Pazopanib

Identification

Summary

Pazopanib is an antineoplastic agent used in the treatment of advanced renal cell cancer and advanced soft tissue sarcoma in patients with prior chemotherapy.

Brand Names

Votrient

Generic Name

Pazopanib

DrugBank Accession Number

DB06589

Background

Pazopanib is a small molecule inhibitor of multiple protein tyrosine kinases with potential antineoplastic activity. It is developed by GlaxoSmithKline and was FDA approved on October 19, 2009.

Type

Small Molecule

Groups

Approved

Structure

Similar Structures

Weight: Average: 437.518
Monoisotopic: 437.163393705
Chemical Formula: C₂₁H₂₃N₇O₂S

Synonyms

Pazopanib
Pazopanibum

External IDs

GW 78603
GW-786034
GW786034

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Pharmacology

Indication

Treatment of advanced renal cell cancer and advanced soft tissue sarcoma (in patients previously treated with chemotherapy)

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Associated Conditions

Indication Type	Indication	Approval Level
Treatment of	Advanced renal cell carcinoma	••••••••••••
Treatment of	Advanced soft tissue sarcoma	••••••••••••
Treatment of	Advanced thyroid cancer	••• •••••

Contraindications & Blackbox Warnings

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Pharmacodynamics

Pazopanib is a synthetic indazolylpyrimidine and reaches steady state concentrations of >15 μg/ml. This concentration is high enough to observe maximal inhibition of VEGFR2 phosphorylation and some anti-tumour activity (concentration required to inhibit receptors is 0.01 - 0.084 μmol/L). A reduction in tumour blood flow, increased tumour apoptosis, inhibition of tumour growth, reduction in tumour interstitial fluid pressure, and hypoxia in cancer cells can be observed in patients receiving treatment.

Mechanism of action

Pazopanib is a second-generation multitargeted tyrosine kinase inhibitor against vascular endothelial growth factor receptor-1, -2, and -3, platelet-derived growth factor receptor-alpha, platelet-derived growth factor receptor-beta, and c-kit. These receptor targets are part of the angiogenesis pathway that facilitates the formation of tumour blood vessel for tumour survival and growth.

Target	Actions	Organism
AVascular endothelial growth factor receptor 1	inhibitor	Humans
AVascular endothelial growth factor receptor 2	inhibitor	Humans
AVascular endothelial growth factor receptor 3	Not Available	Humans
APlatelet-derived growth factor receptor alpha	inhibitor	Humans
APlatelet-derived growth factor receptor beta	inhibitor	Humans
AMast/stem cell growth factor receptor Kit	inhibitor	Humans
UFibroblast growth factor receptor 3	inhibitor	Humans
UTyrosine-protein kinase ITK/TSK	inhibitor	Humans
UFibroblast growth factor 1	inhibitor	Humans
USH2B adapter protein 3	inhibitor	Humans

Absorption

Absorption of pazopanib in cancer patients is slow and incomplete. In patients with solid tumour, over a dose range of 50-2000 mg, absorption is nonlinear. Significant accumulation of pazopanib can also be observed in patients receiving 800 mg once daily for 22 days. Crushing tablets may increase exposure (increase in Cmax and AUC, while Tmax decreases by 2 hours). Bioavailability, oral tablet 800 mg, cancer patient = 21%; Bioavailability may be low due to incomplete absorption from the gastrointestinal tract. The major circulating component of the drug in the systemic is pazopanib, and not its metabolites. Mean maximum plasma concentration= 58.1 µg/mL; Mean AUC= 1037 µg · h/mL;

Volume of distribution

Vd steady state, IV administration 5 mg, cancer patient = 11.1 L (range of 9.15 - 13.4)

Protein binding

>99% protein bound, independent of concentrations over a range of 10-100 μg/mL.

Metabolism

Metabolized by CYP3A4 and to a lesser extent by CYP1A2 and CYP2C8. Metabolites are less active than pazopanib (10 to 20-fold less active). Three of its metabolites can be observed in the systemic and account for <10% of plasma radioactivity.

