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IC50: Imiquimod activates toll-like receptor 7 (EC50 2.1 μM) on immune cells and also enables an OGF-mediated block of cell proliferation (IC50 2 μM) [1].

Toll-like receptor 7, also known as TLR7, is protein that in humans is encoded by the TLR7 gene. It is a member of the toll-like receptor (TLR) family. The TLR family plays an important role in pathogen recognition and activation of innate immunity. Imiquimod is a prescription medication that acts as an immune response modifier activating toll-like receptor 7. It is marketed by Meda AB, Graceway Pharmaceuticals, and iNova Pharmaceuticals under the trade names Aldara and Zyclara, and by Farmacoquímica Médica (FQM) in Brazil as Ixium.

In vitro: Results from a previous study demonstrate that imiquimod were capable of inducing interleukin-12 and interferon-g in mouse and human cell cultures. Imiquimod was also found to inhibit IL-4 and IL-5 production in mouse and human culture systems. These data suggested that imiquimod might have clinical utility in diseases where cellmediated immune responseswere important and in diseases associated with overexpression of IL-4 or IL-5, such as atopic disease. [2].

In vivo: The findings from animal study suggested that imiquimod could inhibit the airway inflammation of asthma animals by reducing GATA-3 mRNA and protein expression and increasing T-bet, STAT(6) mRNA and protein expression [3]..
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