DAPANSUTRILE

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C4H7NO2S
Molecular Weight	133.169
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CS(=O)(=O)CCC#N

InChI

InChIKey=LQFRYKBDZNPJSW-UHFFFAOYSA-N

InChI=1S/C4H7NO2S/c1-8(6,7)4-2-3-5/h2,4H2,1H3

HIDE SMILES / InChI

Molecular Formula	C4H7NO2S
Molecular Weight	133.169
Charge	0
Count

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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/30747785 | https://www.ncbi.nlm.nih.gov/pubmed/30075804 | https://ard.bmj.com/content/78/Suppl_1/A70 | http://www.olatec.com/lead-compound.html

Dapansutrile is an inhibitor of the NLRP3 inflammasome, developed by Olatec Therapeutics LLC. NLRP3 inflammasome is a driver of sterile inflammation in response to myocardial ischemia-reperfusion and other inflammatory conditions. Dapansutrile limits infarct size and prevents left ventricular systolic dysfunction in the mouse model of ischemia-reperfusion injury and suppresses joint inflammation in the mouse model of acute arthritis. Dapansutrile demonstrated a clinical and inflammatory cytokine response in a clinical trial for the treatment of acute gout and is being investigated for the treatment of Systolic Heart Failure and Schnitzler Syndrome.

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Interleukin-1 beta 22 Target ID: CHEMBL1909490 Sources: https://adisinsight.springer.com/drugs/800036472\|http://www.olatec.com/science.html	Modulator 846
inflammasome complex 2 Target ID: GO:0061702 Sources: https://adisinsight.springer.com/drugs/800036472	Inhibitor 8504

C_max

Value	Dose	Analyte	Population
2700 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29378952/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	DAPANSUTRILE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
9800 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29378952/	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	DAPANSUTRILE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
32000 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29378952/	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	DAPANSUTRILE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4800 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29378952/	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DAPANSUTRILE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
15800 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29378952/	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DAPANSUTRILE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
41400 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29378952/	1000 mg 1 times / day multiple, oral dose: 1000 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DAPANSUTRILE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
40121.19 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29378952/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	DAPANSUTRILE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
157378.19 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29378952/	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	DAPANSUTRILE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
464809.56 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29378952/	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	DAPANSUTRILE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
70288.75 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29378952/	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DAPANSUTRILE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
260409.24 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29378952/	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DAPANSUTRILE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
723127.43 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29378952/	1000 mg 1 times / day multiple, oral dose: 1000 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DAPANSUTRILE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
23.01 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29378952/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	DAPANSUTRILE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
22.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29378952/	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	DAPANSUTRILE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
24.15 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29378952/	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	DAPANSUTRILE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
16.01 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29378952/	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DAPANSUTRILE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
21.34 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29378952/	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DAPANSUTRILE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
24.72 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29378952/	1000 mg 1 times / day multiple, oral dose: 1000 mg route of administration: Oral experiment type: MULTIPLE co-administered:	DAPANSUTRILE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Substance Class	Chemical Created by `admin` on `Mon Mar 31 22:17:39 GMT 2025` Edited by `admin` on `Mon Mar 31 22:17:39 GMT 2025`
Record UNII	2Z03364G96
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

dapansutrile [INN]

Preferred Name

English

DAPANSUTRILE

Official Name

English

OLT1177

Code

English

PROPANENITRILE, 3-(METHYLSULFONYL)-

Systematic Name

English

3-METHYLSULFONYLPROPIONITRILE

Systematic Name

English

DAPANSUTRILE [USAN]

Common Name

English

Dapansutrile [WHO-DD]

Common Name

English

OLT-1177

Code

English

Code System Code Type Description

CAS

54863-37-5