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

Details

Stereochemistry ACHIRAL
Molecular Formula C21H23N7O2S
Molecular Weight 437.518
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PAZOPANIB

SMILES

CN(C1=CC2=NN(C)C(C)=C2C=C1)C3=CC=NC(NC4=CC(=C(C)C=C4)S(N)(=O)=O)=N3

InChI

InChIKey=CUIHSIWYWATEQL-UHFFFAOYSA-N
InChI=1S/C21H23N7O2S/c1-13-5-6-15(11-19(13)31(22,29)30)24-21-23-10-9-20(25-21)27(3)16-7-8-17-14(2)28(4)26-18(17)12-16/h5-12H,1-4H3,(H2,22,29,30)(H,23,24,25)

HIDE SMILES / InChI
Molecular Formula C21H23N7O2S
Molecular Weight 437.518
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://adisinsight.springer.com/drugs/800016874 | https://www.ncbi.nlm.nih.gov/pubmed/26767042 | https://www.ncbi.nlm.nih.gov/pubmed/17620431

Pazopanib (VOTRIENT) is an orally bioavailable multi-targeted tyrosine kinase receptor inhibitor. Pazopanib inhibits vascular endothelial growth factor receptor (VEGFR)-1, VEGFR-2, VEGFR-3, platelet-derived growth factor receptor (PDGFR)-α and -β, fibroblast growth factor receptor (FGFR) -1 and -3, cytokine receptor (Kit), interleukin-2 receptor inducible T-cell kinase (Itk), leukocyte-specific protein tyrosine kinase (Lck), and transmembrane glycoprotein receptor tyrosine kinase (c-Fms). In an vitro study, pazopanib exerted anti-tumor effect through mechanisms including the Raf-MAPK/ERK (MEK)-extracellular signal-regulated kinase (ERK) pathway. It has good oral exposure and inhibits angiogenesis and tumor growth in mice. Pazopanib (VOTRIENT) was developed by GlaxoSmithKline for the treatment of solid tumours and age-related macular degeneration. However, Novartis acquired all the rights to the drug from GlaxoSmithKline. Pazopanib (VOTRIENT) is indicated for the treatment of patients with advanced renal cell carcinoma and advanced soft tissue sarcoma.

CNS Activity

Originator

Approval Year

2009
364
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8504
 0.14 µM [IC50]
Inhibitor
8504
 0.13 µM [IC50]
Inhibitor
8504
 0.146 µM [IC50]
Inhibitor
8504
 0.071 µM [IC50]
Inhibitor
8504
 0.084 µM [IC50]
Inhibitor
8504
 0.074 µM [IC50]
Inhibitor
8504
 0.43 µM [IC50]
Inhibitor
8504
 0.411 µM [IC50]
Inhibitor
8504
 0.01 µM [IC50]
Inhibitor
8504
 0.03 µM [IC50]
Inhibitor
8504
 0.047 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
VOTRIENT

Approved Use

VOTRIENT® is indicated for the treatment of patients with advanced renal cell carcinoma (RCC). VOTRIENT is indicated for the treatment of patients with advanced soft tissue sarcoma (STS) who have received prior chemotherapy. Limitation of Use: The efficacy of VOTRIENT for the treatment of patients with adipocytic STS or gastrointestinal stromal tumors has not been demonstrated. VOTRIENT is a kinase inhibitor indicated for the treatment of patients with: •advanced renal cell carcinoma. (1) •advanced soft tissue sarcoma who have received prior chemotherapy. (1) Limitation of Use: The efficacy of VOTRIENT for the treatment of patients with adipocytic soft tissue sarcoma or gastrointestinal stromal tumors has not been demonstrated.

Launch Date

2009
Primary
Approved
8583
VOTRIENT

Approved Use

VOTRIENT® is indicated for the treatment of patients with advanced renal cell carcinoma (RCC). VOTRIENT is indicated for the treatment of patients with advanced soft tissue sarcoma (STS) who have received prior chemotherapy. Limitation of Use: The efficacy of VOTRIENT for the treatment of patients with adipocytic STS or gastrointestinal stromal tumors has not been demonstrated. VOTRIENT is a kinase inhibitor indicated for the treatment of patients with: •advanced renal cell carcinoma. (1) •advanced soft tissue sarcoma who have received prior chemotherapy. (1) Limitation of Use: The efficacy of VOTRIENT for the treatment of patients with adipocytic soft tissue sarcoma or gastrointestinal stromal tumors has not been demonstrated.

