Table 1: Development status of oligonucleotide agents that target TLRs for SLE treatment.

From: Toll-like receptors: potential targets for lupus treatment

CompoundTargetSequenceIndicationClinical phaseDosage regimenRef
IRS-954TLR7 and TLR9 antagonist5′-TGCTCCTGG AGGGGTTGT-3′SLEPreclinical15 and 45 μg, twice/week, sc (NZB/W F1 mice)66,67,68
DV-1179TLR7 and TLR9 antagonist-SLEPhase I/II≤60 mg/week, sc (patients, tolerability study)69
IMO-3100TLR7 and TLR9 antagonist-Multiple sclerosis; Plaque psoriasis; Rheumatoid arthritis; SLEPhase II0.16 and 0.32 mg/kg, once/week, sc (patients)70,71
IMO-8400TLR7, TLR8 and TLR9 antagonist-Graft-versus-host Disease; Arthritis; Sjogren's syndrome; Plaque psoriasis; SLEPhase II0.3 and 0.6 mg/kg, once/week, sc (patients)72
IRO-5TLR9 antagonist5′-CTATCTGAC GTTCTCTGT-3′SLEBiological100 μg, once/week, sc (MRL/lpr mice)73
Testing300 μg, once/2 week, sc (NZB/W F1 mice)
INH-ODN-24888TLR7 and TLR9 antagonist5′-TCCTGGCG GGGAAGT-3′SLEPreclinical-74,75