PAZOPANIB

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 Search

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
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/022465s-010S-012lbl.pdf
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

Targets

Primary Target	Pharmacology	Potency
Fibroblast growth factor receptor 1 46 Target ID: CHEMBL3650 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17620431/	Inhibitor 8504	0.14 µM [IC50]
Fibroblast growth factor receptor 3 32 Target ID: CHEMBL2742 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17620431/	Inhibitor 8504	0.13 µM [IC50]
Macrophage colony stimulating factor receptor 24 Target ID: CHEMBL1844 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17620431/	Inhibitor 8504	0.146 µM [IC50]
Platelet-derived growth factor receptor alpha 33 Target ID: CHEMBL2007 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17620431/	Inhibitor 8504	0.071 µM [IC50]
Platelet-derived growth factor receptor beta 56 Target ID: CHEMBL1913 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17620431/	Inhibitor 8504	0.084 µM [IC50]
Stem cell growth factor receptor 57 Target ID: CHEMBL1936 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17620431/	Inhibitor 8504	0.074 µM [IC50]
Tyrosine-protein kinase ITK/TSK 4 Target ID: CHEMBL2959 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17620431/	Inhibitor 8504	0.43 µM [IC50]
Tyrosine-protein kinase LCK 14 Target ID: CHEMBL258 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17620431/	Inhibitor 8504	0.411 µM [IC50]
Vascular endothelial growth factor receptor 1 44 Target ID: CHEMBL1868 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17620431/	Inhibitor 8504	0.01 µM [IC50]
Vascular endothelial growth factor receptor 2 112 Target ID: CHEMBL279 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17620431/	Inhibitor 8504	0.03 µM [IC50]
Vascular endothelial growth factor receptor 3 41 Target ID: CHEMBL1955 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17620431/	Inhibitor 8504	0.047 µM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Renal cell carcinoma 33 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/022465s-010S-012lbl.pdf https://www.ncbi.nlm.nih.gov/pubmed/22341567	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
Soft tissue sarcoma 10 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/022465s-010S-012lbl.pdf https://www.ncbi.nlm.nih.gov/pubmed/23488774	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

C_max

Value	Dose	Analyte	Population
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

Value	Dose	Analyte	Population
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

F_unbound

Value	Dose	Co-administered	Analyte	Population
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

Dose	Population	Adverse 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

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inhibitor 2252 inducer 1087	inhibitor 2438	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other 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

Target	Modality	Activity	Clinical evidence
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32.0	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%; Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32.0
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32,36	moderate [IC50 11 uM]	no (co-administration study) Comment: no effect Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32,36
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=33 Page: 33,37	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%; Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=33 Page: 33,37
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32.0	moderate [IC50 15 uM]
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32,36	moderate [IC50 16 uM]	no (co-administration study) Comment: no effect Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32,36
CYP2E1 1146	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32.0	moderate [IC50 17 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32,37	moderate [IC50 18 uM]	yes (co-administration study) Comment: increased the AUC of CYP2D6 substrate (dextromethorphan) by 64% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32,37
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32,36	moderate [IC50 7.9 uM]	no (co-administration study) Comment: no effect Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32,36
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32,33	moderate
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32,33,37	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%; Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32,33,37
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=33 Page: 33.0	no
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=34 Page: 34.0	no
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=34 Page: 34.0	yes [IC50 0.79 uM]
UGT1A1 303	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=34 Page: 34,4	yes [IC50 1.2 uM]	yes (pharmacogenomic study) Comment: Certain UGT1A1 genotypes are associated with an increase in the risk of pazopanib induced hyperbilirubinemia. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=34 Page: 34,4

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32,35	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; Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32,35
CYP1A2 1197	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32.0	minor
CYP2C8 810	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=32 Page: 32.0	minor
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=34 Page: 34,35	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; Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_ClinPharmR.pdf#page=34 Page: 34,35

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022465s000_PharmR.pdf#PAGE=68 Page: 68.0