Route of elimination

Primarily excreted via feces (82.2%) and to a negligible extent via urine (<4%) in cancer patients. Most of the administered dose is excreted unchanged. Approximately 10% of dose are oxidative metabolites and are mostly eliminated via the feces.

Half-life

35 hours. Oral absorption is not the rate limiting step of elimination from the plasma.

Clearance

CL, cancer patient, IV administration 5 mg = 4mL/min Half of the absorbed dose is cleared via oxidative metabolism.

Adverse Effects

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Toxicity

Not Available

Pathways

Not Available

Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">

Interacting Gene/Enzyme	Allele name	Genotype(s)	Defining Change(s)	Type(s)	Description	Details
UDP-glucuronosyltransferase 1-1	UGT1A1*28	(TA;TA)	TA pair insertion	ADR Directly Studied	The presence of this polymorphism in UGT1A1 is associated with an increase in the incidence of hyperbilirubinemia when treated with pazopanib.	Details
HLA class I histocompatibility antigen protein P5	HLA-B*57:01	(G;G)	G allele	ADR Directly Studied	The presence of this polymorphism in HCP5 may indicate an increased risk of ALT elevation leading to drug-related hepatotoxicty from pazpanib therapy.	Details

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

Drug	Interaction
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Abacavir	The metabolism of Abacavir can be decreased when combined with Pazopanib.
Abametapir	The serum concentration of Pazopanib can be increased when it is combined with Abametapir.
Abatacept	The metabolism of Pazopanib can be increased when combined with Abatacept.
Abemaciclib	The metabolism of Abemaciclib can be decreased when combined with Pazopanib.
Abiraterone	The metabolism of Pazopanib can be decreased when combined with Abiraterone.

Food Interactions

Avoid grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of pazopanib.
Avoid St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce the serum concentration of pazopanib.
Take on an empty stomach. Separate pazopanib from meals by at least 1 hour before and 2 hours after eating as food increases pazopanib bioavailability.
Take separate from antacids. Separate the administration of pazopanib and antacids by several hours.

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Pazopanib hydrochloride	33Y9ANM545	635702-64-6	MQHIQUBXFFAOMK-UHFFFAOYSA-N

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Votrient	Tablet	200 mg	Oral	Novartis	2010-08-13	Not applicable
Votrient	Tablet, film coated	200 mg/1	Oral	Glaxosmithkline Inc	2009-10-19	2017-11-30
Votrient	Tablet, film coated	400 mg	Oral	Novartis Europharm Limited	2016-09-08	Not applicable
Votrient	Tablet, film coated	200 mg	Oral	Novartis Europharm Limited	2016-09-08	Not applicable
Votrient	Tablet	400 mg	Oral	Novartis	Not applicable	Not applicable

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Pazopanib	Tablet, film coated	200 mg/1	Oral	Teva Pharmaceuticals, Inc.	2023-10-20	Not applicable
Pazopanib	Tablet	200 mg/1	Oral	Golden State Medical Supply, Inc.	2023-10-19	Not applicable
Pazopanib	Tablet, film coated	200 mg/1	Oral	Sun Pharmaceutical Industries, Inc.	2023-10-20	Not applicable
Pazopanib	Tablet	200 mg/1	Oral	Apotex Corp.	2023-10-19	Not applicable
PMS-pazopanib	Tablet	200 mg	Oral	Pharmascience Inc	2022-08-31	Not applicable

Chemical Identifiers

UNII: 7RN5DR86CK
CAS number: 444731-52-6
InChI Key: CUIHSIWYWATEQL-UHFFFAOYSA-N
InChI: 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)
IUPAC Name: 5-({4-[(2,3-dimethyl-2H-indazol-6-yl)(methyl)amino]pyrimidin-2-yl}amino)-2-methylbenzene-1-sulfonamide
SMILES: CN(C1=CC2=NN(C)C(C)=C2C=C1)C1=CC=NC(NC2=CC=C(C)C(=C2)S(N)(=O)=O)=N1

