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Details

Stereochemistry ACHIRAL
Molecular Formula C13H8N6
Molecular Weight 248.2428
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TOPIROXOSTAT

SMILES

N#CC1=NC=CC(=C1)C2=NNC(=N2)C3=CC=NC=C3

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

Molecular Formula C13H8N6
Molecular Weight 248.2428
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

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.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
5.3 nM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
URIADEC
Primary
URIADEC

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
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
In Vitro Use Guide
IC50 values (50% inhibitory concentrations) of topiroxostat against plasma XOR activity were 5.84 nmol/l in mice.
Substance Class Chemical
Record UNII
0J877412JV
Record Status Validated (UNII)
Record Version