OZAGREL SODIUM

Possibly Marketed Outside US

Details

Stereochemistry	ACHIRAL
Molecular Formula	C13H11N2O2.Na
Molecular Weight	250.2284
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[Na+].[O-]C(=O)\C=C\C1=CC=C(CN2C=CN=C2)C=C1

InChI

InChIKey=NCNYJCOBUTXCBR-IPZCTEOASA-M

InChI=1S/C13H12N2O2.Na/c16-13(17)6-5-11-1-3-12(4-2-11)9-15-8-7-14-10-15;/h1-8,10H,9H2,(H,16,17);/q;+1/p-1/b6-5+;

HIDE SMILES / InChI

Description
Sources: http://www.pathophysiologyjournal.com/article/S0928-4680(97)00013-8/pdf | http://www.ncbi.nlm.nih.gov/pubmed/14720071 | http://www.ncbi.nlm.nih.gov/pubmed/7758058

Ozagrel is a thromboxane A2 synthesis inhibitor used for the treatment of cerebral vasospasm and asthma due to its antiplatelet and anti-inflammation properties.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Thromboxane-A synthase 21 Target ID: P24557\|\|\|Q8IUN1\|\|\|Q9HD82 Gene ID: 6916.0 Gene Symbol: TBXAS1 Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/14720071	Inhibitor 8504		11.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Bronchial asthma 50 Sources: http://onlinelibrary.wiley.com/doi/10.1111/j.1440-1843.2006.00920_6.x/pdf	Palliative		Approved 8583	DOMENAN Approved Use Unknown
Cerebral vasospasm 9 Sources: http://apps.who.int/medicinedocs/index/assoc/h5778e/h5778e.pdf	Primary		Approved 8583	XANBON Approved Use Cerebral vasospasm and ischaemia following surgical management of subarachnoid haemorrhage.

C_max

Value	Dose	Analyte	Population
97 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_3999411H2038_1_005_1F.pdf#page=25	1 μg/kg/min single, intravenous dose: 1 μg/kg/min route of administration: Intravenous experiment type: SINGLE co-administered:	OZAGREL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1657.3 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_3999411H2038_1_005_1F.pdf#page=25	15 μg/kg/min single, intravenous dose: 15 μg/kg/min route of administration: Intravenous experiment type: SINGLE co-administered:	OZAGREL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
576.5 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_3999411H2038_1_005_1F.pdf#page=26	5 mg single, intravenous dose: 5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OZAGREL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1928.8 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	OZAGREL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2020 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OZAGREL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1940 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OZAGREL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
281 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_3999411H2038_1_005_1F.pdf#page=25	1 μg/kg/min single, intravenous dose: 1 μg/kg/min route of administration: Intravenous experiment type: SINGLE co-administered:	OZAGREL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4659.2 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_3999411H2038_1_005_1F.pdf#page=25	15 μg/kg/min single, intravenous dose: 15 μg/kg/min route of administration: Intravenous experiment type: SINGLE co-administered:	OZAGREL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
197.4 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_3999411H2038_1_005_1F.pdf#page=26	5 mg single, intravenous dose: 5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OZAGREL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3913.2 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	OZAGREL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3360 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OZAGREL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3500 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OZAGREL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
0.79 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_3999411H2038_1_005_1F.pdf#page=25	1 μg/kg/min single, intravenous dose: 1 μg/kg/min route of administration: Intravenous experiment type: SINGLE co-administered:	OZAGREL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.66 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_3999411H2038_1_005_1F.pdf#page=25	15 μg/kg/min single, intravenous dose: 15 μg/kg/min route of administration: Intravenous experiment type: SINGLE co-administered:	OZAGREL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.09 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_3999411H2038_1_005_1F.pdf#page=26	5 mg single, intravenous dose: 5 mg route of administration: Intravenous experiment type: SINGLE co-administered:	OZAGREL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.45 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	OZAGREL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.74 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OZAGREL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.76 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	OZAGREL plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
46% OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/230034_4490012F1026_1_003_1F.pdf#page=19			OZAGREL serum	Homo sapiens

Doses

Dose	Population	Adverse events
800 mg 1 times / day multiple, oral Highest studied dose Dose: 800 mg, 1 times / day Route: oral Route: multiple Dose: 800 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/9792572/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/9792572/	Sources: https://pubmed.ncbi.nlm.nih.gov/9792572/

PubMed

Title	Date	PubMed
Thromboxane synthase mutations in an increased bone density disorder (Ghosal syndrome).	2008-03	18264100
Effect of sodium ozagrel on the activity of rat CYP2D6.	2007-11-14	17651725
Heparin-protamine complexes cause pulmonary hypertension in goats.	1995-10	7574058
Thromboxane A2 and development of genetic hypertension in the Lyon rat strain.	1990-12	2147173

Patents

Sample Use Guides

In Vivo Use Guide

1 tablet (200 mg of the active ingredient) at a time, twice a day after breakfast and before bedtime (for asthma). Intravenous infusion of 80mg, twice a day, solute in 500ml normal saline or 5% glucose solution (cerebral vasospasm).

Route of Administration: Other

In Vitro Use Guide

The inﬂuence of ozagrel on platelets aggregation was investigated. Platelet aggregation which was induced by ADP (5 uM) was inhibited by ozagrel. This inhibition was dependent on the concentration of the drug and was significant at 10(−6)–10(−3) M.

Name

Type

Language

CATACLOT

Preferred Name

English

OZAGREL SODIUM

Common Name

English

2-PROPENOIC ACID, 3-(4-(1H-IMIDAZOL-1-YLMETHYL)PHENYL)-, SODIUM SALT, (2E)-

Common Name

English

KW-01

Code

English

OZAGREL SODIUM SALT [MI]

Common Name

English

2-PROPENOIC ACID, 3-(4-(1H-IMIDAZOL-1-YLMETHYL)PHENYL)-, SODIUM SALT, (E)-

Common Name

English

SODIUM OZAGREL

Common Name

English

Ozagrel sodium [WHO-DD]

Common Name

English

ATHROMBONE

Common Name

English

2-PROPENOIC ACID, 3-(4-(1H-IMIDAZOL-1-YLMETHYL)PHENYL)-, SODIUM SALT (1:1), (2E)-

Common Name

English

XANBON

Brand Name

English

OZAGREL SODIUM [JAN]

Common Name

English

KADENIN

Common Name

English

Code System Code Type Description

MESH

C034364