References

General References

Sonpavde G, Hutson TE, Sternberg CN: Pazopanib, a potent orally administered small-molecule multitargeted tyrosine kinase inhibitor for renal cell carcinoma. Expert Opin Investig Drugs. 2008 Feb;17(2):253-61. doi: 10.1517/13543784.17.2.253. [Article]
Verweij J, Sleijfer S: Pazopanib, a new therapy for metastatic soft tissue sarcoma. Expert Opin Pharmacother. 2013 May;14(7):929-35. doi: 10.1517/14656566.2013.780030. Epub 2013 Mar 14. [Article]
Deng Y, Sychterz C, Suttle AB, Dar MM, Bershas D, Negash K, Qian Y, Chen EP, Gorycki PD, Ho MY: Bioavailability, metabolism and disposition of oral pazopanib in patients with advanced cancer. Xenobiotica. 2013 May;43(5):443-53. doi: 10.3109/00498254.2012.734642. Epub 2012 Nov 16. [Article]
Deeks ED: Pazopanib: in advanced soft tissue sarcoma. Drugs. 2012 Nov 12;72(16):2129-40. doi: 10.2165/11209950-000000000-00000. [Article]

External Links

KEGG Drug: D05380
PubChem Compound: 10113978
PubChem Substance: 175427074
ChemSpider: 8289501
BindingDB: 26474
RxNav: 714438
ChEBI: 71219
ChEMBL: CHEMBL477772
ZINC: ZINC000011617039
RxList: RxList Drug Page
Drugs.com: Drugs.com Drug Page
Wikipedia: Pazopanib

FDA label

Download (593 KB)

MSDS

Download (70.4 KB)

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Completed	Other	Metastatic Renal Cell Carcinoma ( mRCC)	1
4	Completed	Treatment	Cancer	1
4	Completed	Treatment	Locally Advanced and/or Metastatic Renal Cell Carcinoma / Metastatic Clear Cell Renal Cell Carcinoma (ccRCC) / Renal Cell Carcinoma (RCC)	1
4	Not Yet Recruiting	Treatment	Breast Carcinoma / Endometrium Carcinoma / Ovarian Carcinoma / Renal Cell Carcinoma (RCC) / Thyroid Carcinoma	1
4	Terminated	Basic Science	Metastatic Clear Cell Renal Cell Carcinoma (ccRCC)	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Tablet	Oral	200 mg/1
Tablet	Oral	200 mg
Tablet	Oral	400 mg
Tablet	Oral	433.400 mg
Tablet, film coated	Oral
Tablet, film coated	Oral	200 mg/1
Tablet, coated	Oral
Tablet, film coated	Oral	200 mg
Tablet, film coated	Oral	400 mg
Tablet, coated	Oral	200 mg
Tablet, coated	Oral	400 mg

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
US7262203	No	2007-08-28	2021-12-19
US8114885	No	2012-02-14	2021-12-19
US7105530	No	2006-09-12	2023-10-19

Properties

State

Solid

Experimental Properties

Not Available

Predicted Properties

Property	Value	Source
Water Solubility	0.0433 mg/mL	ALOGPS
logP	3.59	ALOGPS
logP	3.55	Chemaxon
logS	-4	ALOGPS
pKa (Strongest Acidic)	10.41	Chemaxon
pKa (Strongest Basic)	4.36	Chemaxon
Physiological Charge	0	Chemaxon
Hydrogen Acceptor Count	7	Chemaxon
Hydrogen Donor Count	2	Chemaxon
Polar Surface Area	119.03 Å²	Chemaxon
Rotatable Bond Count	5	Chemaxon
Refractivity	132.18 m³·mol^-1	Chemaxon
Polarizability	45.4 Å³	Chemaxon
Number of Rings	4	Chemaxon
Bioavailability	1	Chemaxon
Rule of Five	Yes	Chemaxon
Ghose Filter	No	Chemaxon
Veber's Rule	No	Chemaxon
MDDR-like Rule	No	Chemaxon

