U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C21H23N7O2S.ClH.H2O
Molecular Weight 491.994
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PAZOPANIB HYDROCHLORIDE MONOHYDRATE

SMILES

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

InChI

InChIKey=RGKFSIOGIJNWPQ-UHFFFAOYSA-N
InChI=1S/C21H23N7O2S.ClH.H2O/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);1H;1H2

HIDE SMILES / InChI
Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
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
Molecular Formula H2O
Molecular Weight 18.0153
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
Analytical control of process impurities in Pazopanib hydrochloride by impurity fate mapping.
2010-08-01
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).
2010-08
Plethora of agents, plethora of targets, plethora of side effects in metastatic renal cell carcinoma.
2010-08
An exploratory study of sunitinib plus paclitaxel as first-line treatment for patients with advanced breast cancer.
2010-07
[Antiangionic drugs in soft tissue sarcoma].
2010-06
Pazopanib: an oral multitargeted tyrosine kinase inhibitor for use in renal cell carcinoma.
2010-06
Current status of vascular endothelial growth factor inhibition in age-related macular degeneration.
2010-06
Bevacizumab salvage therapy following progression in high-grade glioma patients treated with VEGF receptor tyrosine kinase inhibitors.
2010-06
Growth factors in multiple myeloma: a comprehensive analysis of their expression in tumor cells and bone marrow environment using Affymetrix microarrays.
2010-05-13
Antitumor and antiangiogenic effect of the dual EGFR and HER-2 tyrosine kinase inhibitor lapatinib in a lung cancer model.
2010-05-11
Initial assessment, surveillance, and management of blood pressure in patients receiving vascular endothelial growth factor signaling pathway inhibitors.
2010-05-05
Everolimus and pazopanib: two new drugs for renal cell cancer.
2010-05-03
Pazopanib: a multikinase inhibitor with activity in advanced renal cell carcinoma.
2010-05
Targeted therapy and hand-foot skin reaction in advanced renal cell carcinoma.
2010-05
The complexity of the complicity of mast cells in cancer.
2010-05
Pazopanib-induced hyperbilirubinemia is associated with Gilbert's syndrome UGT1A1 polymorphism.
2010-04-27
New therapeutic strategies for renal cell carcinoma.
2010-04-03
Potent preclinical impact of metronomic low-dose oral topotecan combined with the antiangiogenic drug pazopanib for the treatment of ovarian cancer.
2010-04
Bridging the gap between cytotoxic and biologic therapy with metronomic topotecan and pazopanib in ovarian cancer.
2010-04
Plasma cytokine and angiogenic factor profiling identifies markers associated with tumor shrinkage in early-stage non-small cell lung cancer patients treated with pazopanib.
2010-03-15
Recent advances and future directions in the management of metastatic renal cell carcinoma.
2010-03
[Management of metastatic HER2-positive breast cancer: present and future].
2010-03
Anti-angiogenic tyrosine kinase inhibitors: what is their mechanism of action?
2010-03
StatBite: FDA oncology drug product approvals in 2009.
2010-02-24
Pazopanib in locally advanced or metastatic renal cell carcinoma: results of a randomized phase III trial.
2010-02-20
Prognostic stratification of patients with advanced renal cell carcinoma treated with sunitinib: comparison with the Memorial Sloan-Kettering prognostic factors model.
2010-02-18
Prognostic factors in patients treated with VEGF-targeted therapies.
2010-02
Noninvasive assessment of tumor VEGF receptors in response to treatment with pazopanib: a molecular imaging study.
2010-02
Angiogenesis inhibitors in the management of breast cancer.
2010-02
Anti-angiogenesis agents in metastatic or recurrent cervical cancer.
2010-02
Efficacy and safety of pazopanib in patients with metastatic renal cell carcinoma.
2010-01-20
New weapons against kidney cancer. Two recent drug options appear to extend survival for kidney cancer patients who can't tolerate existing medications.
2010-01
Molecular basis for the treatment of renal cell carcinoma.
2010-01
Pazopanib.
2010-01
VEGF signalling inhibition-induced proteinuria: Mechanisms, significance and management.
2010-01
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
Everolimus (RAD001) in the treatment of advanced renal cell carcinoma: a review.
2010
Anticancer Role of PPARgamma Agonists in Hematological Malignancies Found in the Vasculature, Marrow, and Eyes.
2010
Targeting signal transduction pathways in metastatic breast cancer: a comprehensive review.
2010
Targeted therapies in epithelial ovarian cancer.
2010
A current review of targeted therapeutics for ovarian cancer.
2010
Major clinical research advances in gynecologic cancer 2009.
2009-12
Impact of anti-angiogenic treatments on metastatic renal cell carcinoma.
2009-12
Pazopanib: therapeutic developments.
2009-12
Tyrosine kinase inhibitors and the thyroid.
2009-12
Selective inhibition of retinal angiogenesis by targeting PI3 kinase.
2009-11-17
Pazopanib: an antiangiogenic drug in perspective.
2009-11
Pazopanib for the treatment of renal cell carcinoma and other malignancies.
2009-09
Targeted therapy in the treatment of metastatic renal cell cancer.
2009
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 17:20:30 GMT 2025
Edited
by admin
on Wed Apr 02 17:20:30 GMT 2025
Record UNII
HH55AX8FNP
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PAZOPANIB HYDROCHLORIDE MONOHYDRATE
Common Name English
Benzenesulfonamide, 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-, hydrochloride, hydrate (1:1:1)
Preferred Name English
5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)(methyl)amino]pyrimidin-2-yl]amino]-2-methylbenzenesulfonamide hydrochloride monohydrate
Systematic Name English
Code System Code Type Description
CAS
635702-66-8
Created by admin on Wed Apr 02 17:20:30 GMT 2025 , Edited by admin on Wed Apr 02 17:20:30 GMT 2025
PRIMARY
FDA UNII
HH55AX8FNP
Created by admin on Wed Apr 02 17:20:30 GMT 2025 , Edited by admin on Wed Apr 02 17:20:30 GMT 2025
PRIMARY
PUBCHEM
49872085
Created by admin on Wed Apr 02 17:20:30 GMT 2025 , Edited by admin on Wed Apr 02 17:20:30 GMT 2025
PRIMARY
Related Record Type Details
Structure of PAZOPANIB HYDROCHLORIDE
ANHYDROUS->SOLVATE
Structure of PAZOPANIB
PARENT -> SALT/SOLVATE
Related Record Type Details
Structure of PAZOPANIB
ACTIVE MOIETY
NIH
NCATS
PRIVACY NOTICE
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966