Launch Date

2009
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
58.1 μg/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022465lbl.pdf
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PAZOPANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
44.8 mg/L
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/31125423
800 mg 1 times / day multiple, oral
dose: 800 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
PAZOPANIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
50.2 mg/L
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/31125423
600 mg 1 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
PAZOPANIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1037 μg × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022465lbl.pdf
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
PAZOPANIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
821 mg × h/L
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/31125423
800 mg 1 times / day multiple, oral
dose: 800 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
PAZOPANIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
895 mg × h/L
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/31125423
600 mg 1 times / day multiple, oral
dose: 600 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
PAZOPANIB blood
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/022465s-010S-012lbl.pdf
PAZOPANIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
PAZOPANIB
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
PAZOPANIB
Disc. AE: Proteinuria...
AEs leading to
discontinuation/dose reduction:
Proteinuria (5 patients)
Sources:
PAZOPANIB
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Disc. AE: ALT increased, AST increased...
AEs leading to
discontinuation/dose reduction:
ALT increased (11 patient)
AST increased (11 patient)
Bilirubin increased (11 patient)
Myocardial infarction (6 patients)
Ischemic stroke (6 patients)
Transient ischemic attack (6 patients)
Fatigue (5 patients)
Diarrhea (7 patients)
Anorexia (7 patients)
Vomiting (7 patients)
Proteinuria (3 patients)
Hypertension (2 patients)
Hemorrhage (2 patients)
Confusion (12 patients)
Infection (12 patients)
Hand-and-foot syndrome (12 patients)
Edema (12 patients)
Dehydration (12 patients)
Anemia (12 patients)
Anxiety (12 patients)
Convulsion (12 patients)
Atrial fibrillation (12 patients)
Hypertension (20 patients)
Gastrointestinal disturbance (17 patients)
Liver function test abnormal (16 patients)
Fatigue (10 patients)
Hematologic disorder (4 patients)
Rash (5 patients)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
DLT: Neutropenia, Aspartate aminotransferase increased...
Other AEs: Diarrhea, Hypertension...
Dose limiting toxicities:
Neutropenia (grade 2, 1 patient)
Aspartate aminotransferase increased (grade 2, 1 patient)
Hyperbilirubinemia (grade 2, 1 patient)
Other AEs:
Diarrhea (all grades, 50%)
Hypertension (grade 3, 13%)
AST increased (grade 3, 13%)
ALT increased (all grades, 25%)
Cough (all grades, 13%)
Skin hypopigmentation (all grades, 50%)
Weight decrease (all grades, 25%)
Alopecia (all grades, 13%)
Dizziness (all grades, 13%)
Hyperbilirubinemia (all grades, 25%)
Abdominal distension (all grades, 25%)
Abdominal pain (all grades, 25%)
Fatigue (all grades, 13%)
Leukopenia (all grades, 13%)
Muscle spasms (all grades, 25%)
Upper respiratory tract infection (all grades, 13%)
Hypercholesterolemia (grade 3, 13%)
Gastrointestinal hemorrhage (grade 4, 13%)
Hypoglycemia (grade 4, 13%)
Transaminases increased (grade 4, 13%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
800 mg 1 times / day multiple, oral
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
DLT: Aspartate aminotransferase increase, Malaise...
Dose limiting toxicities:
Aspartate aminotransferase increase (grade 3, 2 patients)
Malaise (grade 3, 2 patients)
ALT increased (grade 3, 2 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022465lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022465lbl.pdf
Other AEs: Hepatotoxicity...
Other AEs:
Hepatotoxicity (severe|grade 5)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022465lbl.pdf
2000 mg 1 times / day multiple, oral
Highest studied dose
Dose: 2000 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2000 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022465lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022465lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
DLT: Fatigue...
Dose limiting toxicities:
Fatigue (grade 3, 1 patient)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022465lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
1000 mg 1 times / day multiple, oral
Dose: 1000 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1000 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022465lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022465lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
DLT: Hypertension...
Dose limiting toxicities:
Hypertension (grade 3, 1 patient)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022465lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
AEs