Predicted ADMET Features

Property	Value	Probability
Human Intestinal Absorption	+	1.0
Blood Brain Barrier	+	0.8788
Caco-2 permeable	+	0.5
P-glycoprotein substrate	Non-substrate	0.8307
P-glycoprotein inhibitor I	Non-inhibitor	0.8126
P-glycoprotein inhibitor II	Inhibitor	0.5
Renal organic cation transporter	Non-inhibitor	0.8152
CYP450 2C9 substrate	Non-substrate	0.7797
CYP450 2D6 substrate	Non-substrate	0.8008
CYP450 3A4 substrate	Non-substrate	0.6024
CYP450 1A2 substrate	Non-inhibitor	0.5
CYP450 2C9 inhibitor	Non-inhibitor	0.5065
CYP450 2D6 inhibitor	Non-inhibitor	0.7779
CYP450 2C19 inhibitor	Non-inhibitor	0.6811
CYP450 3A4 inhibitor	Non-inhibitor	0.5385
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.5668
Ames test	Non AMES toxic	0.6543
Carcinogenicity	Non-carcinogens	0.8567
Biodegradation	Not ready biodegradable	0.9935
Rat acute toxicity	2.3961 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.9219
hERG inhibition (predictor II)	Non-inhibitor	0.7129

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
MS/MS Spectrum - , positive	LC-MS/MS	splash10-052r-0118900000-097bcfa914e959e3d51a
MS/MS Spectrum - , positive	LC-MS/MS	splash10-004i-0910000000-fd84ad14c383d8fa623f
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	splash10-0079-0000900000-821fb55586b95dca3134
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-000i-0000900000-99bcc508f51f5cf42cb1
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-00dr-0003900000-23c10ffe64d67edddf3e
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-000i-1010900000-78e5124432c17683ced2
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-0037-0539100000-64eade2a9f32a41bb9ce
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-056r-5951000000-443138a7acf127c4c6be
Predicted 1H NMR Spectrum	1D NMR	Not Applicable
Predicted 13C NMR Spectrum	1D NMR	Not Applicable

Chromatographic Properties

Collision Cross Sections (CCS)

Adduct	CCS Value (Å²)	Source type	Source
[M-H]-	231.2643348	predicted	DarkChem Lite v0.1.0
[M-H]-	192.55301	predicted	DeepCCS 1.0 (2019)
[M+H]+	232.5783348	predicted	DarkChem Lite v0.1.0
[M+H]+	194.94856	predicted	DeepCCS 1.0 (2019)
[M+Na]+	200.8611	predicted	DeepCCS 1.0 (2019)

Targets

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insights and accelerate drug research.

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Property	Measurement	pH	Temperature (°C)	References
Kd (nM)	14	N/A	N/A	A28055 / A28058
Kd (nM)	14000	7.4	25	A18427

Details1. Vascular endothelial growth factor receptor 1

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor

General Function: Vegf-b-activated receptor activity
Specific Function: Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFB and PGF, and plays an essential role in the development of embryonic vasculature, the regulation of angiogenesis, cell ...
Gene Name: FLT1
Uniprot ID: P17948
Uniprot Name: Vascular endothelial growth factor receptor 1
Molecular Weight: 150767.185 Da

References

Sonpavde G, Hutson TE: Pazopanib: a novel multitargeted tyrosine kinase inhibitor. Curr Oncol Rep. 2007 Mar;9(2):115-9. [Article]

Property	Measurement	pH	Temperature (°C)	References
IC 50 (nM)	30	N/A	N/A	A28075
Kd (nM)	14	N/A	N/A	A28055 / A28058
Kd (nM)	14000	N/A	N/A	A18427

Details2. Vascular endothelial growth factor receptor 2

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor

General Function: Vascular endothelial growth factor-activated receptor activity
Specific Function: Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFC and VEGFD. Plays an essential role in the regulation of angiogenesis, vascular development, vascular permeability, and ...
Gene Name: KDR
Uniprot ID: P35968
Uniprot Name: Vascular endothelial growth factor receptor 2
Molecular Weight: 151525.555 Da

References

Sonpavde G, Hutson TE: Pazopanib: a novel multitargeted tyrosine kinase inhibitor. Curr Oncol Rep. 2007 Mar;9(2):115-9. [Article]

Property	Measurement	pH	Temperature (°C)	References
Kd (nM)	27	N/A	N/A	A28055 / A28058

