. 2015 Nov 23;36(12):1395–1407. doi: 10.1038/aps.2015.91

Table 3. Development status of antibody agents targeting TLR signaling pathway for SLE treatment.

Compound	Target	Description	Indication	Clinical phase	Dosage regimen	Ref
OPN-305	TLR2 antagonist	Humanized monoclonal IgG4κ antibody targeting TLR2	Myelodysplastic syndrome; Transplant rejection; Autoimmune diseases	Phase II	1.5 mg/kg, iv (patients, efficacy and safety study)	^97,98
NI-0101	TLR4 antagonist	Humanized monoclonal antibody binding to human TLR4	Inflammation; Autoimmune disorders	Phase I	≤15 mg/kg, iv (healthy objects, tolerability study)	⁹⁹
Mab 9F3	Anti-IFN-α	Murine monoclonal antibody that neutralizes human IFN-α	Type 1 diabetes; SLE	Biological testing	-	-
13H5	Anti-IFN-α	Human monoclonal IgG1 antibody against human IFN-α	Transplant rejection; SLE	Biological testing	-	-
ACO-1	Anti-IFN-α	IgG2a murine monoclonal antibody against IFN-α	Psoriasis; SLE	Biological testing	-	-
AGS-009 (NNC-0152-0000-0001)	Anti-IFN-α	Humanized monoclonal IgG4 antibody targeting human IFN-α	SLE	Phase I	0.01-30 mg/kg, iv (patients, tolerability study)	¹⁰⁵
Rontalizumab (PRO-155767)	Anti-IFN-α	Recombinant humanized monoclonal antibody targeting human IFN-α	SLE	Phase II (Discontinued)	750 mg, once/4 week, iv or 300 mg, once/2 week, sc (patients, efficacy and safety study)	¹⁰⁰
Sifalimumab (MEDI-545; MDX-1103)	Anti-IFN-α	Full human monoclonal IgG1 antibody targeting human IFN-α	Inflammatory myopathy; Myositis; Polymyositis; Psoriasis; SLE	Phase II	200, 600 and 1200 mg, once/2 week, iv (patients, efficacy and safety study)	^{101,102,103,104}
Anifrolumab (MEDI-546; MDX-1333)	Anti-IFN α receptor 1	Full human monoclonal IgG1κ antibody targeting the type I IFN receptor 1	Scleroderma; SLE	Phase II/III	100, 300 and 1000 mg, once/4 week, iv (patients, efficacy and safety study)	^106,107