AEs

AESignificanceDosePopulation
Proteinuria 5 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
PAZOPANIB
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
PAZOPANIB
Fatigue 10 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
ALT increased 11 patient
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
AST increased 11 patient
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Bilirubin increased 11 patient
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Anemia 12 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Anxiety 12 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Atrial fibrillation 12 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Confusion 12 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Convulsion 12 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Dehydration 12 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Edema 12 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Hand-and-foot syndrome 12 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Infection 12 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Liver function test abnormal 16 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Gastrointestinal disturbance 17 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Hemorrhage 2 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Hypertension 2 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Hypertension 20 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Proteinuria 3 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Hematologic disorder 4 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Fatigue 5 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Rash 5 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Ischemic stroke 6 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Myocardial infarction 6 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Transient ischemic attack 6 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Anorexia 7 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Diarrhea 7 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Vomiting 7 patients
Disc. AE
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy, 59 years
Health Status: unhealthy
Age Group: 59 years
Sex: M+F
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Alopecia all grades, 13%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Cough all grades, 13%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Dizziness all grades, 13%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Fatigue all grades, 13%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Leukopenia all grades, 13%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Upper respiratory tract infection all grades, 13%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
ALT increased all grades, 25%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Abdominal distension all grades, 25%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Abdominal pain all grades, 25%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Hyperbilirubinemia all grades, 25%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Muscle spasms all grades, 25%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Weight decrease all grades, 25%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Diarrhea all grades, 50%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Skin hypopigmentation all grades, 50%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Aspartate aminotransferase increased grade 2, 1 patient
DLT
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Hyperbilirubinemia grade 2, 1 patient
DLT
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Neutropenia grade 2, 1 patient
DLT
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
AST increased grade 3, 13%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Hypercholesterolemia grade 3, 13%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Hypertension grade 3, 13%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Gastrointestinal hemorrhage grade 4, 13%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Hypoglycemia grade 4, 13%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Transaminases increased grade 4, 13%
600 mg 1 times / day multiple, oral
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
ALT increased grade 3, 2 patients
DLT
800 mg 1 times / day multiple, oral
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Aspartate aminotransferase increase grade 3, 2 patients
DLT
800 mg 1 times / day multiple, oral
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Malaise grade 3, 2 patients
DLT
800 mg 1 times / day multiple, oral
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
unhealthy, 61 years (range: 38–76 years)
Health Status: unhealthy
Age Group: 61 years (range: 38–76 years)
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/21831954
Hepatotoxicity severe|grade 5
800 mg 1 times / day multiple, oral
Recommended
Dose: 800 mg, 1 times / day
Route: oral
Route: multiple
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022465lbl.pdf
unhealthy, adult
Health Status: unhealthy
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022465lbl.pdf
Fatigue grade 3, 1 patient
DLT, Disc. AE
2000 mg 1 times / day multiple, oral
Highest studied dose
Dose: 2000 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2000 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022465lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022465lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Hypertension grade 3, 1 patient
DLT, Disc. AE
1000 mg 1 times / day multiple, oral
Dose: 1000 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1000 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022465lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
unhealthy
Health Status: unhealthy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2009/022465lbl.pdf
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_MedR.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1946

