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

Details

Stereochemistry ACHIRAL
Molecular Formula C13H8N6
Molecular Weight 248.2433
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TOPIROXOSTAT

SMILES

c1cnccc1-c2nc(-c3ccnc(c3)C#N)[nH]n2

InChI

InChIKey=UBVZQGOVTLIHLH-UHFFFAOYSA-N
InChI=1S/C13H8N6/c14-8-11-7-10(3-6-16-11)13-17-12(18-19-13)9-1-4-15-5-2-9/h1-7H,(H,17,18,19)

HIDE SMILES / InChI

Description
Curator's Comment:: Description was created based on several sources, including http://www.pharmacodia.com/yaodu/html/v1/chemicals/ee14c41e92ec5c97b54cf9b74e25bd99.html

Topiroxostat was approved by Pharmaceuticals Medical Devices Agency of Japan (PMDA) on June 28, 2013. It was co-developed and marketed as Uriadec®/Topiloric® by Sanwa Kagaku Kenkyusho & Fuji Yakuhin. Topiroxostat is a xanthine oxidase inhibitor. Xanthine oxidase (XO) is a type of enzyme that generates reductive oxygen species, which catalyze the oxidation of hypoxanthine to xanthine and can further catalyze the oxidation of xanthine to uric acid. Topiroxostat could reduce the production of uric acid in the body through the inhibition of xanthine oxidase. It is usually used for the treatment of gout and hyperuricemia.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
5.3 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
URIADEC

Approved Use

Used for the treatment of gout and hyperuricemia

Launch Date

1.3722912E12
Primary
URIADEC

Approved Use

Used for the treatment of gout and hyperuricemia

Launch Date

1.3722912E12
PubMed

PubMed

TitleDatePubMed
Study on species differences in nephropathy induced by FYX-051, a xanthine oxidoreductase inhibitor.
2011 May
Patents

Patents

Sample Use Guides

In general, for adults, the initial dose is started with 20mg of the active ingredient at a time, twice a day, in the morning and in the evening, and the dosage may be gradually increased according to your blood uric acid levels. The maintenance dose is usually 1 tablet (60mg) at a time, twice a day. The dosage may be adjusted according to the disease, age or symptoms. The maximum dosage is 80mg at a time, twice a day. This preparation contains 60mg of the active ingredient in a tablet.
Route of Administration: Oral
IC50 values (50% inhibitory concentrations) of topiroxostat against plasma XOR activity were 5.84 nmol/l in mice.
Name Type Language
TOPIROXOSTAT
INN   WHO-DD  
INN  
Official Name English
TOPIROXOSTAT [WHO-DD]
Common Name English
FYX-051
Code English
TOPIROXOSTAT [MI]
Common Name English
TOPIROXOSTAT [INN]
Common Name English
4-(5-(PYRIDIN-4-YL)-1H-1,2,4-TRIAZOL-3-YL)PYRIDINE-2-CARBONITRILE
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C1637
Created by admin on Sat Jun 26 02:39:12 UTC 2021 , Edited by admin on Sat Jun 26 02:39:12 UTC 2021
Code System Code Type Description
EVMPD
SUB177917
Created by admin on Sat Jun 26 02:39:12 UTC 2021 , Edited by admin on Sat Jun 26 02:39:12 UTC 2021
PRIMARY
FDA UNII
0J877412JV
Created by admin on Sat Jun 26 02:39:12 UTC 2021 , Edited by admin on Sat Jun 26 02:39:12 UTC 2021
PRIMARY
DRUG BANK
DB01685
Created by admin on Sat Jun 26 02:39:12 UTC 2021 , Edited by admin on Sat Jun 26 02:39:12 UTC 2021
PRIMARY
MERCK INDEX
M11864
Created by admin on Sat Jun 26 02:39:12 UTC 2021 , Edited by admin on Sat Jun 26 02:39:12 UTC 2021
PRIMARY
INN
9220
Created by admin on Sat Jun 26 02:39:12 UTC 2021 , Edited by admin on Sat Jun 26 02:39:12 UTC 2021
PRIMARY
PUBCHEM
5288320
Created by admin on Sat Jun 26 02:39:12 UTC 2021 , Edited by admin on Sat Jun 26 02:39:12 UTC 2021
PRIMARY
EPA CompTox
577778-58-6
Created by admin on Sat Jun 26 02:39:12 UTC 2021 , Edited by admin on Sat Jun 26 02:39:12 UTC 2021
PRIMARY
NCI_THESAURUS
C96311
Created by admin on Sat Jun 26 02:39:12 UTC 2021 , Edited by admin on Sat Jun 26 02:39:12 UTC 2021
PRIMARY
DRUG CENTRAL
4888
Created by admin on Sat Jun 26 02:39:12 UTC 2021 , Edited by admin on Sat Jun 26 02:39:12 UTC 2021
PRIMARY
CAS
577778-58-6
Created by admin on Sat Jun 26 02:39:12 UTC 2021 , Edited by admin on Sat Jun 26 02:39:12 UTC 2021
PRIMARY