56 years
Sex: M+F
Sources:
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:
unhealthy, median age 64.8 years
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:
unhealthy, median age 64.8 years
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy, median age of 62.5 years
Health Status: unhealthy
Age Group: median age of 62.5 years
Sex: M+F
Sources:
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
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:
unhealthy
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no
yes [IC50 7 uM]
yes [IC50 >20 uM]
yes [Ki 10.4 uM]
yes [Ki 28.8 uM]
yes [Ki 282 uM]
yes [Ki 4.6 uM]
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
yes [IC50 3.2 uM]
yes [IC50 5.94 uM]
yes
yes
no (co-administration study)
Comment: Inhibition of CYP2C9 had a minimal effect on cabozantinib metabolite formation (i.e., a <20% reduction).
Page: -
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
PubMed

PubMed

TitleDatePubMed
Cabozantinib versus Everolimus in Advanced Renal-Cell Carcinoma.
2015 Nov 5
Patents

Sample Use Guides

Recommended Dose: 140 mg orally, once daily
Route of Administration: Oral
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 Fri Jun 25 21:41:10 UTC 2021
Edited
by admin
on Fri Jun 25 21:41:10 UTC 2021
Record UNII
1C39JW444G
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
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
BMS-907351 FREE BASE
Code English
XL-184 FREE BASE
Code English
CABOZANTINIB [VANDF]
Common Name English
CABOZANTINIB [WHO-DD]
Common Name English
CABOZANTINIB [INN]
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
FDA ORPHAN DRUG 552916
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
NCI_THESAURUS C1967
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
NCI_THESAURUS C1742
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
FDA ORPHAN DRUG 297109
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
NCI_THESAURUS C129825
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
LIVERTOX 136
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
NDF-RT N0000175605
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
EMA ASSESSMENT REPORTS COMETRIQ (AUTHORIZED: THYROID NEOPLASMS)
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
WHO-ATC L01XE26
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
NCI_THESAURUS C93259
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
Code System Code Type Description
WIKIPEDIA
Cabozantinib
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
PRIMARY
MERCK INDEX
M11686
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
PRIMARY
DRUG BANK
DB08875
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
PRIMARY
EVMPD
SUB93452
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
PRIMARY
IUPHAR
5887
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
PRIMARY
INN
9297
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
PRIMARY
ChEMBL
CHEMBL2105717
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
PRIMARY
RXCUI
1363268
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
PRIMARY RxNorm
DRUG CENTRAL
4715
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
PRIMARY
NCI_THESAURUS
C52200
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
PRIMARY
FDA UNII
1C39JW444G
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
PRIMARY
PUBCHEM
25102847
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
PRIMARY
LACTMED
Cabozantinib
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
PRIMARY
CAS
849217-68-1
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
PRIMARY
EPA CompTox
849217-68-1
Created by admin on Fri Jun 25 21:41:10 UTC 2021 , Edited by admin on Fri Jun 25 21:41:10 UTC 2021
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
TRANSPORTER -> SUBSTRATE
TARGET -> INHIBITOR
TRANSPORTER -> INHIBITOR
IC50
TARGET -> INHIBITOR
TARGET -> INHIBITOR
TRANSPORTER -> INHIBITOR
IC50
SALT/SOLVATE -> PARENT
BINDER->LIGAND
BINDING
TARGET -> INHIBITOR
Related Record Type Details
METABOLITE -> PARENT
PLASMA
METABOLITE -> PARENT
MAJOR
PLASMA
METABOLITE -> PARENT
MAJOR
URINE
METABOLITE -> PARENT
MAJOR
PLASMA
METABOLITE -> PARENT
MAJOR
URINE
METABOLITE -> PARENT
MAJOR
PLASMA
METABOLITE -> PARENT
MAJOR
FECAL
METABOLITE -> PARENT
MAJOR
FECAL
METABOLITE -> PARENT
FECAL
METABOLITE -> PARENT
MAJOR
URINE
METABOLITE -> PARENT
FECAL
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
Tmax PHARMACOKINETIC ORAL ADMINISTRATION