3M-011 is a potent dual toll-like receptor TLR7/8 agonist and a cytokine inducer.
Firstly, in B16-F10 melanoma cells, 3M-011 treatment can decrease B16-F10 melanoma cell counts as a dose-dependent manner. 3M-011 potentiates natural killer (NK) cells cytotoxicity.
The NF-κB reporter stably expresses in HEK-293 cells Then the cells subsequently transiently transfected with human or mouse TLR7 or TLR8. 3M-011 results in a dose-dependent induction of NF-κB-controlled luciferase activity. 3M-011 in humans activates both TLR7 and TLR8, whereas, in mice, 3M-011 activates only TLR7 and not TLR8.
In vivo, in Female SCID/NOD mice with B16-F10 cells. 3M-011 treatment shows antitumor effects in SCID/NOD mice by intravenous injection. In Wild-type C57BL/6 mice, 3M-011 at different doses induce a dose-dependent increase in serum concentrations of both TNF-α and IFN-α/β. Which possesses strongly has antitumor action. Innate immune stimulation with TLR agonists is a proposed modality for immunotherapy of melanoma.
3M-011 is a potent adjuvant to radiotherapy that induces local and profound systemic immune responses during radiotherapy.
Toll-like receptors (TLR) can detect pathogens-expressing molecular patterns. 3M-011 can be a cytokine inducer. In a rat model of human influenza. It is a stand-alone immune response modifier. 3M-011 can significantly inhibit H3N2 influenza viral replication in the nasal cavity after an intranasal (IN) administration.
the ability of the TLR7/8 agonist 3M-011 corrects with Viral inhibition, additionally, some cytokines such as tumor necrosis factor-alpha, interleukin-12, and IFN-gamma from rat peripheral blood mononuclear cells also play roles in vivo.
Prophylactic administration of 3M-011 suppresses. influenza viral titers in the lung. When compares to rat recombinant IFN-alpha administration as a high dose, the activity of 3M-011 leads to greater inhibition of viral titers.
In conclusion, 3M-011 significantly inhibits H3N2 influenza viral replication in the nasal cavity. It has the potential for the treatment of respiratory viral infections, such as influenza.
Dumitru CD, et al. Cancer Immunol Immunother. 2009 Apr;58(4):575-87.