Sourcing

Vendor/Aggregator	ID	URL
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

Title	Date	PubMed
Analytical control of process impurities in Pazopanib hydrochloride by impurity fate mapping.	2010-08-01	20189340
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	20200024
Plethora of agents, plethora of targets, plethora of side effects in metastatic renal cell carcinoma.	2010-08	20163917
An exploratory study of sunitinib plus paclitaxel as first-line treatment for patients with advanced breast cancer.	2010-07	20032126
[Antiangionic drugs in soft tissue sarcoma].	2010-06	20483703
Pazopanib: an oral multitargeted tyrosine kinase inhibitor for use in renal cell carcinoma.	2010-06	20407031
Current status of vascular endothelial growth factor inhibition in age-related macular degeneration.	2010-06	20210371
Bevacizumab salvage therapy following progression in high-grade glioma patients treated with VEGF receptor tyrosine kinase inhibitors.	2010-06	20156808
Growth factors in multiple myeloma: a comprehensive analysis of their expression in tumor cells and bone marrow environment using Affymetrix microarrays.	2010-05-13	20465808
Antitumor and antiangiogenic effect of the dual EGFR and HER-2 tyrosine kinase inhibitor lapatinib in a lung cancer model.	2010-05-11	20459769
Initial assessment, surveillance, and management of blood pressure in patients receiving vascular endothelial growth factor signaling pathway inhibitors.	2010-05-05	20351338
Everolimus and pazopanib: two new drugs for renal cell cancer.	2010-05-03	20431519
Pazopanib: a multikinase inhibitor with activity in advanced renal cell carcinoma.	2010-05	20469994
Targeted therapy and hand-foot skin reaction in advanced renal cell carcinoma.	2010-05	20113155
The complexity of the complicity of mast cells in cancer.	2010-05	20026421
Pazopanib-induced hyperbilirubinemia is associated with Gilbert's syndrome UGT1A1 polymorphism.	2010-04-27	20389299
New therapeutic strategies for renal cell carcinoma.	2010-04-03	20359144
Potent preclinical impact of metronomic low-dose oral topotecan combined with the antiangiogenic drug pazopanib for the treatment of ovarian cancer.	2010-04	20371722
Bridging the gap between cytotoxic and biologic therapy with metronomic topotecan and pazopanib in ovarian cancer.	2010-04	20371710
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	20215520
Recent advances and future directions in the management of metastatic renal cell carcinoma.	2010-03	20184547
[Management of metastatic HER2-positive breast cancer: present and future].	2010-03	20176546
Anti-angiogenic tyrosine kinase inhibitors: what is their mechanism of action?	2010-03	20012482
StatBite: FDA oncology drug product approvals in 2009.	2010-02-24	20145211
Pazopanib in locally advanced or metastatic renal cell carcinoma: results of a randomized phase III trial.	2010-02-20	20100962
Prognostic stratification of patients with advanced renal cell carcinoma treated with sunitinib: comparison with the Memorial Sloan-Kettering prognostic factors model.	2010-02-18	20163744
Prognostic factors in patients treated with VEGF-targeted therapies.	2010-02	20386528
Noninvasive assessment of tumor VEGF receptors in response to treatment with pazopanib: a molecular imaging study.	2010-02	20165696
Angiogenesis inhibitors in the management of breast cancer.	2010-02	19952746
Anti-angiogenesis agents in metastatic or recurrent cervical cancer.	2010-02	19861227
Efficacy and safety of pazopanib in patients with metastatic renal cell carcinoma.	2010-01-20	20008644
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	20148481
Molecular basis for the treatment of renal cell carcinoma.	2010-01	20080466
Pazopanib.	2010-01	20043026
VEGF signalling inhibition-induced proteinuria: Mechanisms, significance and management.	2010-01	20006922
Targeting angiogenesis with multitargeted tyrosine kinase inhibitors in the treatment of non-small cell lung cancer.	2010	20427383
Antiangiogenic therapy and mechanisms of tumor resistance in malignant glioma.	2010	20414333
Everolimus (RAD001) in the treatment of advanced renal cell carcinoma: a review.	2010	20215359
Anticancer Role of PPARgamma Agonists in Hematological Malignancies Found in the Vasculature, Marrow, and Eyes.	2010	20204067
Targeting signal transduction pathways in metastatic breast cancer: a comprehensive review.	2010	20200040
Targeted therapies in epithelial ovarian cancer.	2010	20111741
A current review of targeted therapeutics for ovarian cancer.	2010	20069122
Major clinical research advances in gynecologic cancer 2009.	2009-12	20041096
Impact of anti-angiogenic treatments on metastatic renal cell carcinoma.	2009-12	19954291
Pazopanib: therapeutic developments.	2009-12	19954277
Tyrosine kinase inhibitors and the thyroid.	2009-12	19942148
Selective inhibition of retinal angiogenesis by targeting PI3 kinase.	2009-11-17	19924235
Pazopanib: an antiangiogenic drug in perspective.	2009-11	19903063
Pazopanib for the treatment of renal cell carcinoma and other malignancies.	2009-09	19956806
Targeted therapy in the treatment of metastatic renal cell cancer.	2009	20130440

Patents

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

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Name

Type

Language

GW786034

Preferred Name

English

PAZOPANIB

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