SUPLATAST TOSILATE

Details

Stereochemistry	RACEMIC
Molecular Formula	C16H26NO4S.C7H7O3S
Molecular Weight	499.641
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=CC=C(C=C1)S([O-])(=O)=O.CCOCC(O)COC2=CC=C(NC(=O)CC[S+](C)C)C=C2

InChI

InChIKey=RYVJQEZJUFRANT-UHFFFAOYSA-N

InChI=1S/C16H25NO4S.C7H8O3S/c1-4-20-11-14(18)12-21-15-7-5-13(6-8-15)17-16(19)9-10-22(2)3;1-6-2-4-7(5-3-6)11(8,9)10/h5-8,14,18H,4,9-12H2,1-3H3;2-5H,1H3,(H,8,9,10)

HIDE SMILES / InChI

Molecular Formula	C16H26NO4S
Molecular Weight	328.447
Charge	1
Count

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

Molecular Formula	C7H7O3S
Molecular Weight	171.194
Charge	-1
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.astellas.com/en/corporate/news/yamanouchi/030123.html
Curator's Comment: Description was created based on several sources, including https://www.jstage.jst.go.jp/article/allergolint/54/4/54_4_533/_pdf

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 Target	Pharmacology	Condition	Potency
Interleukin-4 2 Target ID: P05112 Gene ID: 3565.0 Gene Symbol: IL4 Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/10466742	Inhibitor 8504
Interleukin-5 3 Target ID: CHEMBL1169600 Sources: http://www.ncbi.nlm.nih.gov/pubmed/10466742	Inhibitor 8504
Histidine decarboxylase 9 Target ID: CHEMBL3243911 Sources: http://www.ncbi.nlm.nih.gov/pubmed/19596986	Inhibitor 8504

Conditions

Condition	Modality	Highest Phase	Product
Cutaneous mastocytosis 2 Sources: http://www.ncbi.nlm.nih.gov/pubmed/25779849	Primary	Basic research	Unknown Approved Use Unknown
Eosinophilic cystitis 2 Sources: http://www.ncbi.nlm.nih.gov/pubmed/25293800	Primary	Basic research	Unknown Approved Use Unknown
Non-episodic angioedema 2 Sources: http://www.ncbi.nlm.nih.gov/pubmed/24723649	Primary	Basic research	Unknown Approved Use Unknown
Bronchial asthma 50 Sources: https://www.jstage.jst.go.jp/article/allergolint/54/4/54_4_533/_pdf	Primary	Phase III 665	Unknown Approved Use Unknown
Kimura's disease 2 Sources: http://www.ncbi.nlm.nih.gov/pubmed/21914581	Primary	Basic research	Unknown Approved Use Unknown
Interstitial cystitis 6 Sources: http://www.clinicaltrials.jp/user/showCteDetailE.jsp?japicId=JapicCTI-060257	Primary	Phase III 665	Unknown Approved Use Unknown
Perennial allergic rhinitis 47 Sources: http://www.ncbi.nlm.nih.gov/pubmed/9879412	Primary	Basic research	Unknown Approved Use Unknown
Bronchial asthma 50 Sources: http://www.ncbi.nlm.nih.gov/pubmed/24561769	Preventing	Phase II 1147	Unknown Approved Use Unknown
Vitiligo 9 Sources: http://www.ncbi.nlm.nih.gov/pubmed/9609984	Primary	Basic research	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
27.6 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/400107_4490016R1020_1_03B_1F.pdf#page=17	2 mg/kg single, oral dose: 2 mg/kg route of administration: Oral experiment type: SINGLE co-administered:	SUPLATAST plasma	Homo sapiens population: UNHEALTHY age: CHILD sex: FEMALE / MALE food status: FED
59.6 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/400107_4490016R1020_1_03B_1F.pdf#page=17	3 mg/kg single, oral dose: 3 mg/kg route of administration: Oral experiment type: SINGLE co-administered:	SUPLATAST plasma	Homo sapiens population: UNHEALTHY age: CHILD sex: FEMALE / MALE food status: FED
39.6 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/400107_4490016R1020_1_03B_1F.pdf#page=17	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	SUPLATAST plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED

