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Details

Stereochemistry ACHIRAL
Molecular Formula C13H8N6.C7H8O3S
Molecular Weight 420.444
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TOPIROXOSTAT TOSYLATE

SMILES

CC1=CC=C(C=C1)S(O)(=O)=O.N#CC2=NC=CC(=C2)C3=NNC(=N3)C4=CC=NC=C4

InChI

InChIKey=HCEPIFBYVFRGOI-UHFFFAOYSA-N
InChI=1S/C13H8N6.C7H8O3S/c14-8-11-7-10(3-6-16-11)13-17-12(18-19-13)9-1-4-15-5-2-9;1-6-2-4-7(5-3-6)11(8,9)10/h1-7H,(H,17,18,19);2-5H,1H3,(H,8,9,10)

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

2013
Primary
URIADEC

Approved Use

Used for the treatment of gout and hyperuricemia

Launch Date

2013
PubMed

PubMed

TitleDatePubMed
FYX-051, a xanthine oxidoreductase inhibitor, induces nephropathy in rats, but not in monkeys.
2009 Jun
Discovery of 3-(2-cyano-4-pyridyl)-5-(4-pyridyl)-1,2,4-triazole, FYX-051 - a xanthine oxidoreductase inhibitor for the treatment of hyperuricemia [corrected].
2009 Nov 1
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 TOSYLATE
Common Name English
2-PYRIDINECARBONITRILE, 4-(3-(4-PYRIDINYL)-1H-1,2,4-TRIAZOL-5-YL)-, 4-METHYLBENZENESULFONATE (1:1)
Systematic Name English
2-PYRIDINECARBONITRILE, 4-(5-(4-PYRIDINYL)-1H-1,2,4-TRIAZOL-3-YL)-, MONO(4-METHYLBENZENESULFONATE)
Systematic Name English
TOPIROXOSTAT TOSYLATE [MI]
Common Name English
Code System Code Type Description
MERCK INDEX
m11864
Created by admin on Sat Dec 16 15:20:25 GMT 2023 , Edited by admin on Sat Dec 16 15:20:25 GMT 2023
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CAS
577778-88-2
Created by admin on Sat Dec 16 15:20:25 GMT 2023 , Edited by admin on Sat Dec 16 15:20:25 GMT 2023
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PUBCHEM
11327608
Created by admin on Sat Dec 16 15:20:25 GMT 2023 , Edited by admin on Sat Dec 16 15:20:25 GMT 2023
PRIMARY
FDA UNII
BT21GN8CE8
Created by admin on Sat Dec 16 15:20:25 GMT 2023 , Edited by admin on Sat Dec 16 15:20:25 GMT 2023
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