Table 1.
Potent agonists.
| Ligands | Chemical family | Agonist | Biological evaluations | References |
|---|---|---|---|---|
| S28690 | Imidazoquinoline derivative | TLR7 | Immunogeneicity effect on chronic lymphocytic leukemia | [[263], [264], [265], [266]] |
| SB 9922 | Nucleic acid hybrid | TLR7 | Potent vaccine adjuvant used in combination with BCG vaccine against Mycobacterium tuberculosis | [267,268] |
| RO6870868 and RO6864018 (ANA773 or RG7795) | Tosylate prodrug of isatoribine | TLR7 | Treatment for hepatitis C and cancers | [[269], [270], [271]] |
| RO7020531 | TLRs 7/8 | Cure chronic HBV infection | [272] | |
| AZD8848 (DSP-3025) | – | TLR7 | Long-term remission in allergic disorders such as bronchial asthma and allergic rhinitis | [273] |
| DSP-0509 | TLR7 | Potent immunostimulatory and antineoplastic activities | [274,275] | |
| BNT411 | – | TLR7 | Combination with chemotherapy and checkpoint inhibitors in preclinical development | [276] |
| JNJ-4964 (AL-034 or TQ-A3334) | – | TLR7 | Clinical development for the treatment of chronic hepatitis B (CHB) | [[277], [278], [279], [280]] |
| NKTR-262 | TLRs 7/8 | Induction of antigen-specific immunity and tumor regression effects | [281,282] |