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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
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

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

ConditionModalityTargetsHighest PhaseProduct
Secondary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
2.24 μg/mL
100 mg single, oral
ACTARIT plasma
Homo sapiens
3.87 μg/mL
200 mg single, oral
ACTARIT plasma
Homo sapiens
7.91 μg/mL
400 mg single, oral
ACTARIT plasma
Homo sapiens
14.1 μg/mL
800 mg single, oral
ACTARIT plasma
Homo sapiens
2.24 μg/mL
100 mg single, oral
ACTARIT plasma
Homo sapiens
2.09 μg/mL
100 mg single, oral
ACTARIT plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
4.56 μg × h/mL
100 mg single, oral
ACTARIT plasma
Homo sapiens
7.66 μg × h/mL
200 mg single, oral
ACTARIT plasma
Homo sapiens
16 μg × h/mL
400 mg single, oral
ACTARIT plasma
Homo sapiens
28.7 μg × h/mL
800 mg single, oral
ACTARIT plasma
Homo sapiens
4.56 μg × h/mL
100 mg single, oral
ACTARIT plasma
Homo sapiens
4.16 μg × h/mL
100 mg single, oral
ACTARIT plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
0.862 h
100 mg single, oral
ACTARIT plasma
Homo sapiens
0.803 h
200 mg single, oral
ACTARIT plasma
Homo sapiens
0.909 h
400 mg single, oral
ACTARIT plasma
Homo sapiens
0.851 h
800 mg single, oral
ACTARIT plasma
Homo sapiens
0.86 h
100 mg single, oral
ACTARIT plasma
Homo sapiens
1.13 h
100 mg single, oral
ACTARIT plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
80%
ACTARIT plasma
Homo sapiens

Doses

AEs

PubMed

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
Record UNII
HW5B6351RZ
Record Status Validated (UNII)
Record Version