Table 5.

The development status of TLR antagonists/inhibitors: classes of lipid A analogs, miRNAs and “nano-drugs.”

Compound	Target	Indication	Status	Company	References
CLASS OF LIPID A ANALOGS
Eritoran (E5564)	TLR4/MD2	Sepsis	Phase IIIa	Eisai (Boston)	Barochia et al., 2011; Opal et al., 2013
		Influenza infection, cardiac hypertrophy, myocardial IR injury, renal IR injury	Animal study	–	Shimamoto et al., 2006; Liu et al., 2010; Ehrentraut et al., 2011; Shirey et al., 2013
CLASS OF miRNAs
miR-146a	TLR4	Autoimmune diseases, SLE	Animal study	–	Taganov et al., 2006; Tang et al., 2009; Boldin et al., 2011; Pan et al., 2012
miR-21	TLR4	Anti-inflammation	Animal study	–	Sheedy et al., 2010
CLASS OF “NANO-DRUGS”
NAHNP	TLR4	Anti-inflammation	Experimental	–	Babazada et al., 2014a,b
HDL-like NP	TLR4	Anti-inflammation	Experimental	–	Foit and Thaxton, 2016
Bare GNP	TLR4	Eye inflammation	Animal study	–	Pereira et al., 2012
Glycolipid-coated GNP	TLR4/MD2	Sepsis	Experimental	–	Rodriguez Lavado et al., 2014
Peptide-GNP hybrid	TLR2/3/4/5	Anti-inflammation	Experimental	–	Yang et al., 2015, 2016

SLE. systemic lupus erythematosus; NAHNP, non-anticoagulant heparin nanoparticle; HDL, high-density lipoprotein; NP, nanoparticle; GNP, gold nanoparticle.

^aStudy discontinued.