Table 1.
The characteristics and clinical applications of inhibitors targeting innate immune sensors in autoimmune diseases
| Target | Inhibitor | Character | Application | Autoimmune disease | References |
|---|---|---|---|---|---|
| Inhibitors targeting innate receptors | |||||
| TLR4 | NI-0101 | Antibody | Phase II clinical trial | RA | [145] |
| TLR3/4 | Baclofen | Small molecule | Phase III clinical trial | MS | [146, 147] |
| TLR7/9 | IMO-3100 | Oligonucleotides | Phase II clinical trial | Psoriasis | [209] |
| TLR7/9 | Chloroquine | Small molecule | Clinical medicine | SLE and RA | [46, 141] |
| TLR7/9 | Hydroxychloroquine | Small molecule | Clinical medicine | SLE and RA | [46, 141] |
| TLR7/9 | Quinacrine | Small molecule | Clinical medicine | SLE and RA | [46, 141] |
| TLR7/8/9 | CpG-52364 | Small molecule | Phase I clinical trial | SLE | [143] |
| TLR7/8/9 | IMO-8400 | Oligonucleotides | Phase II clinical trial | Psoriasis | [144] |
| Inhibitors targeting signal transduction molecules | |||||
| IRAK4 | PF-06650833 | Small molecule | Phase II clinical trial | RA | [171] |
| IRAK4 | BAY1834845 | Small molecule | Phase I clinical trial | RA and psoriasis | [171] |
| Syk | R788 | Small molecule | Phase I clinical trial | RA | [210] |
| Inhibitors targeting terminal proinflammatory cytokines | |||||
| TNF | Adalimumab | Monoclonal antibody | Clinical medicine | RA | [6, 202] |
| TNF | Certolizumab pegol | F(ab’) fragment of a humanized monoclonal antibody | Clinical medicine | RA | [6] |
| TNF | Etanercept | p75 (of TNFRII)-Fc (of IgG1) fusion protein | Clinical medicine | RA | [6, 202] |
| TNF | Golimumab | Monoclonal antibody | Clinical medicine | RA | [6] |
| TNF | Infliximab | Monoclonal antibody | Clinical medicine | RA | [6, 202] |
| IL-6R | Tocilizumab | Monoclonal antibody | Clinical medicine | RA | [197] |
| IL-6 | Sarilumab | Monoclonal antibody | Phase III clinical trial | RA | [203] |
| IL-6 | ALX-0061 | Small molecule | Phase II clinical trial | RA | [203] |
| IL-6 | Sirukumab | Monoclonal antibody | Phase II clinical trial | RA | [211] |
| IL-6 | MEDI5117 | Monoclonal antibody | Phase I clinical trial | RA | [212] |
| IL-6 | Clazakizumab | Monoclonal antibody | Phase II clinical trial | RA | [213] |
| IL-6 | Olokizumad | Monoclonal antibody | Phase II clinical trial | RA | [214] |
| IL-1 | Anakinra | Recombinant | Clinical medicine | RA | [198] |
| IL-1 | Rilonacept | Soluble decoy receptor | Clinical medicine | RA | [198] |
| IL-1 | Canakinumab | Monoclonal antibody | Clinical medicine | RA | [198] |
| IFN-α | Sifalimumab | Monoclonal antibody | Phase II clinical trial | SLE | [215] |
| IFNAR | Anifrolumab | Monoclonal antibody | Phase III clinical trial | SLE | [216] |
| IFN-α | Rontalizumab | Monoclonal antibody | Phase II clinical trial | SLE | [204] |
| IL-18 | Tadekinig alfa | Recombinant | Phase III clinical trial | NLRC4 and XIAP deficiency | [205] |