TABLE 1.
TLR-based ligands in clinical trials.
| Name | TLR being targeted | Agonist/antagonist | Disease | Identifier number | Last updated | Status | Phase |
| Cancers | |||||||
| CBLB612 | TLR2 | Agonist | Breast cancer | NCT02778763 | July 20, 2016 | Completed | Phase 2 |
| Hespecta | TLR2 | Agonist | Head and neck cancer | NCT02821494 | February 21, 2021 | Completed | Phase 2 |
| Poly-ICLC | TLR3 | Agonist | Low grade lymphoma | NCT01976585 | November 19, 2020 | Recruiting | Phase1/2 |
| Poly-ICLC | TLR3 | Agonist | Advanced Cutaneous T Cell Lymphoma | NCT02061449 | December 24, 2018 | Terminated | Phase 1 |
| GLA-SE | TLR4 | Agonist | Melanoma | NCT02320305 | January 14, 2020 | Completed | Early phase 1 |
| GLA-SE | TLR4 | Agonist | Soft tissue sarcoma | NCT02180698 | November 6, 2019 | Completed | Phase 1 |
| GLA-SE | TLR4 | Agonist | Follicular Non-Hodgkin’s Lymphoma | NCT02501473 | September 9, 2020 | Terminated | Phase 1/2 |
| ONT-10 | TLR4 | Agonist | Ovarian or breast cancer | NCT02270372 | May 17, 2018 | Completed | Phase 1 |
| Mobilan | TLR5 | Agonist | Prostate Cancer | NCT02844699 | September 20, 2017 | Unknown | Phase 1/2 |
| Entolimod | TLR5 | Agonist | Metastatic solid tumors | NCT01527136 | January 12, 2016 | Completed | Phase 1 |
| Entolimod | TLR5 | Agonist | Squamous Cell Head and Neck Cancer | NCT01728480 | December 11, 2013 | Withdrawn | Phase 1 |
| Imiquimod | TLR7 | Agonist | Breast cancer | NCT01421017 | December 24, 2018 | Completed | Phase1/2 |
| Resiquimod | TLR7/8 | Agonist | Tumors | NCT00821652 | January 8, 2015 | Completed | Phase 1 |
| IMO-8400 | TLR7/8/9 | Antagonist | Diffuse Large B Cell Lymphoma | NCT02252146 | December 12, 2017 | Completed | Phase 1/2 |
| VTX-2337 | TLR8 | Agonist | Metastatic Squamous Cell Carcinoma of the Head and Neck | NCT01836029 | October 29, 2019 | Completed | Phase 2 |
| Eritoran (E5564) | TLR4 | Antagonist | Leukemia | NCT00756912 | July 11, 2014 | Terminated | Phase 1 |
| Viral infections | |||||||
| SD-101 | TLR9 | Agonist | HCV | NCT00823862 | April 16, 2019 | Completed | Phase 1 |
| Resiquimod | TLR7/8 | Agonist | Influenza | NCT01737580 | August 28, 2013 | Completed | Phase 1 |
| Lefitolimod | TLR9 | Agonist | HIV | NCT04357821 | November 17, 2020 | Recruiting | Phase1/2 |
| Vesatolimod | TLR7 | Agonist | CHB | NCT02166047 | October 14, 2020 | Completed | Phase 2 |
| GS-9620 | TLR9 | Agonist | HBV | NCT01590654 | December 20, 2013 | Completed | Phase 1 |
| CpG 1018 | TLR9 | Agonist | HIV | NCT04177355 | September 2, 2021 | Recruiting | Phase 1 |
| VAX125 | TLR5 | Agonist | Influenza | NCT00966238 | October 2, 2014 | Completed | Phase 2 |
| Poly-ICLC | TLR3 | Agonist | HIV | NCT02071095 | March 13, 2018 | Completed | Phase 1/2 |
| Poly-ICLC | TLR3 | Agonist | HIV | NCT01127464 | May 8, 2014 | Completed | Phase 1 |
| Imiquimod | TLR7 | Agonist | Influenza | NCT02103023 | December 5, 2014 | Completed | Phase 3 |
| Imiquimod | TLR7 | Agonist | HPV | NCT00941811 | June 16, 2015 | Completed | Phase 2 |
| Vesatolimod | TLR7 | Agonist | HBV | NCT02166047 | October 14, 2020 | Completed | Phase 2 |
| GS-9620 | TLR7 | Agonist | HBV | NCT01590654 | December 20, 2013 | Completed | Phase 1 |
| RO7020531 | TLR7 | Agonist | CHB | NCT02956850 | July 7, 2021 | Completed | Phase 1 |
| MGN1703 | TLR9 | Agonist | HIV | NCT02443935 | June 29, 2017 | Completed | Phase 1/2 |
| CpG 7909 | TLR9 | Agonist | HIV | NCT00562939 | January 21, 2009 | Completed | Phase 1/2 |
| IMO-2125 | TLR9 | Agonist | HCV | NCT00728936 | February 15, 2019 | Completed | Phase 1 |
| M5049 | TLR7/8 | Antagonist | SARS-CoV-2 | NCT04448756 | August 5, 2021 | Active, not recruiting | Phase 2 |
| Pul-042 | TLR2/6/9 | Agonist | SARS-CoV-2 | NCT04313023 | September 2, 2021 | Completed | Phase 2 |
| Autoimmune diseases and bacterial diseases | |||||||
| TAK-242 | TLR4 | Antagonist | Sepsis | NCT00143611 | February 2, 2012 | Completed | Phase 3 |
| TAK-242 | TLR4 | Antagonist | Sepsis | NCT00633477 | January 18, 2013 | Terminated | Phase 3 |
| TAK-242 | TLR4 | Antagonist | Alcoholic hepatitis | NCT04620148 | August 2, 2021 | Recruiting | Phase 2 |
| IMO-3100 | TLR7/9 | Antagonist | Psoriasis | NCT01622348 | January 9, 2018 | Completed | Phase 2 |
| IMO-8400 | TLR7/8/9 | Antagonist | Psoriasis | NCT01899729 | August 10, 2020 | Completed | Phase 2 |
| LPS | TLR4 | Agonist | Sepsis | NCT02554630 | February 2, 2021 | Recruiting | NA |
| Eritoran (E5564) | TLR4 | Antagonist | Sepsis | NCT00334828 | July 25, 2017 | Completed | Phase 3 |
| Eritoran (E5564) | TLR4 | Antagonist | Severe sepsis | NCT00046072 | December 12, 2005 | Completed | Phase 1 |
| Eritoran (E5564) | TLR4 | Antagonist | Obese and Type 2 Diabetic Subjects | NCT02267317 | March 4, 2020 | Terminated | Phase 2 |
| JKB-122 | TLR4 | Antagonist | Autoimmune hepatitis | NCT02556372 | July 21, 2020 | Completed | Phase 2 |
HCV, Hepatitis C Virus; HBV, Hepatitis B Virus; HPV, Human Papilloma Virus; HIV, Human Immunodeficiency Virus; CHB, Chronic Hepatitis B; NA, not available.