Table 7.
TLR3/7/8/9 targeting ligands in clinical trials
| Ligand | Phase | Application | Target TLR adjuvant/drug | Sponsor/collaborators | NCT number | Type | Purpose/mechanism |
|---|---|---|---|---|---|---|---|
| Resiquimod, poly‐ICLC | Phase 2 | Glioma, anaplastic astrocytoma, anaplastic astro‐oligodendroglioma | TLR3/7/8 agonist/adjuvant | Jonsson Comprehensive Cancer Center | NCT01204684 | SM, synthetic dsRNA | Antitumor and antiviral immune stimulation |
| Poly‐ICLC, resiquimod (R848) | Phases 1 and 2 | Melanoma and its metastatic mucosal variants | TLR3/7/8 agonist/adjuvant | Craig L Slingluff, Jr, University of Virginia | NCT02126579 | SM, synthetic dsRNA | Antitumor immune stimulation |
| Resiquimod (R848) | Phase 1 | Influenza vaccination in seniors | TLR7/8 agonist/adjuvant | University of British Columbia | NCT01737580 | SM | Immune stimulation |
| MEDI9197 (durvalumab) | Phase 1 | Solid tumors, cutaneous T cell lymphoma | TLR7/8 agonist/adjuvant | MedImmune LLC | NCT02556463 | SM | Improving antigen presentation |
| Resiquimod (NY‐ESO‐1) | Phase 1 | Tumors | TLR7/8 agonist/adjuvant | Nina Bhardwaj, CRI New York City, Icahn School of Medicine at Mount Sinai | NCT00821652 | SM | Immune stimulation |
| IMO‐8400 | Phases 1 and 2 | Waldenstrom's macroglobulinemia | TLR7/8/9 antagonist/adjuvant | Idera Pharmaceuticals, Inc | NCT02092909 | Oligonucleotide antagonist | Immune suppression, TLR7/8/9 signaling blocker |
| IMO‐8400 | Phase 2 | Plaque psoriasis | TLR7/8/9 antagonist/drug | Idera Pharmaceuticals, Inc | NCT01899729 | Oligonucleotide antagonist | Immune suppression |
| CPG‐52364 | Phase 1 | Healthy volunteers | TLR7/8/9 antagonist/drug | Pfizer | NCT00547014 | SM | Immune suppression |
| IMO‐8400 | Phases 1 and 2 | Diffuse large B cell lymphoma | TLR7/8/9/ antagonist/drug | Idera Pharmaceuticals, Inc | NCT02252146 | Oligonucleotide antagonist | Immune suppression |
Abbreviations: CRI, Cancer Research Institute; dsRNA, double‐stranded RNA; NA, not available; NCT, national clinical trial; SLE, systematic lupus erythematosus; SM, small molecule; TLR, Toll‐like receptor.