Table 1.
TLR7 and 8 agonists in clinical trials
| Agonist | Targeted TLR | NCT# | Phase | Application | Sponsor | Mechanism | Status | Enrollment |
|---|---|---|---|---|---|---|---|---|
| 852A | TLR7 | NCT00319748 | II | Breast, ovarian, endometrial and cervical cancers | Masonic Cancer Center, University of Minnesota | Anti-tumor | Completed | 15 |
| BNT411 | TLR7 | NCT04101357 | I | Solid tumors, ES-SCLC | BioNTech Small Molecules GmbH | Anti-tumor | Recruiting | 60 |
| DN1508052 | TLR8 | NCT03934359 | Ib/II | Advanced Solid Tumors | Shanghai De Novo Pharmatech Co., Ltd. | Anti-tumor | Unknown | 25 |
| DSP-0509 | TLR7 | NCT03416335 | I/II | Advanced solid tumors | Sumitomo Pharma Oncology, Inc. | Anti-tumor | Recruiting | 100 |
| Immiquimod | TLR7 | NCT00899574 | II | Breast cancer | NYU Langone Health | Anti-tumor | Completed | 10 |
| Immiquimod | TLR7 | NCT01421017 | I/II | Breast cancer | NYU Langone Health | Anti-tumor | Completed | 31 |
| Immiquimod | TLR7 | NCT04116320 | I | Advanced solid tumors | Craig L Slingluff, Jr | Anti-tumor | Recruiting | 32 |
| MEDI9197 (3 M-052) | TLR7/8 | NCT02556463 | I | Solid tumors or CTCL | MedImmune LLC | Anti-tumor | Terminated | 53 |
| TLR agonist PolyICLC | TLR7/8 | NCT02643303 | I/II | Advanced solid tumors | MedImmune LLC | Anti-tumor | Completed | 58 |
| VTX-2337 | TLR8 | NCT01289210 | I, II | Low-grade B-cell lymphomas | Celgene | Anti-tumor | Terminated | 2 |
| VTX-2337 | TLR8 | NCT01294293 | I | Ovarian epithelial, fallopian tube, or peritoneal cavity cancer | Celgene | Anti-tumor | Completed | 20 |
| VTX-2337 | TLR8 | NCT01334177 | I | Squamous Cell Carcinomas of the Head and Neck (SCCHN) | Celgene | Anti-tumor | Completed | 13 |
| VTX-2337 | TLR8 | NCT01666444 | II | Epithelial ovarian, fallopian tube or primary peritoneal cancer | Celgene | Anti-tumor | Completed | 297 |
| VTX-2337 | TLR8 | NCT01836029 | II | Squamous cell carcinoma of the head and neck | Celgene | Anti-tumor | Completed | 195 |
| VTX-2337 | TLR8 | NCT02431559 | I,II | Ovarian cancer | Celgene | Anti-tumor | Completed | 53 |
| VTX-2337 | TLR8 | NCT02650635 | Ib | Advanced solid tumors | Celgene | Anti-tumor | terminated | 4 |
| VTX-2337 | TLR8 | NCT03906526 | Ib | Head and neck cancer | Celgene | Anti-tumor | Completed | 15 |
| GS-9620 | TLR7 | NCT02166047 | II | Chronic hepatitis B virus in virally suppressed subjects | Gilead Sciences | Antiviral treatment | Completed | 162 |
| GS-9688 | TLR8 | NCT03491553 | II | Virally suppressed adults with chronic hepatitis B | Gilead Sciences | Antiviral treatment | Completed | 48 |
| GS-9688 | TLR8 | NCT03615066 | II | Naive CHB patients | Gilead Sciences | Antiviral treatment | Completed | 67 |
| imiquimod | TLR7 | NCT00453050 | I | Melanoma | 3 M | Enhancing vaccination | Completed | 11 |
| PolyICLC | TLR7/8 | NCT04364230 | I/II | Melanoma | Celldex Therapeutics | Enhancing vaccination | Recruiting | 44 |
| Resiquimod | TLR7/8 | NCT02126579 | I/II | Melanoma vaccination | Mologen AG | Enhancing vaccination | Active, not recruiting | 62 |
| Resiquimod | TLR7/8 | NCT00960752 | II | Melanoma | Mologen AG | Enhancing vaccination | Completed | 47 |
| Resiquimod | TLR7/8 | NCT02126579 | I/II | Melanoma vaccination | Mologen AG | Enhancing vaccination | Active, not recruiting | 62 |
| TLR agonist PolyICLC | TLR7/8 | NCT01585350 | I | Melanoma vaccination | Oncovir, Inc. | Enhancing vaccination | Completed | 52 |