Details3. Vascular endothelial growth factor receptor 3

Kind: Protein
Organism: Humans
Pharmacological action: Yes

General Function: Vascular endothelial growth factor-activated receptor activity
Specific Function: Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFC and VEGFD, and plays an essential role in adult lymphangiogenesis and in the development of the vascular network and the cardi...
Gene Name: FLT4
Uniprot ID: P35916
Uniprot Name: Vascular endothelial growth factor receptor 3
Molecular Weight: 152755.94 Da

References

Sonpavde G, Hutson TE: Pazopanib: a novel multitargeted tyrosine kinase inhibitor. Curr Oncol Rep. 2007 Mar;9(2):115-9. [Article]

Property	Measurement	pH	Temperature (°C)	References
Kd (nM)	4.9	N/A	N/A	A28055 / A28058
Kd (nM)	4900	N/A	N/A	A18427

Details4. Platelet-derived growth factor receptor alpha

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor

General Function: Vascular endothelial growth factor-activated receptor activity
Specific Function: Tyrosine-protein kinase that acts as a cell-surface receptor for PDGFA, PDGFB and PDGFC and plays an essential role in the regulation of embryonic development, cell proliferation, survival and chem...
Gene Name: PDGFRA
Uniprot ID: P16234
Uniprot Name: Platelet-derived growth factor receptor alpha
Molecular Weight: 122668.46 Da

References

Sonpavde G, Hutson TE: Pazopanib: a novel multitargeted tyrosine kinase inhibitor. Curr Oncol Rep. 2007 Mar;9(2):115-9. [Article]

Property	Measurement	pH	Temperature (°C)	References
Kd (nM)	2	N/A	N/A	A28055 / A28058
Kd (nM)	2000	N/A	N/A	A18427

Details5. Platelet-derived growth factor receptor beta

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor

General Function: Vascular endothelial growth factor binding
Specific Function: Tyrosine-protein kinase that acts as cell-surface receptor for homodimeric PDGFB and PDGFD and for heterodimers formed by PDGFA and PDGFB, and plays an essential role in the regulation of embryonic...
Gene Name: PDGFRB
Uniprot ID: P09619
Uniprot Name: Platelet-derived growth factor receptor beta
Molecular Weight: 123966.895 Da

References

Sonpavde G, Hutson TE: Pazopanib: a novel multitargeted tyrosine kinase inhibitor. Curr Oncol Rep. 2007 Mar;9(2):115-9. [Article]

Details6. Mast/stem cell growth factor receptor Kit

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor

General Function: Transmembrane receptor protein tyrosine kinase activity
Specific Function: Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine KITLG/SCF and plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell main...
Gene Name: KIT
Uniprot ID: P10721
Uniprot Name: Mast/stem cell growth factor receptor Kit
Molecular Weight: 109863.655 Da

References

Sonpavde G, Hutson TE: Pazopanib: a novel multitargeted tyrosine kinase inhibitor. Curr Oncol Rep. 2007 Mar;9(2):115-9. [Article]

Details7. Fibroblast growth factor receptor 3

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Protein tyrosine kinase activity
Specific Function: Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation and apoptosis. Plays an...
Gene Name: FGFR3
Uniprot ID: P22607
Uniprot Name: Fibroblast growth factor receptor 3
Molecular Weight: 87708.905 Da

References

Deeks ED: Pazopanib: in advanced soft tissue sarcoma. Drugs. 2012 Nov 12;72(16):2129-40. doi: 10.2165/11209950-000000000-00000. [Article]

Property	Measurement	pH	Temperature (°C)	References
Kd (nM)	>10000	N/A	N/A	A28055 / A28058

Details8. Tyrosine-protein kinase ITK/TSK

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Non-membrane spanning protein tyrosine kinase activity
Specific Function: Tyrosine kinase that plays an essential role in regulation of the adaptive immune response. Regulates the development, function and differentiation of conventional T-cells and nonconventional NKT-c...
Gene Name: ITK
Uniprot ID: Q08881
Uniprot Name: Tyrosine-protein kinase ITK/TSK
Molecular Weight: 71830.405 Da

