Table 1 The characteristics and clinical applications of inhibitors targeting innate immune sensors in autoimmune diseases

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]