SERATRODAST

Possibly Marketed Outside US

Details

Stereochemistry	RACEMIC
Molecular Formula	C22H26O4
Molecular Weight	354.4394
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CC1=C(C)C(=O)C(C(CCCCCC(O)=O)C2=CC=CC=C2)=C(C)C1=O

InChI

InChIKey=ZBVKEHDGYSLCCC-UHFFFAOYSA-N

InChI=1S/C22H26O4/c1-14-15(2)22(26)20(16(3)21(14)25)18(17-10-6-4-7-11-17)12-8-5-9-13-19(23)24/h4,6-7,10-11,18H,5,8-9,12-13H2,1-3H3,(H,23,24)

HIDE SMILES / InChI

Molecular Formula	C22H26O4
Molecular Weight	354.4394
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description

Seratrodast belongs to a class of medication called thromboxane A2/prostaglandin endoperoxide receptor antagonist. Seratrodast blocks the broncho-constrictor effects of certain chemicals (prostaglandins) in the body. Seratrodast also decreases the inflammation by antagonising the thromboxane A2 receptor. Adverse effects include gastrointestinal disturbances, drowsiness, headache, palpitations, and hepatitis. Seradair may interact with Ozagrel.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Thromboxane A2 receptor 20	Antagonist 2,849		60.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Asthma 244	Primary		Approved 8,583	Bronica

C_max

Value	Dose	Analyte	Population
8.8 μg/mL	80 mg 1 times / day multiple, oral	SERATRODAST plasma	Homo sapiens
13.88 μg/mL	120 mg 1 times / day multiple, oral	SERATRODAST plasma	Homo sapiens
11.4 μg/mL	160 mg single, oral	SERATRODAST plasma	Homo sapiens
10.4 μg/mL	160 mg single, oral	SERATRODAST plasma	Homo sapiens
13.8 μg/mL	240 mg single, oral	SERATRODAST plasma	Homo sapiens
11.6 μg/mL	320 mg single, oral	SERATRODAST plasma	Homo sapiens
14.7 μg/mL	320 mg single, oral	SERATRODAST plasma	Homo sapiens
15.7 μg/mL	160 mg 1 times / day steady-state, oral	SERATRODAST plasma	Homo sapiens
25.3 μg/mL	160 mg 1 times / day steady-state, oral	SERATRODAST plasma	Homo sapiens
23.2 μg/mL	240 mg 1 times / day steady-state, oral	SERATRODAST plasma	Homo sapiens
39.9 μg/mL	240 mg 1 times / day steady-state, oral	SERATRODAST plasma	Homo sapiens
22.9 μg/mL	320 mg 1 times / day steady-state, oral	SERATRODAST plasma	Homo sapiens
37.4 μg/mL	320 mg 1 times / day steady-state, oral	SERATRODAST plasma	Homo sapiens

AUC

Value	Dose	Analyte	Population
22.96 μg × h/mL	80 mg 1 times / day multiple, oral	SERATRODAST plasma	Homo sapiens
36.52 μg × h/mL	120 mg 1 times / day multiple, oral	SERATRODAST plasma	Homo sapiens
192 μg × h/mL	160 mg single, oral	SERATRODAST plasma	Homo sapiens
197 μg × h/mL	160 mg single, oral	SERATRODAST plasma	Homo sapiens
302 μg × h/mL	240 mg single, oral	SERATRODAST plasma	Homo sapiens
271 μg × h/mL	320 mg single, oral	SERATRODAST plasma	Homo sapiens
350 μg × h/mL	320 mg single, oral	SERATRODAST plasma	Homo sapiens
166 μg × h/mL	160 mg 1 times / day steady-state, oral	SERATRODAST plasma	Homo sapiens
231 μg × h/mL	160 mg 1 times / day steady-state, oral	SERATRODAST plasma	Homo sapiens
334 μg × h/mL	240 mg 1 times / day steady-state, oral	SERATRODAST plasma	Homo sapiens
435 μg × h/mL	240 mg 1 times / day steady-state, oral	SERATRODAST plasma	Homo sapiens
351 μg × h/mL	320 mg 1 times / day steady-state, oral	SERATRODAST plasma	Homo sapiens
582 μg × h/mL	320 mg 1 times / day steady-state, oral	SERATRODAST plasma	Homo sapiens

T_1/2

Value	Dose	Analyte	Population
18.5 h	160 mg single, oral	SERATRODAST plasma	Homo sapiens
19.7 h	160 mg single, oral	SERATRODAST plasma	Homo sapiens
26.2 h	240 mg single, oral	SERATRODAST plasma	Homo sapiens
16.5 h	320 mg single, oral	SERATRODAST plasma	Homo sapiens
18 h	320 mg single, oral	SERATRODAST plasma	Homo sapiens
34.3 h	160 mg 1 times / day steady-state, oral	SERATRODAST plasma	Homo sapiens
40.6 h	160 mg 1 times / day steady-state, oral	SERATRODAST plasma	Homo sapiens
34.1 h	240 mg 1 times / day steady-state, oral	SERATRODAST plasma	Homo sapiens
40.3 h	240 mg 1 times / day steady-state, oral	SERATRODAST plasma	Homo sapiens
42 h	320 mg 1 times / day steady-state, oral	SERATRODAST plasma	Homo sapiens
27.9 h	320 mg 1 times / day steady-state, oral	SERATRODAST plasma	Homo sapiens

Doses

Doses

Show entries

Dose	Population	Adverse events
120 mg 1 times / day multiple, oral Highest studied dose	unhealthy, ADULT
120 mg single, oral Highest studied dose	healthy, ADULT

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Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1,946	inhibitor 2,438	substrate 1,388 inhibitor 2,507	inhibitor 2,217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP19A1 429 CYP2E1 1,060 CYP3A 227 CYP2A6 879 CYP1A2 2,153 BSEP 550 CYP2C19 2,057	CYP2B6 776 CYP2C8 810 CYP2C9/10 4 CYP2C19 1,119 CYP1A2 1,197 CYP2E1 729 CYP2A6 626

Drug as perpetrator

Show entries

Target	Modality	Activity
CYP2E1 1,146	inhibitor 4,027	no [IC50 >200 uM]
CYP19A1 430	inhibitor 4,027	no
CYP3A 317	inhibitor 4,027	no
CYP1A2 2,333	inhibitor 4,027	weak [IC50 180 uM]
CYP2D6 2,546	inhibitor 4,027	weak [IC50 200 uM]

Showing 1 to 5 of 9 entries

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Drug as victim

Show entries

Target	Modality	Activity
CYP2C9/10 4	substrate 4,014	major
CYP3A4 1,946	substrate 4,014	major
CYP2C19 1,119	substrate 4,014	minor
CYP2C8 810	substrate 4,014	minor
CYP1A2 1,197	substrate 4,014	no

Showing 1 to 5 of 9 entries

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Tox targets

Show entries

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2,263	inhibitor 2,237

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PubMed

Title	Date	PubMed
No data available in table

Patents

Sample Use Guides

In Vivo Use Guide

It is given in single doses of 80 mg in the evening after food.

Route of Administration: Oral

In Vitro Use Guide

Seratrodast competitively inhibited the contractile response to U-46619, PGD2, 9-alpha, 11beta-PGF2, or PGF2-alpha with pA2 values of 7.69, 7.20, 7.79, and 5.71, respectively.