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Details

Stereochemistry ACHIRAL
Molecular Formula C10H11NO3
Molecular Weight 193.1992
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ACTARIT

SMILES

CC(=O)NC1=CC=C(CC(O)=O)C=C1

InChI

InChIKey=MROJXXOCABQVEF-UHFFFAOYSA-N
InChI=1S/C10H11NO3/c1-7(12)11-9-4-2-8(3-5-9)6-10(13)14/h2-5H,6H2,1H3,(H,11,12)(H,13,14)

HIDE SMILES / InChI

Molecular Formula C10H11NO3
Molecular Weight 193.1992
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: description was created based on several sources, including http://www.clinexprheumatol.org/article.asp?a=1640

Actarit (MS-932) is an anti-inflammatory drug developed in Japan for use in rheumatoid arthritis (RA). Actarit suppresses adjuvant arthritis through modulation of the immune system. Actarit acts on RA synovial cells to reduce cell-cell interactions with autologous synovium infiltrating lymphocytes and to inhibit proinflammatory cytokine and MMP production, leading to amelioration of symptoms of RA.

Approval Year

Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Secondary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
2.24 μg/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ACTARIT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
3.87 μg/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ACTARIT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
7.91 μg/mL
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ACTARIT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
14.1 μg/mL
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ACTARIT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
2.24 μg/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ACTARIT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
2.09 μg/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ACTARIT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
4.56 μg × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ACTARIT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
7.66 μg × h/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ACTARIT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
16 μg × h/mL
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ACTARIT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
28.7 μg × h/mL
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ACTARIT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
4.56 μg × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ACTARIT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
4.16 μg × h/mL
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ACTARIT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
0.862 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ACTARIT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
0.803 h
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ACTARIT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
0.909 h
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ACTARIT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
0.851 h
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ACTARIT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
0.86 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ACTARIT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FED
1.13 h
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ACTARIT plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
80%
ACTARIT plasma
Homo sapiens
Doses

Doses

DosePopulationAdverse events​
100 mg 3 times / day multiple, oral
Recommended
Dose: 100 mg, 3 times / day
Route: oral
Route: multiple
Dose: 100 mg, 3 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
100 mg 3 times / day multiple, oral
Recommended
Dose: 100 mg, 3 times / day
Route: oral
Route: multiple
Dose: 100 mg, 3 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Disc. AE: Nephrotic syndrome, Interstitial pneumonia...
AEs leading to
discontinuation/dose reduction:
Nephrotic syndrome
Interstitial pneumonia
Aplastic anemia
Pancytopenia
Agranulocytosis
Thrombocytopenia
Liver disorder
Peptic ulcer
Hemorrhagic colitis
Sources:
AEs

AEs

AESignificanceDosePopulation
Agranulocytosis Disc. AE
100 mg 3 times / day multiple, oral
Recommended
Dose: 100 mg, 3 times / day
Route: oral
Route: multiple
Dose: 100 mg, 3 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Aplastic anemia Disc. AE
100 mg 3 times / day multiple, oral
Recommended
Dose: 100 mg, 3 times / day
Route: oral
Route: multiple
Dose: 100 mg, 3 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Hemorrhagic colitis Disc. AE
100 mg 3 times / day multiple, oral
Recommended
Dose: 100 mg, 3 times / day
Route: oral
Route: multiple
Dose: 100 mg, 3 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Interstitial pneumonia Disc. AE
100 mg 3 times / day multiple, oral
Recommended
Dose: 100 mg, 3 times / day
Route: oral
Route: multiple
Dose: 100 mg, 3 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Liver disorder Disc. AE
100 mg 3 times / day multiple, oral
Recommended
Dose: 100 mg, 3 times / day
Route: oral
Route: multiple
Dose: 100 mg, 3 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Nephrotic syndrome Disc. AE
100 mg 3 times / day multiple, oral
Recommended
Dose: 100 mg, 3 times / day
Route: oral
Route: multiple
Dose: 100 mg, 3 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Pancytopenia Disc. AE
100 mg 3 times / day multiple, oral
Recommended
Dose: 100 mg, 3 times / day
Route: oral
Route: multiple
Dose: 100 mg, 3 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Peptic ulcer Disc. AE
100 mg 3 times / day multiple, oral
Recommended
Dose: 100 mg, 3 times / day
Route: oral
Route: multiple
Dose: 100 mg, 3 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
Thrombocytopenia Disc. AE
100 mg 3 times / day multiple, oral
Recommended
Dose: 100 mg, 3 times / day
Route: oral
Route: multiple
Dose: 100 mg, 3 times / day
Sources:
unhealthy, ADULT
Health Status: unhealthy
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Sources:
PubMed

