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Details

Stereochemistry RACEMIC
Molecular Formula C16H26NO4S
Molecular Weight 328.447
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 1

SHOW SMILES / InChI
Structure of SUPLATAST

SMILES

CCOCC(O)COC1=CC=C(NC(=O)CC[S+](C)C)C=C1

InChI

InChIKey=DYZJXZOQQRXDLE-UHFFFAOYSA-O
InChI=1S/C16H25NO4S/c1-4-20-11-14(18)12-21-15-7-5-13(6-8-15)17-16(19)9-10-22(2)3/h5-8,14,18H,4,9-12H2,1-3H3/p+1

HIDE SMILES / InChI

Description

Suplatast is a novel immunomodulator that can adjust the imbalance in the Th1/Th2 immune response and shows clear clinical efficacy against bronchial asthma (BA). Suplatast tosilate helps to suppress the production of IgE, to block the production of cytokines and to suppress allergy-related eosinophils. Clinical studies on the efficacy of Suplatast were carried out in Japan. Suplatast showed adequate efficacy for the treatment of BA, allergic rhinitis and atopic dermatitis. Suplatast is now available for the management of BA as a controller of the Th2-dependent allergic inflammation. Suplatast tosilate is not approved in the United States, but is available in Japan as Tosilart® and IPD Capsules®. IPD-1151T (suplatast tosilate) was originated by Taiho and is being developed for the treatment of interstitial cystitis and chronic non-bacterial prostatitis as additional indications. IPD-1151T treatment for 1 year resulted in a significantly increased bladder capacity and decreased symptoms, such as urinary urgency, frequency and lower abdominal pain, in patients with nonulcerative interstitial cystitis.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown
Primary
Unknown
Primary
Unknown
Primary
Unknown
Primary
Unknown
Primary
Unknown
Primary
Unknown
Preventing
Unknown
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
27.6 ng/mL
2 mg/kg single, oral
SUPLATAST plasma
Homo sapiens
59.6 ng/mL
3 mg/kg single, oral
SUPLATAST plasma
Homo sapiens
39.6 ng/mL
100 mg single, oral
SUPLATAST plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
230.5 ng × h/mL
2 mg/kg single, oral
SUPLATAST plasma
Homo sapiens
407.4 ng × h/mL
3 mg/kg single, oral
SUPLATAST plasma
Homo sapiens
257 ng × h/mL
100 mg single, oral
SUPLATAST plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
3.1 h
2 mg/kg single, oral
SUPLATAST plasma
Homo sapiens
3 h
3 mg/kg single, oral
SUPLATAST plasma
Homo sapiens
2.8 h
100 mg single, oral
SUPLATAST plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
97.87%
SUPLATAST serum
Homo sapiens

Doses

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
IPD-1151T (suplatast tosilate) 100 mg capsules was orally administered to the patients 3 times daily for 12 weeks of treatment period.
Route of Administration: Oral
In Vitro Use Guide
In vitro, NCI-H292 cells were preincubated with suplatast tosilate (0.1-100 u/mL) 1 hour.