dapansutrile   Click here for help

GtoPdb Ligand ID: 10056

Synonyms: OLT-1177 | OLT1177
Immunopharmacology Ligand
Compound class: Synthetic organic
Comment: Dapansutrile (OLT1177) acts as a NLRP3 inflammasome inhibitor. It is a clinical candidate that is being developed by Olatec Therapeutics. Inhibition of the NLRP3 inflammasome reduces maturation of the pro-inflammatory, disease-associated cytokines IL-1β and IL-18 [3]. Immunoprecipitation and FRET analysis indicates that OLT1177 inhibits inflammasome oligomerization by blocking NLRP3-ASC, and NLRP3-caspase-1 interaction, but may also directly target NLRP3 (as assessed by inhibition of recombinant NLRP3 ATPase activity by dapansutrile) [3].
2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 3
Hydrogen bond donors 0
Rotatable bonds 2
Topological polar surface area 66.31
Molecular weight 133.02
XLogP -0.32
No. Lipinski's rules broken 0
SMILES / InChI / InChIKey
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Canonical SMILES N#CCCS(=O)(=O)C
Isomeric SMILES N#CCCS(=O)(=O)C
InChI InChI=1S/C4H7NO2S/c1-8(6,7)4-2-3-5/h2,4H2,1H3
InChI Key LQFRYKBDZNPJSW-UHFFFAOYSA-N
No information available.
Summary of Clinical Use Click here for help
Clinical trials using dapansutrile (OLT1177) in acute and chronic inflammatory conditions were initiated, to evaluate both topical and oral efficacy [2,6]. The only active study listed on ClinicalTrials.org in Feb. 2024 was in participants with gouty arthritis. There are also plans to assess dapansutrile to tackle neuroinflammatory pathology in Parkinson's disease [5] based on evidence from preclinical animal models [1].

SARS-CoV-2 and COVID-19: Dapansutrile's anti-inflammatory potential (via oral administration) was planned to be investigated in COVID-19 patients with moderate symptoms, but that clinical trial (NCT04540120) was terminated in response to the successful deployment of anti-SARS-CoV-2 vaccines.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT04540120 Safety and Efficacy of Dapansutrile for Treatment of Moderate COVID-19 Symptoms and Evidence of Early Cytokine Release Syndrome Phase 2 Interventional Olatec Therapeutics LLC
NCT01768975 Phase 2 Efficacy Trial of OLT1177 Gel in Subjects With Moderate to Severe Pain Associated With OA of the Knee Phase 2 Interventional Olatec Therapeutics LLC
NCT02104050 Study of OLT1177 Gel to Treat Moderate to Severe OA Knee Pain Phase 2 Interventional Olatec Therapeutics LLC