References

Deeks ED: Pazopanib: in advanced soft tissue sarcoma. Drugs. 2012 Nov 12;72(16):2129-40. doi: 10.2165/11209950-000000000-00000. [Article]

Details9. Fibroblast growth factor 1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: S100 protein binding
Specific Function: Plays an important role in the regulation of cell survival, cell division, angiogenesis, cell differentiation and cell migration. Functions as potent mitogen in vitro.
Gene Name: FGF1
Uniprot ID: P05230
Uniprot Name: Fibroblast growth factor 1
Molecular Weight: 17459.58 Da

References

Deeks ED: Pazopanib: in advanced soft tissue sarcoma. Drugs. 2012 Nov 12;72(16):2129-40. doi: 10.2165/11209950-000000000-00000. [Article]

Details10. SH2B adapter protein 3

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Signaling adaptor activity
Specific Function: Links T-cell receptor activation signal to phospholipase C-gamma-1, GRB2 and phosphatidylinositol 3-kinase.
Gene Name: SH2B3
Uniprot ID: Q9UQQ2
Uniprot Name: SH2B adapter protein 3
Molecular Weight: 63224.45 Da

References

Deeks ED: Pazopanib: in advanced soft tissue sarcoma. Drugs. 2012 Nov 12;72(16):2129-40. doi: 10.2165/11209950-000000000-00000. [Article]

Enzymes

Details1. Cytochrome P450 2D6

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Steroid hydroxylase activity
Specific Function: Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name: CYP2D6
Uniprot ID: P10635
Uniprot Name: Cytochrome P450 2D6
Molecular Weight: 55768.94 Da

References

Keisner SV, Shah SR: Pazopanib: the newest tyrosine kinase inhibitor for the treatment of advanced or metastatic renal cell carcinoma. Drugs. 2011 Mar 5;71(4):443-54. doi: 10.2165/11588960-000000000-00000. [Article]
Goh BC, Reddy NJ, Dandamudi UB, Laubscher KH, Peckham T, Hodge JP, Suttle AB, Arumugham T, Xu Y, Xu CF, Lager J, Dar MM, Lewis LD: An evaluation of the drug interaction potential of pazopanib, an oral vascular endothelial growth factor receptor tyrosine kinase inhibitor, using a modified Cooperstown 5+1 cocktail in patients with advanced solid tumors. Clin Pharmacol Ther. 2010 Nov;88(5):652-9. doi: 10.1038/clpt.2010.158. Epub 2010 Sep 29. [Article]

Details2. Cytochrome P450 2C8

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate
Inhibitor

General Function: Steroid hydroxylase activity
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name: CYP2C8
Uniprot ID: P10632
Uniprot Name: Cytochrome P450 2C8
Molecular Weight: 55824.275 Da

References

Keisner SV, Shah SR: Pazopanib: the newest tyrosine kinase inhibitor for the treatment of advanced or metastatic renal cell carcinoma. Drugs. 2011 Mar 5;71(4):443-54. doi: 10.2165/11588960-000000000-00000. [Article]
Verweij J, Sleijfer S: Pazopanib, a new therapy for metastatic soft tissue sarcoma. Expert Opin Pharmacother. 2013 May;14(7):929-35. doi: 10.1517/14656566.2013.780030. Epub 2013 Mar 14. [Article]

Details3. Cytochrome P450 1A2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name: CYP1A2
Uniprot ID: P05177
Uniprot Name: Cytochrome P450 1A2
Molecular Weight: 58293.76 Da

References

Verweij J, Sleijfer S: Pazopanib, a new therapy for metastatic soft tissue sarcoma. Expert Opin Pharmacother. 2013 May;14(7):929-35. doi: 10.1517/14656566.2013.780030. Epub 2013 Mar 14. [Article]
FDA Label, Pazopanib [File]

Details4. Cytochrome P450 3A4

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate
Inhibitor

General Function: Vitamin d3 25-hydroxylase activity
Specific Function: Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name: CYP3A4
Uniprot ID: P08684
Uniprot Name: Cytochrome P450 3A4
Molecular Weight: 57342.67 Da

