| In Vitro | In vitro activity: Imiquimod is an immune response modifier that acts as an agonist of the TLR7 (toll-like receptor 7). Imiquimod is a prescription medication that is used to treat genital warts, superficial basal cell carcinoma, and actinic keratosis. Scientists at 3M's pharmaceuticals division discovered the drug and 3M obtained the first FDA approval in 1997 under the brand name of Aldara. As of 2015, imiquimod is generic and is available worldwide under many brands. Imiquimod signals to the innate arm of the immune system through the TLR7, commonly involved in pathogen recognition. Cells activated by imiquimod via TLR-7 secrete cytokines such as interferon-α (INF-α), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α). Imiquimod has been studied in combination with pembrolizumab for treating stage IIIB-IV melanoma. |
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| In Vivo | Imiquimod stimulates the innate immune response by increasing NK cell activity, activating macrophages to secrete cytokines and nitric oxide, and inducing proliferation and differentiation of B lymphocytes in animal models. Imiquimod stimulates the innate immune response through induction, synthesis, and release of cytokines, including interferon-a (IFN-α), interleukin (IL)-6, and tumour necrosis factor (TNF)-α |
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| Animal model | Tissue ELISA revealed that imiquimod specifically reduced IL-1β and IL-6
secretion in the treated mouse paws (Panels F-G), whereas neutrophil
infiltration (visualized by MPO quantification, Panel H) and TNF-α
production (panel I) remained unaffected. RTqPCR and western blot
analysis further documented the negative effect of imiquimod on the
transcription of the Il-1β and Il-6 genes (Panels J-K) and IL-1β
pro-form expression (Panel L). |
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| Formulation & Dosage |
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| References | Actas Dermosifiliogr. 2018 May 23. pii: S0001-7310(18)30177-7; Br J Dermatol. 2003 Nov;149 Suppl 66:5-8.; Theranostics. 2020; 10(5): 2158–2171. |
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