Table 1 Therapeutic applications of TLR agonists and antagonists
From: Phytochemicals targeting Toll-like receptors 4 (TLR4) in inflammatory bowel disease
Class | Drug | Explanation | References |
|---|---|---|---|
TLR2 agonist | SMP-105 | It has been approved for the treatment of bladder cancer | [36] |
TLR3 agonist | Poly-IC12U | It is used in combination with vaccines for the treatment of ovarian, breast, colorectal, and brain tumors | [37] |
TLR4 antagonist | TAK-242 | It could enhance the sensitivity of cancer cells to doxorubicin and cisplatin, respectively | [38] |
TLR4 agonist | MPLA | MPLA (monophosphoryl lipid A) is the only TLR4 agonist to be approved by the FDA for the use as a vaccine adjuvant in humans (Cervarix®, Fendrix®) | |
TLR2/4 agonist | BCG | BCG (bacillus Calmette–Guerin) has been approved by the FDA for intravesical treatment of bladder carcinoma in situ and superficial bladder cancers | [41] |
TLR7 agonist | Imiquimod | Imiquimod is an FDA approved immune response modifier for the topical treatment of genital warts caused by HPV and has also been proposed as a therapeutic adjunct for COVID-19 and related infections | |
TLR9 antagonist | IROs | IROs (immunoregulatory oligonucleotides) can be used to suppress autoimmune and inflammatory diseases | [44] |