TOPIROXOSTAT

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 Search

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

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: http://www.rad-ar.or.jp/siori/english/kekka.cgi?n=33460
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
Xanthine dehydrogenase 33 Target ID: CHEMBL1929 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27038523	Inhibitor 8504		5.3 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hyperuricemia 8 Sources: http://www.rad-ar.or.jp/siori/english/kekka.cgi?n=33460	Primary		Approved 8583	URIADEC Approved Use Used for the treatment of gout and hyperuricemia Launch Date 2013
Gout 28 Sources: http://www.rad-ar.or.jp/siori/english/kekka.cgi?n=33460	Primary		Approved 8583	URIADEC Approved Use Used for the treatment of gout and hyperuricemia Launch Date 2013

C_max

Value	Dose	Analyte	Population
579.3 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=29	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
375.8 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=29	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
229.9 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
469.4 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
288.7 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
822.3 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
755.2 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
1318.4 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1773.5 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	180 mg single, oral dose: 180 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
466.8 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=34	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
501.9 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=34	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
208.7 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=34	80 mg 2 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
172.9 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=34	80 mg 2 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
552.8 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=34	160 mg 2 times / day multiple, oral dose: 160 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
608.5 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=34	160 mg 2 times / day multiple, oral dose: 160 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
740.3 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=36	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
806.7 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=36	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
713.2 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=36	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
969.1 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=37	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
741.1 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=37	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
719 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=38	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED

AUC

Value	Dose	Analyte	Population
793.5 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=29	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
838.8 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=29	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
225.4 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
580.2 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
499.1 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
1206.6 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1278.6 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
2366.7 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2838.2 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	180 mg single, oral dose: 180 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
944.3 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=34	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
964.3 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=34	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
419.8 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=34	80 mg 2 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
443.9 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=34	80 mg 2 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
1044.4 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=34	160 mg 2 times / day multiple, oral dose: 160 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
1137.1 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=34	160 mg 2 times / day multiple, oral dose: 160 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
1161.5 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=36	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1372.7 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=36	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
1426.6 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=36	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
1264 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=37	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1213.8 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=37	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1523.5 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=38	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
10.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=29	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6.7 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=29	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
5 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
7.5 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
5.2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.1 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
4.6 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	120 mg single, oral dose: 120 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
7.1 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=32	180 mg single, oral dose: 180 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=34	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
6.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=34	80 mg 1 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
4.3 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=34	80 mg 2 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
6.2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=34	80 mg 2 times / day multiple, oral dose: 80 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
5.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=34	160 mg 2 times / day multiple, oral dose: 160 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=34	160 mg 2 times / day multiple, oral dose: 160 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
8.4 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=36	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6.7 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=36	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
7.2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=36	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: FASTED
7.3 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=37	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=37	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
8.2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=38	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	TOPIROXOSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
1.2% OTHER GOV'T https://www.pmda.go.jp/drugs/2013/P201300069/670242000_22500AMX00987000_A100_2.pdf#page=31			TOPIROXOSTAT plasma	Homo sapiens

Doses

Dose	Population	Adverse events
180 mg single, oral Highest studied dose Dose: 180 mg Route: oral Route: single Dose: 180 mg Sources: https://pubmed.ncbi.nlm.nih.gov/24214189/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/24214189/	Sources: https://pubmed.ncbi.nlm.nih.gov/24214189/
240 mg 2 times / day multiple, oral Highest studied dose Dose: 240 mg, 2 times / day Route: oral Route: multiple Dose: 240 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/30219951/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/30219951/	Other AEs: Gouty arthritis, Beta 2 microglobuli... Other AEs: Gouty arthritis (7.7%) Beta 2 microglobuli (7.7%) Beta 2 microglobulin uri (30.8%) Beta-N-acetyl-D-glucosaminidase increased (7.7%) Blood triglycerides increased (15.4%) Alpha 1 microglobuli (15.4%) Sources: https://pubmed.ncbi.nlm.nih.gov/30219951/

AEs

AE	Significance	Dose	Population
Alpha 1 microglobuli	15.4%	240 mg 2 times / day multiple, oral Highest studied dose Dose: 240 mg, 2 times / day Route: oral Route: multiple Dose: 240 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/30219951/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/30219951/
Blood triglycerides increased	15.4%	240 mg 2 times / day multiple, oral Highest studied dose Dose: 240 mg, 2 times / day Route: oral Route: multiple Dose: 240 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/30219951/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/30219951/
Beta 2 microglobulin uri	30.8%	240 mg 2 times / day multiple, oral Highest studied dose Dose: 240 mg, 2 times / day Route: oral Route: multiple Dose: 240 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/30219951/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/30219951/
Beta 2 microglobuli	7.7%	240 mg 2 times / day multiple, oral Highest studied dose Dose: 240 mg, 2 times / day Route: oral Route: multiple Dose: 240 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/30219951/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/30219951/
Beta-N-acetyl-D-glucosaminidase increased	7.7%	240 mg 2 times / day multiple, oral Highest studied dose Dose: 240 mg, 2 times / day Route: oral Route: multiple Dose: 240 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/30219951/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/30219951/
Gouty arthritis	7.7%	240 mg 2 times / day multiple, oral Highest studied dose Dose: 240 mg, 2 times / day Route: oral Route: multiple Dose: 240 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/30219951/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/30219951/

PubMed

Title	Date	PubMed
Study on species differences in nephropathy induced by FYX-051, a xanthine oxidoreductase inhibitor.	2011-05	20936465
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].	2009-11-01	19783139
FYX-051, a xanthine oxidoreductase inhibitor, induces nephropathy in rats, but not in monkeys.	2009-06	19336671
Characterization of N-glucuronidation of 4-(5-pyridin-4-yl-1H-[1,2,4]triazol-3-yl) pyridine-2-carbonitrile (FYX-051): a new xanthine oxidoreductase inhibitor.	2007-12	17761779
Metabolic profile of FYX-051 (4-(5-pyridin-4-yl-1h-[1,2,4]triazol-3-yl)pyridine-2-carbonitrile) in the rat, dog, monkey, and human: identification of N-glucuronides and N-glucosides.	2006-11	16914512

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 Created by `admin` on `Mon Mar 31 18:35:00 GMT 2025` Edited by `admin` on `Mon Mar 31 18:35:00 GMT 2025`
Record UNII	0J877412JV
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

FYX-051

Preferred Name

English

TOPIROXOSTAT

Official Name

English

TOPIROXOSTAT [MI]

Common Name

English

Topiroxostat [WHO-DD]

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

TOPIROXOSTAT [JAN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1637