inhibitor
2252

inducer
1087
inhibitor
2438
inhibitor
2507
inhibitor
2217

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
2153

CYP2B6
926

CYP2C8
1057

CYP2C19
2057

CYP2E1
1060

P-gp
1741

UGT1A1
246

OATP1B1
1079
CYP1A2
1197

CYP2C8
810

P-gp
2052
CYP2B6
669

CYP1A2
832
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP2C8
1117
 moderate [IC50 10 uM]
weak (co-administration study)
Comment: AUC of paclitaxel (CYP3A4 and CYP2C8 substrate) increased by 26%, decreased paclitaxel clearance by 14%, and increased paclitaxel Cmax by 31%;
Page: 32.0
CYP2C19
2141
 moderate [IC50 11 uM]
no (co-administration study)
Comment: no effect
Page: 32,36
CYP3A4
2633
 moderate [IC50 11 uM]
weak (co-administration study)
Comment: pazopanib increased the AUC of CYP3A4 substrate (midazolam) by 32%; AUC of paclitaxel (CYP3A4 and CYP2C8 substrate) increased by 26%, decreased paclitaxel clearance by 14%, and increased paclitaxel Cmax by 31%;
Page: 33,37
CYP2B6
1160
 moderate [IC50 15 uM]
CYP1A2
2333
 moderate [IC50 16 uM]
no (co-administration study)
Comment: no effect
Page: 32,36
CYP2E1
1146
 moderate [IC50 17 uM]
CYP2D6
2546
 moderate [IC50 18 uM]
yes (co-administration study)
Comment: increased the AUC of CYP2D6 substrate (dextromethorphan) by 64%
Page: 32,37
CYP2C9
2497
 moderate [IC50 7.9 uM]
no (co-administration study)
Comment: no effect
Page: 32,36
CYP2B6
1160
 moderate
CYP3A4
2633
 moderate
weak (co-administration study)
Comment: pazopanib increased the AUC of CYP3A4 substrate (midazolam) by 32%; AUC of paclitaxel (CYP3A4 and CYP2C8 substrate) increased by 26%, decreased paclitaxel clearance by 14%, and increased paclitaxel Cmax by 31%;
Page: 32,33,37
CYP1A2
2333
 no
P-gp
1932
 no
OATP1B1
1095
 yes [IC50 0.79 uM]
UGT1A1
303
 yes [IC50 1.2 uM]
yes (pharmacogenomic study)
Comment: Certain UGT1A1 genotypes are associated with an increase in the risk of pazopanib induced hyperbilirubinemia.
Page: 34,4
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP3A4
1946
 major
yes (co-administration study)
Comment: pazopanib AUC (0-t), Cmax, and half-life were increased 1.47, 2.21, and 2.81 fold, respectively;
Page: 32,35
CYP1A2
1197
 minor
CYP2C8
810
 minor
P-gp
2052
 yes
yes (co-administration study)
Comment: AUC(0-t) and Cmax values of pazopanib are increased by 59 and 50%, respectively, when coadministered with lapatinib;
Page: 34,35
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
2263
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:71219
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:71219
eMolecules
30151586
https://www.emolecules.com/cgi-bin/more?vid=30151586
MolPort
MolPort-006-827-156
https://www.molport.com/shop/molecule-link/MolPort-006-827-156
Selleck Chemicals
pazopanib
http://www.selleckchem.com/products/pazopanib.html
ZINC
ZINC000011617039
http://zinc15.docking.org/substances/ZINC000011617039
PubMed

PubMed

TitleDatePubMed
Recent advances in the therapy of renal cancer.
2007 Feb
Pazopanib: a novel multitargeted tyrosine kinase inhibitor.
2007 Mar
Novel therapies in genitourinary cancer: an update.
2008 Aug 11
New drugs for ovarian cancer.
2008 Feb
Novel drugs for renal cell carcinoma.
2008 Oct
Signaling inhibitors in metastatic renal cell carcinoma.
2008 Sep-Oct
Targeted therapy in the treatment of metastatic renal cell cancer.
2009
Suppression and regression of choroidal neovascularization by the multitargeted kinase inhibitor pazopanib.
2009 Apr
VEGFR1 activity modulates myeloid cell infiltration in growing lung metastases but is not required for spontaneous metastasis formation.
2009 Sep 18
Targeting angiogenesis with multitargeted tyrosine kinase inhibitors in the treatment of non-small cell lung cancer.
2010
Antiangiogenic therapy and mechanisms of tumor resistance in malignant glioma.
2010
Phase II trial of pazopanib (GW786034), an oral multi-targeted angiogenesis inhibitor, for adults with recurrent glioblastoma (North American Brain Tumor Consortium Study 06-02).
2010 Aug
Plethora of agents, plethora of targets, plethora of side effects in metastatic renal cell carcinoma.
2010 Aug
Analytical control of process impurities in Pazopanib hydrochloride by impurity fate mapping.
2010 Aug 1
Pazopanib in locally advanced or metastatic renal cell carcinoma: results of a randomized phase III trial.
2010 Feb 20
StatBite: FDA oncology drug product approvals in 2009.
2010 Feb 24
Molecular basis for the treatment of renal cell carcinoma.
2010 Jan
An exploratory study of sunitinib plus paclitaxel as first-line treatment for patients with advanced breast cancer.
2010 Jul
[Antiangionic drugs in soft tissue sarcoma].
2010 Jun
Pazopanib: a multikinase inhibitor with activity in advanced renal cell carcinoma.
2010 May
Targeted therapy and hand-foot skin reaction in advanced renal cell carcinoma.
2010 May
The complexity of the complicity of mast cells in cancer.
2010 May
Antitumor and antiangiogenic effect of the dual EGFR and HER-2 tyrosine kinase inhibitor lapatinib in a lung cancer model.
2010 May 11
Growth factors in multiple myeloma: a comprehensive analysis of their expression in tumor cells and bone marrow environment using Affymetrix microarrays.
2010 May 13
Patents

