Synonyms: OLT-1177 | OLT1177
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].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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No information available. |
Summary of Clinical Use |
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 |