General
Preferred name
PAZOPANIB
Synonyms
GW786034 ()
GW786034, Votrient, Pazopanib HCl, GW786034B ()
Votrient ()
Votrient HCl ()
Pazopanib HCl ()
GW786034 HCl ()
Pazopanib HCl (GW786034) ()
Pazopanib(GW-786034) ()
PAZOPANIB HYDROCHLORIDE ()
pazopanib hydrochloride (ophthalmic) ()
Pazopanib (Hydrochloride) ()
GW786034 (Hydrochloride) ()
Pazopanib HCl (GW786034 HCl) ()
GW786034B ()
NSC-752782 ()
GW-786034 ()
Pazopanib (as hydrochloride) ()
Pazopanib monohydrochloride ()
GW-786034B ()
Pazopanib-d6 ()
P&D ID
PD003339
CAS
444731-52-6
635702-64-6
790713-33-6
1219592-01-4
Tags
available
drug
Approved by
FDA
EMA
First approval
2009
Drug indication
Renal cell carcinoma
Sarcoma
Neoplasm
Drug Status
approved
Max Phase
4.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
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;
DESCRIPTION
Pazopanib is a Type-1 kinase inhibitor. Its discovery is reported in . It targets multiple receptor tyrosine kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRβ, FGFR1, Kit and CSF1R).
(GtoPdb)
DESCRIPTION
Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR¦Â, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
PRICE
35
DESCRIPTION
Pazopanib (GW786034) is an inhibitor of protein tyrosine kinases that inhibits VEGFR1, VEGFR2, VEGFR3, PDGFR??, c-Kit, FGFR1, and c-Fms (IC50=10/30/47/84/74/140/146 nM). Pazopanib has antitumor activity.
DESCRIPTION
Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR¦Â, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
PRICE
40
DESCRIPTION
inhibitor of VEGFRs, c-KIT, and PDGFRB
(Informer Set)
DESCRIPTION
Treatment of advanced renal cell cancer and advanced soft tissue sarcoma (in patients previously treated with chemotherapy)
(PKIDB)
DESCRIPTION
Pazopanib is an antineoplastic agent used in the treatment of advanced renal cell cancer and advanced soft tissue sarcoma in patients with prior chemotherapy.
(Enamine Bioactive Compounds)
DESCRIPTION
Pazopanib (GW786034) is an inhibitor of protein tyrosine kinases that inhibits VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms (IC50=10/30/47/84/74/140/146 nM). Pazopanib has antitumor activity.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Pazopanib Hydrochloride (Votrient HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
344
Organisms
0
Compound Sets
38
Axon Medchem Screening Library
CeMM library of unique drugs (CLOUD)
ChEMBL Approved Drugs
ChEMBL Drugs
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
Enamine Bioactive Compounds
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
Informer Set
JUMP-Target 1 Compound Set
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
NCATS Inxight Approved Drugs
NIH Approved Oncology Drugs
NPC Screening Collection
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
Welcome Trust Cancer Drugs
ZINC Tool Compounds
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
65
Molecular Weight
437.16
Hydrogen Bond Acceptors
8
Hydrogen Bond Donors
2
Rotatable Bonds
5
Ring Count
4
Aromatic Ring Count
4
cLogP
3.14
TPSA
119.03
Fraction CSP3
0.19
Chiral centers
0.0
Largest ring
6.0
QED
0.49
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
FLT1
FLT3
KDR
KIT
PDGFRB
Vascular endothelial growth factor receptor
Autophagy
c-Fms
c-Kit
FGFR
PDGFR
VEGFR
VEGFR, PDGFRA, PDGFRB, KIT
Tyrosine-protein kinase ITK/TSK
Fibroblast growth factor receptor 3
Platelet-derived growth factor receptor
Fibroblast growth factor receptor 1
Stem cell growth factor receptor
Macrophage colony stimulating factor receptor
Tyrosine-protein kinase LCK
CSF1R, FGF1, FGFR1, FGFR3, FLT1, FLT4, ITK, KDR, KIT, PDGFRA, PDGFRB, SH2B3
Multiple TKI
FGF1
Autophagy,c-Kit,CSF-1R,FGFR,PDGFR,VEGFR
Autophagy,Cathepsin B,c-Kit,CSF-1R,Cysteine Protease,FGFR,PDGFR,VEGFR
FLT4
PDGFRA
FGFR3
ITK
FGFR1
VEGFR1
VEGFR2
VEGFR3
Compound status
FDA
Pathway
RTK signaling
Angiogenesis
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
MOA
receptor protein-tyrosine kinase inhibitor
KIT inhibitor, PDGFR tyrosine kinase receptor inhibitor, VEGFR inhibitor
Targets
FLT1,KDR,FLT4
Indication
renal cell carcinoma (RCC), soft tissue sarcoma (STS)
Source data