Patents

20040242578
3
JP2011528326A
17
JP2013536243A
5
JP2013537228A
5

Sample Use Guides

In Vivo Use Guide
800 mg orally once daily without food (at least 1 hour before or 2 hours after a meal). Baseline moderate hepatic impairment – 200 mg orally once daily. Not recommended in patients with severe hepatic impairment.
Route of Administration: Oral
In Vitro Use Guide
Treatment of the KATO-III, OCUM-2M, SNU-16, and HSC-39 gastric cancer cell lines harboring FGFR2 amplification with pazopanib resulted in marked decreases of cell survival with IC50 in ranges of 0.1 to 2.0 uM, whereas the same treatment of those cell lines without FGFR2 amplification had no growth-inhibitory effects
Substance Class Chemical
Created
by admin
on Wed Apr 02 06:59:08 GMT 2025
Edited
by admin
on Wed Apr 02 06:59:08 GMT 2025
Record UNII
7RN5DR86CK
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
GW786034
Preferred Name English
PAZOPANIB
DASH   EMA EPAR   INN   MI   VANDF   WHO-DD  
INN  
Official Name English
PAZOPANIB [VANDF]
Common Name English
PAZOPANIB [EMA EPAR]
Common Name English
5-((4-((2,3-DIMETHYL-2H-INDAZOL-6-YL)(METHYL)AMINO)PYRIMIDIN-2-YL)AMINO)-2-METHYLBENZENESULFONAMIDE
Systematic Name English
pazopanib [INN]
Common Name English
PAZOPANIB [MI]
Common Name English
BENZENESULFONAMIDE, 5-((4-((2,3-DIMETHYL-2H-INDAZOL-6-YL)METHYLAMINO)-2-PYRIMIDINYL)AMINO)-2-METHYL-
Systematic Name English
Pazopanib [WHO-DD]
Common Name English
NSC-752782
Code English
Classification Tree Code System Code
FDA ORPHAN DRUG 705819
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
NCI_THESAURUS C1967
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
EMA ASSESSMENT REPORTS VOTRIENT (AUTHORIZED: CARCINOMA, RENAL CELL)
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
FDA ORPHAN DRUG 383912
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
WHO-ATC L01XE11
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
WHO-VATC QL01XE11
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
LIVERTOX NBK548110
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
NCI_THESAURUS C1742
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
NDF-RT N0000175605
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
FDA ORPHAN DRUG 293809
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
Code System Code Type Description
EVMPD
SUB29175
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
PRIMARY
ChEMBL
CHEMBL477772
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
PRIMARY
PUBCHEM
10113978
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
PRIMARY
NDF-RT
N0000182137
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
PRIMARY Cytochrome P450 2D6 Inhibitors [MoA]
HSDB
8210
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
PRIMARY
WIKIPEDIA
PAZOPANIB
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
PRIMARY
MESH
C516667
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
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DRUG CENTRAL
4118
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
PRIMARY
NDF-RT
N0000182141
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
PRIMARY Cytochrome P450 3A4 Inhibitors [MoA]
NDF-RT
N0000187062
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
PRIMARY Cytochrome P450 2C8 Inhibitors [MoA]
RXCUI
714438
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
PRIMARY RxNorm
NSC
752782
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
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CAS
444731-52-6
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
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EPA CompTox
DTXSID8048733
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
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MERCK INDEX
m8430
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
PRIMARY Merck Index
CHEBI
71219
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
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LACTMED
Pazopanib
