Table 1.
Compounds in development that target human nucleic acid-sensing TLRs for autoimmunity.
| Compound | Drug class | Target | Indications | Company | Status/Trial ID | Reference |
|---|---|---|---|---|---|---|
| CQ/HCG | Small molecule/Inhibitor | TLR7, TLR8 and TLR9 | SLE, RA | Generic | Clinical use | (140) |
| SS | Phase III NCT016001028 NCT00632866 |
(141) | ||||
| M5049 (Enpatoran) | Small molecule/Inhibitor | TLR7 and TLR8 | SLE | Merck | Animal study | (142) |
| SLE | Phase I NCT03676322 |
(143) | ||||
| SLE, CLE | Phase I NCT04647708 | |||||
| SLE, CLE, SCLE, DLE | Phase II NCT05162586 |
|||||
| COVID-19 pneumonia | Phase II NCT04448756 | |||||
| IRS-954 | Oligonucleotide | TLR7 and TLR9 | SLE | – | Animal study | (144, 145) |
| IMO-3100 | IMO | TLR7 and TLR9 | psoriasis | Idera Pharmaceuticals | Phase II NCT01622348 | |
| IMO-8400 | IMO | TLR7, TLR8 and TLR9 | SLE, psoriasis | Idera Pharmaceuticals | Animal study | (146–148) |
| psoriasis | Phase IIa NCT01899729 |
(149) | ||||
| cancer | Preclinical, Animal study | (150) | ||||
| B cell lymphoma | Phase I/II NCT02363439 NCT02252146 |
|||||
| BMS-986256 (Afimetoran) | Small molecule | TLR7 and TLR8 | SLE | Bristol-Myers Squibb | Phase I/II NCT04895696 |
(151, 152) |
| DS-7011a | Antibody | TLR7 | SLE | Daiichi Sankyo | Phase I NCT05203692 |
CLE, cutaneous lupus erythematosus; CQ, chloroquine; DLE, discoid lupus erythematosus; HCQ, hydroxychloroquine; IMO, Immune modulatory oligonucleotide; SCLE, subacute cutaneous lupus erythematosus; SLE, systemic lupus erythematosus.