PAZOPANIB

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National Institutes of Health Divider Arrow

NCATS

Details

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

SHOW SMILES / InChI

Structure of PAZOPANIB

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

Approval Year

Substance Class	Chemical Created by `admin` on `Sat Dec 16 15:59:10 UTC 2023` Edited by `admin` on `Sat Dec 16 15:59:10 UTC 2023`
Record UNII	7RN5DR86CK
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

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

GW786034

Code

English

pazopanib [INN]

Common Name

English

PAZOPANIB [MI]

Common Name

English

BENZENESULFONAMIDE, 5-((4-((2,3-DIMETHYL-2H-INDAZOL-6-YL)METHYLAMINO)-2-PYRIMIDINYL)AMINO)-2-METHYL-

Systematic Name

English

Pazopanib [WHO-DD]

Common Name

English

NSC-752782

Code

English

Classification Tree Code System Code

FDA ORPHAN DRUG

705819

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

NCI_THESAURUS

C1967

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

EMA ASSESSMENT REPORTS

VOTRIENT (AUTHORIZED: CARCINOMA, RENAL CELL)

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

FDA ORPHAN DRUG

383912

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

WHO-ATC

L01XE11

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

WHO-VATC

QL01XE11

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

LIVERTOX

NBK548110

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

NCI_THESAURUS

C1742

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

NDF-RT

N0000175605

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

FDA ORPHAN DRUG

293809

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

Code System Code Type Description

EVMPD

SUB29175

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

ChEMBL

CHEMBL477772

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

PUBCHEM

10113978

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

NDF-RT

N0000182137

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

Cytochrome P450 2D6 Inhibitors [MoA]

HSDB

8210

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

WIKIPEDIA

PAZOPANIB

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

MESH

C516667

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

DRUG CENTRAL

4118

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

NDF-RT

N0000182141

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

Cytochrome P450 3A4 Inhibitors [MoA]

NDF-RT

N0000187062

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

Cytochrome P450 2C8 Inhibitors [MoA]

RXCUI

714438

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

RxNorm

NSC

752782

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

CAS

444731-52-6

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

EPA CompTox

DTXSID8048733

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

MERCK INDEX

m8430

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

Merck Index

CHEBI

71219

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

LACTMED

Pazopanib

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

FDA UNII

7RN5DR86CK

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

SMS_ID

100000090733

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

DAILYMED

7RN5DR86CK

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

DRUG BANK

DB06589

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

INN

8681

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

IUPHAR

5698

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

NCI_THESAURUS

C74547

Created by admin on Sat Dec 16 15:59:10 UTC 2023 , Edited by admin on Sat Dec 16 15:59:10 UTC 2023

PRIMARY

Related Record Type Details


					AIN96D6SGL

OATP1B1

TRANSPORTER -> SUBSTRATE


					HH55AX8FNP

PAZOPANIB HYDROCHLORIDE MONOHYDRATE

SALT/SOLVATE -> PARENT

Amount:


					798536Z7S0

VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2

TARGET -> INHIBITOR


					33Y9ANM545

PAZOPANIB HYDROCHLORIDE

SALT/SOLVATE -> PARENT

Amount:

Related Record Type Details


					SX3LHF7K66

METABOLITE INACTIVE -> PARENT

Comments:

LESS THAN 10%

Qualification:

PLASMA

Amount:


					Z51V93OIDV

METABOLITE INACTIVE -> PARENT

Comments:

In plasma and blood, individual circulating metabolites represented less than 10% total radioactivity

Qualification:

PLASMA

Amount:


					23M9H61WO8

METABOLITE ACTIVE -> PARENT

Comments:

Only one of these metabolites (GSK1268997) has been shown to inhibit the proliferation of VEGF-stimulated human umbilical vein endothelial cells with potency similar to pazopanib. The other metabolites show at least 10- to 20-fold less activity than the parent compound in the same cellular assay.


					SX3LHF7K66

METABOLITE INACTIVE -> PARENT

Qualification:

FECAL

Amount:


					23M9H61WO8

METABOLITE ACTIVE -> PARENT

Comments:

The majority of radiolabeled material recovered in feces constituted unchanged pazopanib, accounting for a mean of 67% of the administered radioactivity activity dose. Pazopanib metabolites GSK1268992 and GSK1268997 accounted for means of approximately 6% and 2% of the administered radioactivity dose, respectively.

Qualification:

FECAL

Amount:


					23M9H61WO8

METABOLITE ACTIVE -> PARENT

Comments:

Renal elimination of pazopanib is accounted for less than 4% of bodily excretion of the administered dose (Table 9). The majority of the radioactivity (82.2%) was recovered in feces by 120 hours (Table 9). Pazopanib undergoes moderate liver metabolism.

Qualification:

FECAL; PLASMA; URINE


					SX3LHF7K66

METABOLITE INACTIVE -> PARENT

Comments:

Four pazopanib metabolites (GSK1268992, GSK1268997, GSK1071306, and GW700201) have been identified. Only one of these metabolites (GSK1268997) has been shown to inhibit the proliferation of VEGF-stimulated human umbilical vein endothelial cells with potency similar to pazopanib. The other metabolites show at least 10- to 20-fold less activity than the parent compound in the same cellular assay.


					SX3LHF7K66

METABOLITE INACTIVE -> PARENT

Comments:

Renal elimination of pazopanib is accounted for less than 4% of bodily excretion of the administered dose (Table 9). The majority of the radioactivity (82.2%) was recovered in feces by 120 hours (Table 9). Pazopanib undergoes moderate liver metabolism. Pazopanib was the major drug-related component in human plasma representing 84% and 91% of the AUC(0-∞) in two of the three subjects that received 400 mg radiolabeled pazopanib.

Qualification:

FECAL; PLASMA; URINE


					Z51V93OIDV

METABOLITE INACTIVE -> PARENT

Comments:

Four pazopanib metabolites (GSK1268992, GSK1268997, GSK1071306, and GW700201) have been identified. Only one of these metabolites (GSK1268997) has been shown to inhibit the proliferation of VEGF-stimulated human umbilical vein endothelial cells with potency similar to pazopanib.

Related Record Type Details


					7RN5DR86CK

PAZOPANIB

ACTIVE MOIETY

Name	Property Type	Amount	Referenced Substance	Defining	Parameters	References
Biological Half-life	PHARMACOKINETIC		`7RN5DR86CK` PAZOPANIB		Elimination PHARMACOKINETIC