PubMed

TitleDatePubMed
A new low-field extremity magnetic resonance imaging and proposed compact MRI score: evaluation of anti-tumor necrosis factor biologics on rheumatoid arthritis.
2009
Drug-target interaction prediction from chemical, genomic and pharmacological data in an integrated framework.
2010 Jun 15
Determination of actarit from human plasma for bioequivalence studies.
2010 Nov
Patents

Sample Use Guides

In Vivo Use Guide
Curator's Comment: Actarit was administered at 300 mg/day and was used throughout the study period. The duration of treatment was 24 weeks. During this study there were no significant adverse reactions requiring the withdrawal of treatment.
300 mg/day, duration of treatment is 24 weeks.
Route of Administration: Oral
In Vitro Use Guide
rheumatoid arthritis primary synovial cells were co-cultured with actarit at 10(-4)-10(-7) M
Substance Class Chemical
Created
by admin
on Mon Mar 31 18:05:27 GMT 2025
Edited
by admin
on Mon Mar 31 18:05:27 GMT 2025
Record UNII
HW5B6351RZ
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ACTARIT
INN   JAN   MART.   MI   WHO-DD  
INN  
Official Name English
ORCL
Preferred Name English
YM-340790
Code English
ACTARIT [JAN]
Common Name English
actarit [INN]
Common Name English
ACTARIT [MART.]
Common Name English
ACTARIT [MI]
Common Name English
NSC-170317
Code English
4-ACETYLAMINOPHENYLACETIC ACID
Systematic Name English
(P-ACETAMIDOPHENYL)ACETIC ACID
Common Name English
MIRABEGRON (M9)
Common Name English
Actarit [WHO-DD]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C29634
Created by admin on Mon Mar 31 18:05:27 GMT 2025 , Edited by admin on Mon Mar 31 18:05:27 GMT 2025
Code System Code Type Description
NSC
170317
Created by admin on Mon Mar 31 18:05:27 GMT 2025 , Edited by admin on Mon Mar 31 18:05:27 GMT 2025
PRIMARY
PUBCHEM
2018
Created by admin on Mon Mar 31 18:05:27 GMT 2025 , Edited by admin on Mon Mar 31 18:05:27 GMT 2025
PRIMARY
EPA CompTox
DTXSID0020020
Created by admin on Mon Mar 31 18:05:27 GMT 2025 , Edited by admin on Mon Mar 31 18:05:27 GMT 2025
PRIMARY
ECHA (EC/EINECS)
242-511-3
Created by admin on Mon Mar 31 18:05:27 GMT 2025 , Edited by admin on Mon Mar 31 18:05:27 GMT 2025
PRIMARY
FDA UNII
HW5B6351RZ
Created by admin on Mon Mar 31 18:05:27 GMT 2025 , Edited by admin on Mon Mar 31 18:05:27 GMT 2025
PRIMARY
ChEMBL
CHEMBL1885632
Created by admin on Mon Mar 31 18:05:27 GMT 2025 , Edited by admin on Mon Mar 31 18:05:27 GMT 2025
PRIMARY
MERCK INDEX
m1394
Created by admin on Mon Mar 31 18:05:27 GMT 2025 , Edited by admin on Mon Mar 31 18:05:27 GMT 2025
PRIMARY Merck Index
WIKIPEDIA
ACTARIT
Created by admin on Mon Mar 31 18:05:27 GMT 2025 , Edited by admin on Mon Mar 31 18:05:27 GMT 2025
PRIMARY
EVMPD
SUB05255MIG
Created by admin on Mon Mar 31 18:05:27 GMT 2025 , Edited by admin on Mon Mar 31 18:05:27 GMT 2025
PRIMARY
CAS
18699-02-0
Created by admin on Mon Mar 31 18:05:27 GMT 2025 , Edited by admin on Mon Mar 31 18:05:27 GMT 2025
PRIMARY
INN
6549
Created by admin on Mon Mar 31 18:05:27 GMT 2025 , Edited by admin on Mon Mar 31 18:05:27 GMT 2025
PRIMARY
SMS_ID
100000087677
Created by admin on Mon Mar 31 18:05:27 GMT 2025 , Edited by admin on Mon Mar 31 18:05:27 GMT 2025
PRIMARY
DRUG CENTRAL
84
Created by admin on Mon Mar 31 18:05:27 GMT 2025 , Edited by admin on Mon Mar 31 18:05:27 GMT 2025
PRIMARY
NCI_THESAURUS
C73298
Created by admin on Mon Mar 31 18:05:27 GMT 2025 , Edited by admin on Mon Mar 31 18:05:27 GMT 2025
PRIMARY
Related Record Type Details
PARENT -> METABOLITE
Related Record Type Details
ACTIVE MOIETY