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
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FDA UNII
7RN5DR86CK
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
PRIMARY
SMS_ID
100000090733
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
PRIMARY
DAILYMED
7RN5DR86CK
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
PRIMARY
DRUG BANK
DB06589
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
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INN
8681
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
PRIMARY
IUPHAR
5698
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
PRIMARY
NCI_THESAURUS
C74547
Created by admin on Wed Apr 02 06:59:08 GMT 2025 , Edited by admin on Wed Apr 02 06:59:08 GMT 2025
PRIMARY
Related Record Type Details
VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2
TARGET -> INHIBITOR
Structure of PAZOPANIB HYDROCHLORIDE MONOHYDRATE
SALT/SOLVATE -> PARENT
OATP1B1
TRANSPORTER -> SUBSTRATE
Structure of PAZOPANIB HYDROCHLORIDE
SALT/SOLVATE -> PARENT
Related Record Type Details
Structure of GSK-1268992
METABOLITE INACTIVE -> PARENT
LESS THAN 10%
PLASMA
Structure of GSK-1071306
METABOLITE INACTIVE -> PARENT
In plasma and blood, individual circulating metabolites represented less than 10% total radioactivity
PLASMA
Structure of GSK-1268997
METABOLITE ACTIVE -> PARENT
Only one of these metabolites (GSK1268997) has been shown to inhibit the proliferation of VEGF-stimulated human umbilical vein endothelial cells with potency similar to pazopanib. The other metabolites show at least 10- to 20-fold less activity than the parent compound in the same cellular assay.
Structure of GSK-1268992
METABOLITE INACTIVE -> PARENT
FECAL
Structure of GSK-1268997
METABOLITE ACTIVE -> PARENT
The majority of radiolabeled material recovered in feces constituted unchanged pazopanib, accounting for a mean of 67% of the administered radioactivity activity dose. Pazopanib metabolites GSK1268992 and GSK1268997 accounted for means of approximately 6% and 2% of the administered radioactivity dose, respectively.
FECAL
Structure of GSK-1268997
METABOLITE ACTIVE -> PARENT
Renal elimination of pazopanib is accounted for less than 4% of bodily excretion of the administered dose (Table 9). The majority of the radioactivity (82.2%) was recovered in feces by 120 hours (Table 9). Pazopanib undergoes moderate liver metabolism.
FECAL; PLASMA; URINE
Structure of GSK-1268992
METABOLITE INACTIVE -> PARENT
Four pazopanib metabolites (GSK1268992, GSK1268997, GSK1071306, and GW700201) have been identified. Only one of these metabolites (GSK1268997) has been shown to inhibit the proliferation of VEGF-stimulated human umbilical vein endothelial cells with potency similar to pazopanib. The other metabolites show at least 10- to 20-fold less activity than the parent compound in the same cellular assay.
Structure of GSK-1268992
METABOLITE INACTIVE -> PARENT
Renal elimination of pazopanib is accounted for less than 4% of bodily excretion of the administered dose (Table 9). The majority of the radioactivity (82.2%) was recovered in feces by 120 hours (Table 9). Pazopanib undergoes moderate liver metabolism. Pazopanib was the major drug-related component in human plasma representing 84% and 91% of the AUC(0-∞) in two of the three subjects that received 400 mg radiolabeled pazopanib.
FECAL; PLASMA; URINE
Structure of GSK-1071306
METABOLITE INACTIVE -> PARENT
Four pazopanib metabolites (GSK1268992, GSK1268997, GSK1071306, and GW700201) have been identified. Only one of these metabolites (GSK1268997) has been shown to inhibit the proliferation of VEGF-stimulated human umbilical vein endothelial cells with potency similar to pazopanib.
Related Record Type Details
Structure of PAZOPANIB
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Structure of PAZOPANIB
Elimination
PHARMACOKINETIC
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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