References

Keisner SV, Shah SR: Pazopanib: the newest tyrosine kinase inhibitor for the treatment of advanced or metastatic renal cell carcinoma. Drugs. 2011 Mar 5;71(4):443-54. doi: 10.2165/11588960-000000000-00000. [Article]
Goh BC, Reddy NJ, Dandamudi UB, Laubscher KH, Peckham T, Hodge JP, Suttle AB, Arumugham T, Xu Y, Xu CF, Lager J, Dar MM, Lewis LD: An evaluation of the drug interaction potential of pazopanib, an oral vascular endothelial growth factor receptor tyrosine kinase inhibitor, using a modified Cooperstown 5+1 cocktail in patients with advanced solid tumors. Clin Pharmacol Ther. 2010 Nov;88(5):652-9. doi: 10.1038/clpt.2010.158. Epub 2010 Sep 29. [Article]
Verweij J, Sleijfer S: Pazopanib, a new therapy for metastatic soft tissue sarcoma. Expert Opin Pharmacother. 2013 May;14(7):929-35. doi: 10.1517/14656566.2013.780030. Epub 2013 Mar 14. [Article]

Transporters

Details1. P-glycoprotein 1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Xenobiotic-transporting atpase activity
Specific Function: Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name: ABCB1
Uniprot ID: P08183
Uniprot Name: Multidrug resistance protein 1
Molecular Weight: 141477.255 Da

References

Deng Y, Sychterz C, Suttle AB, Dar MM, Bershas D, Negash K, Qian Y, Chen EP, Gorycki PD, Ho MY: Bioavailability, metabolism and disposition of oral pazopanib in patients with advanced cancer. Xenobiotica. 2013 May;43(5):443-53. doi: 10.3109/00498254.2012.734642. Epub 2012 Nov 16. [Article]

Details2. ATP-binding cassette sub-family G member 2

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Xenobiotic-transporting atpase activity
Specific Function: High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name: ABCG2
Uniprot ID: Q9UNQ0
Uniprot Name: ATP-binding cassette sub-family G member 2
Molecular Weight: 72313.47 Da

References

Deng Y, Sychterz C, Suttle AB, Dar MM, Bershas D, Negash K, Qian Y, Chen EP, Gorycki PD, Ho MY: Bioavailability, metabolism and disposition of oral pazopanib in patients with advanced cancer. Xenobiotica. 2013 May;43(5):443-53. doi: 10.3109/00498254.2012.734642. Epub 2012 Nov 16. [Article]

Details3. Solute carrier organic anion transporter family member 1B1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Sodium-independent organic anion transmembrane transporter activity
Specific Function: Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name: SLCO1B1
Uniprot ID: Q9Y6L6
Uniprot Name: Solute carrier organic anion transporter family member 1B1
Molecular Weight: 76447.99 Da

References

Deeks ED: Pazopanib: in advanced soft tissue sarcoma. Drugs. 2012 Nov 12;72(16):2129-40. doi: 10.2165/11209950-000000000-00000. [Article]
Hu S, Mathijssen RH, de Bruijn P, Baker SD, Sparreboom A: Inhibition of OATP1B1 by tyrosine kinase inhibitors: in vitro-in vivo correlations. Br J Cancer. 2014 Feb 18;110(4):894-8. doi: 10.1038/bjc.2013.811. Epub 2014 Jan 7. [Article]

Details4. UDP-glucuronosyltransferase 1-1

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Steroid binding
Specific Function: UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name: UGT1A1
Uniprot ID: P22309
Uniprot Name: UDP-glucuronosyltransferase 1-1
Molecular Weight: 59590.91 Da

References

Deeks ED: Pazopanib: in advanced soft tissue sarcoma. Drugs. 2012 Nov 12;72(16):2129-40. doi: 10.2165/11209950-000000000-00000. [Article]

Drug created at March 19, 2008 16:38 / Updated at February 20, 2024 23:54

Pazopanib

Identification

Structure for Pazopanib (DB06589)

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

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Clinical Trials

Pharmacoeconomics

Properties

Spectra

Collision Cross Sections (CCS)

Targets

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Enzymes

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Transporters

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