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
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)
DescriptionCurator's Comment: Description was created based on several sources, including
http://www.pharmacodia.com/yaodu/html/v1/chemicals/ee14c41e92ec5c97b54cf9b74e25bd99.html
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.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL1929 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27038523 |
5.3 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | URIADEC Approved UseUsed for the treatment of gout and hyperuricemia Launch Date2013 |
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Primary | URIADEC Approved UseUsed for the treatment of gout and hyperuricemia Launch Date2013 |
PubMed
Title | Date | PubMed |
---|---|---|
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
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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27038523
IC50 values (50% inhibitory concentrations) of topiroxostat against plasma XOR activity were 5.84 nmol/l in mice.
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ACTIVE MOIETY
SUBSTANCE RECORD