ACTARIT

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 Search

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
Sources: http://www.ncbi.nlm.nih.gov/pubmed/9918236
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.

Originator

Approval Year

Conditions

Condition	Modality	Targets	Highest Phase	Product
Rheumatoid arthritis 320 Sources: http://www.ncbi.nlm.nih.gov/pubmed/9918236	Secondary		Approved 8583	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
2.24 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=17	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 OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=17	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 OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=17	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 OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=17	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 OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=18	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 OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=18	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

Value	Dose	Analyte	Population
4.56 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=17	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 OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=17	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 OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=17	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 OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=17	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 OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=18	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 OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=18	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

T_1/2

Value	Dose	Analyte	Population
0.862 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=17	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 OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=17	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 OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=17	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 OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=17	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 OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=18	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 OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=18	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

F_unbound

Value	Dose	Co-administered	Analyte	Population
80% OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/530263_1149031F1030_1_14F_1F.pdf#page=19			ACTARIT plasma	Homo sapiens

Doses

Dose	Population	Adverse 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: https://pubmed.ncbi.nlm.nih.gov/24383899/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/24383899/	Sources: https://pubmed.ncbi.nlm.nih.gov/24383899/
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: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738	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: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738

AEs

AE	Significance	Dose	Population
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: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738
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: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738
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: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738
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: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738
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: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738
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: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738
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: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738
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: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738
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: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.rad-ar.or.jp/siori/english/kekka.cgi?n=39738

PubMed

Title	Date	PubMed
A new low-field extremity magnetic resonance imaging and proposed compact MRI score: evaluation of anti-tumor necrosis factor biologics on rheumatoid arthritis.	2009	19370385
Drug-target interaction prediction from chemical, genomic and pharmacological data in an integrated framework.	2010 Jun 15	20529913
Determination of actarit from human plasma for bioequivalence studies.	2010 Nov	21969744

Patents

Sample Use Guides

In Vivo Use Guide

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

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