TABLE 1.
Target specificity | Inhibitor | Diseases | Clinical status | References | |
NLRP3 | MCC950 | Inflammatory diseases | Phase II | Coll et al., 2015 | |
NLRP3 | Tranilast (MK-341) | Inflammatory diseases | Approved | Huang et al., 2018 | |
NLRP3 | OLT1177 | Inflammatory diseases | Phase II | Marchetti et al., 2018 | |
NLRP3 | CY-09 | Inflammatory diseases | Preclinical | Jiang et al., 2017 | |
NLRP3 | JC171 | Inflammatory diseases | Preclinical | Guo et al., 2017 | |
NLRP3 | JC124 | Traumatic neuroinflammatory response | Preclinical | Kuwar et al., 2019 | |
NLRP3 | INF39 | Inflammatory diseases | Preclinical | Cocco et al., 2017 | |
NLRP3 | NBCs | Inflammatory diseases | Preclinical | Baldwin et al., 2017 | |
NLRP3 | Apigenin | Inflammatory diseases | Preclinical | Lim et al., 2018 | |
NLRP1, NLRP3, NK-κB, IKKβ | Parthenolide | Inflammatory diseases, Cystic fibrosis | Preclinical | Juliana et al., 2010 | |
NLRP3 | ILG | Obesity, hypercholesterolemia, and insulin resistance | Preclinical | Honda et al., 2014 | |
NLRP3 | Fc11a-2 | Inflammatory diseases | Preclinical | Liu et al., 2013 | |
NLRP3 | NLRP3 | BOT-4-one | Inflammatory diseases | Preclinical | Shim et al., 2017 |
NLRP3 | Glyburide | Inflammatory diseases | Preclinical | Lamkanfi et al., 2009 | |
NLRP3 | MNS | Inflammatory diseases | Preclinical | He et al., 2014 | |
NLRP3 | Flufenamic acid | Alzheimer’s disease | Preclinical | Daniels et al., 2016 | |
NLRP3 | 16673-34-0 | Acute myocardial infarction | Preclinical | Marchetti et al., 2014 | |
NLRP3 | Oridonin | Inflammatory diseases | Preclinical | He et al., 2018 | |
NLRP3 | Kynurenic acid | Stress-related colonic disorder | Preclinical | Zheng et al., 2019 | |
NLRP3 | Formononetin | Inflammatory diseases | Preclinical | Wu D. et al., 2018 | |
NLRP3 | Triptolide | Cardioprotective | Preclinical | Li et al., 2017 | |
NLRP3 | Andrographolide | Inflammatory diseases | Preclinical | Guo et al., 2014 | |
NLRP3 | Celastrol | Inflammatory diseases | Preclinical | Xin et al., 2017 | |
NLRP3 | BHB | Inflammatory diseases | Preclinical | Youm et al., 2015 | |
Caspase-1 | Caspase-1 | VX-740 | Inflammatory diseases | Preclinical | Rudolphi et al., 2003 |
Caspase-1 | VX-765 | Inflammatory diseases | Preclinical | Wannamaker et al., 2007 | |
IL-1R1 | Anakinra | Cystic fibrosis | Approved | Iannitti et al., 2016 | |
IL-1β | Canakinumab | Cardiovascular events | Approved | Shah et al., 2018 | |
IL-1β | Gevokizumab | Cardiac remodeling and coronary dysfunction | Preclinical | Harouki et al., 2017 | |
IL-1β | Pralnacasan | Inflammatory diseases | Preclinical | Rudolphi et al., 2003 | |
Cytokines | IL-1β | Curcumin | Inflammatory diseases | Preclinical | Gong et al., 2018 |
IL-1βR | Rilonacept | CAPS | Approved | Gillespie et al., 2010 | |
IL-1α | Xilonix | Femoral artery restenosis | Phase II | El Sayed et al., 2016 | |
IL-4/IL-13 | SAR156597 | IPF | Phase II | Raghu et al., 2018 | |
TGF-β | SHP-627 | Cardiac fibrosis | Preclinical | Zhang et al., 2012 | |
PDGFR | Imatinib | NSF, IPF | Phase II | Daniels et al., 2010 | |
Endothelin-1 receptor | Macitentan | Heart failure | Phase II | NCT03153111 | |
Angiotensin II | Losartan | Cardiac fibrosis | Preclinical | Gay-Jordi et al., 2013 | |
Related pathways | Relaxin receptor | Serelaxin | Cardiac fibrosis | Preclinical | Wu X. P. et al., 2018 |
IKK | IMD-1041 | Cardiac fibrosis | Preclinical | Tanaka et al., 2012 | |
IKK | Bardoxolone methyl | Pulmonary hypertension | Phase II | Chin et al., 2018 | |
NF-κB | BAY 11-7082 | Inflammatory diseases | Preclinical | Irrera et al., 2017 | |
NK-κB | Baicalein | Renal fibrosis | Preclinical | Zhao et al., 2016 | |
NF-κB | Wogonoside | Inflammatory diseases | Preclinical | Sun et al., 2015 | |
JNK | Tanzisertib (CC930) | IPF | Phase II | NCT01203943 | |
TLR-4 | Alpinetin | Inflammatory diseases | Preclinical | He X. et al., 2016 | |
MAPK | MMI-0100 | Cardiac fibrosis | Preclinical | Meng et al., 2017 | |
Peroxiredoxin 1 | AI-44 | Inflammatory diseases | Preclinical | Liu W. et al., 2018 | |
AhR/Nrf2/NQO1 | Cardamonin | Inflammatory diseases | Preclinical | Wang K. et al., 2018 | |
AMPK/ULK1/p62 | Ginsenoside Rd | Inflammatory diseases | Preclinical | Liu C. et al., 2018 | |
Cathepsin B | VBY-376 | Liver fibrosis | Preclinical | Wree et al., 2016 | |
Smad2/4 | Pentoxifylline | Cardiac fibrosis | Preclinical | Zhang et al., 2016 | |
NOX4 | GKT-137831 | Cardiac fibrosis | Preclinical | Zhao et al., 2015 | |
ROS | N-acetylcysteine | Cardiac fibrosis | Preclinical | Giam et al., 2016 | |
ROS | Levornidazole | Inflammatory diseases | Preclinical | Wang et al., 2015 | |
ROS | Mitoquinone | Cardiac fibrosis | Preclinical | Goh et al., 2019 | |
ROS | LGM2605 | Radiation damage | Preclinical | Chatterjee et al., 2019 |