AUC

Value	Dose	Analyte	Population
230.5 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/400107_4490016R1020_1_03B_1F.pdf#page=17	2 mg/kg single, oral dose: 2 mg/kg route of administration: Oral experiment type: SINGLE co-administered:	SUPLATAST plasma	Homo sapiens population: UNHEALTHY age: CHILD sex: FEMALE / MALE food status: FED
407.4 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/400107_4490016R1020_1_03B_1F.pdf#page=17	3 mg/kg single, oral dose: 3 mg/kg route of administration: Oral experiment type: SINGLE co-administered:	SUPLATAST plasma	Homo sapiens population: UNHEALTHY age: CHILD sex: FEMALE / MALE food status: FED
257 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/400107_4490016R1020_1_03B_1F.pdf#page=17	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	SUPLATAST plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED

T_1/2

Value	Dose	Analyte	Population
3.1 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/400107_4490016R1020_1_03B_1F.pdf#page=17	2 mg/kg single, oral dose: 2 mg/kg route of administration: Oral experiment type: SINGLE co-administered:	SUPLATAST plasma	Homo sapiens population: UNHEALTHY age: CHILD sex: FEMALE / MALE food status: FED
3 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/400107_4490016R1020_1_03B_1F.pdf#page=17	3 mg/kg single, oral dose: 3 mg/kg route of administration: Oral experiment type: SINGLE co-administered:	SUPLATAST plasma	Homo sapiens population: UNHEALTHY age: CHILD sex: FEMALE / MALE food status: FED
2.8 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/400107_4490016R1020_1_03B_1F.pdf#page=17	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	SUPLATAST plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED

F_unbound

Value	Dose	Co-administered	Analyte	Population
97.87% OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/400107_4490016R1020_1_03B_1F.pdf#page=34			SUPLATAST serum	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/21980828/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/21980828/	Sources: https://pubmed.ncbi.nlm.nih.gov/21980828/

PubMed

Title	Date	PubMed
Suplatast tosilate for treating cutaneous mastocytosis.	2015-03-18	25779849
[A case report of eosinophilic cystitis treated with oral suplatast tosilate].	2014-09	25293800
Treatment of non-episodic angioedema associated with eosinophilia with suplatast tosilate, an anti-allergic selective Th2 cytokine inhibitor.	2014-04-12	24723649
Kimura's disease treated with suplatast tosilate and loratadine.	2011-09-15	21914581
Suplatast tosilate inhibits goblet-cell metaplasia of airway epithelium in sensitized mice.	2000-04	10756224
Suplatast tosilate (IPD), a new immunoregulator, is effective in vitiligo treatment.	1998-04	9609984
Suplatast tosilate affects the initial increase in specific IgE and interleukin-4 during immunotherapy for perennial allergic rhinitis.	1998	9879412

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.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 21:38:06 GMT 2025` Edited by `admin` on `Mon Mar 31 21:38:06 GMT 2025`
Record UNII	C9J89787U1
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

SUPLATAST TOSYLATE

Preferred Name

English

SUPLATAST TOSILATE

Official Name

English

Suplatast tosilate [WHO-DD]

Common Name

English

IPD

Brand Name

English

suplatast tosilate [INN]

Common Name

English

SUPLATAST TOSILATE [MART.]

Common Name

English

SUPLATAST TOSYLATE [MI]

Common Name

English

SULFONIUM, (3-((4-(3-ETHOXY-2-HYDROXYPROPOXY)PHENYL)AMINO)-3-OXOPROPYL)DIMETHYL-, SALT WITH 4-METHYLBENZENESULFONIC ACID (1:1)

Common Name

English

SUPLATAST TOSILATE [JAN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C574