Table 2.
Inflammasomes inhibitors.
| Therapeutic agents | Targets | Potential Mechanism | Diseases |
|---|---|---|---|
| Anakinra | IL-1 receptor | Recombinant IL-1Ra | RA, Destructive joint process Autoimmune disease (FMF, CAPS, HIDS, TRAPs), Systemic/common inflammatory diseases (Gout, T2D, Systolic heart failure) |
| Rilonacept | IL-1β | Extracellular portion of the IL-1R and the Fc domain of human IgG1 | CAPS, Diabetes, Gout, Recurrent Pericarditis |
| Canakinumab | IL-1β | Anti-IL-1β antibody | MWS, FCAS |
| Ritonavir | Caspase-1 | Protease inhibitor | Pancreatitis |
| Avastin | P2X7 | P2X7 inhibitor | Solid tumor |
| Glyburide | NLRP3 (Indirect) | Broad-spectrum inhibitor of the ATP-binding cassette transporter and P2X7R | Type2 diabetes |
| Gevokizumab (Xoma 052) | IL-1β | Anti-IL-1β antibody | Diabetes, Osteoarthritis |
| GSK 1070806 | IL-18 | Anti-IL-18 antibody | Diabetes, IBD |
| Ac-YVAD-CHO | Caspase-1 | Caspase-1 inhibitory peptide | Endotoxemia, Pancreatitis |
| VX-765 | Caspase-1 | Selective inhibitor of caspase-1 | CAPS, MWS, RA |
| Pralnacasan (VX-740) | Caspase-1 | Caspase-1 inhibitor | RA, OA |
| Thalidomide | Caspase-1 inhibitor | Myeloma | |
| CRID3 | ASC | Blocking putative association between GSTO1 and ASC | IBD |
| MCC950 | NLRP3 | Inhibitor of ASC oligomerization | experimental autoimmune encephalomyelitis (EAE) |
| AZD9056 | P2X7 | Inhibitor of NLRP3 ATPase | RA |
| GSK1482160 | P2X7 | P2X7 antagonist | RA |
| Bay 11-7082 | NF-κB/NLRP3 ATPase | Inhibitor of NLRP3 ATPase | psoriasis |
| Parthenolide | Caspase-1/NF-κB NLRP3 ATPase | Inhibitor of NLRP1/3/4 or caspase-1, inhibitor of NLRP3 ATPase | Dermatitis |
| 16673-34-0 | NLRP3 (Indirect) | Glyburide derivatives | Acute myocardial infarction |
| β-Hydroxybutyrate (BHB) | NLRP3 (Indirect) | Inhibits K+ efflux resulting in reduced oligomerization ASC and IL-1β/18 release | MWS, FCAS, AD |
| JC124 | NLRP3 | blocks ASC aggregation, caspase-1 activation, and IL-1β secretion. | acute myocardial infarction |
| FC11A-2 | NLRP3 | hindered the proximity-induced autocleavage of procaspase-1 | experimental colitis |
| CY-09 | NLRP3 ATPase | directly binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 ATPase activity | CAPS, T2D |
| OLT1177 | NLRP3 ATPase | reduced ATPase activity of NLRP3 | CAPS |
| Tranilast | NLRP3 oligomerization | directly binds to the NACHT domain of NLRP3 and blocks NLRP3 oligomerization | CAPS, T2D |
| Oridonin | Cysteine 279 of NLRP3 | block the interaction between NLRP3 and NEK7 | peritonitis, gouty arthritis, T2D |