Table 2.

The development status of TLR antagonists/inhibitors: class of SMIs.

Compound	Target	Indication	Status	Company	References
TAK-242	TLR4	Septic shock	Phase IIIa	Takeda	Rice et al., 2010; Matsunaga et al., 2011
Candesartan1	ARB, TLR2/4	Anti-inflammation	Animal study	–	Dasu et al., 2009
Valsartan1	ARB, TLR4	Myocardial IR injury	Animal study	Novartis Pharma	Yang et al., 2009
Fluvastatin1	TLR4	Chronic heart failure	Experimental	–	Foldes et al., 2008
Simvastatin1	TLR4	Atherosclerosis	Experimental	–	Methe et al., 2005
Atorvastatin1	TLR4	Atherosclerosis	Animal study	–	Fang et al., 2014
ST2825	MyD88	SLE	Experimental	–	Loiarro et al., 2007; Capolunghi et al., 2010
CQ, HCQ	TLR7/8/9	RA, SLE	Clinical use	Generic	Wozniacka et al., 2006; Lesiak et al., 2010; Lee et al., 2011
CQ, HCQ	TLR7/8/9	Cerebrovascular ischemia, lupus-associated hypertension, endothelial dysfunction	Animal study	–	Cui et al., 2013; Gomez-Guzman et al., 2014
CQ	TLR7/8/9	Chikungunya infection	Phase IIIa	Generic	Paton et al., 2011; Borges et al., 2013
		Prevention of influenza	Phase IIb
		Dengue infection	Phase I/IIb
CpG-52364	TLR7/8/9	RA, SLE	Phase Ic	Pfizer	Lipford et al., 2007
SM934	TLR7/9	SLE, autoimmune diseases	IND filed1	Shanghai Institute of Materia Medica	Hou et al., 2011; Wu et al., 2016

ARB, angiotensin II receptor blocker; CQ, chloroquine; HCQ, hydroxychloroquine; RA, rheumatoid arthritis; SLE, systemic lupus erythematosus; IND, investigational new drug application.

^aStudy terminated.

^bUnknown status.

^cCompleted with unknown results.

¹Clinical drugs with new applications.