Imiquimod (99011-02-6) is a Toll-like receptor 7/8 agonist with anti-viral and anti-tumor properties.1 Enhances innate immune system leading to Th1-mediated antitumor immune response.2 Increases levels of IFNα, TNFα, and IL-12. Imiquimod has also been shown to act as an antagonist at adenosine A1 and A2A receptors augmenting its proinflammatory effects.3,4 Clinically useful for the treatment of basal cell carcinoma, actinic keratosis, and genital warts. Imiquimod also upregulates the expression of opioid growth factor receptor(OGFr).5,6 OGF is involved in regulation of inhibitory kinases in the cell cycle process.
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2) Stanley et al. (2002), Imiquimod and the imidazoquinolones: mechanism of action and therapeutic potential; Clin. Exp. Dermatol. 27 571
3) Schoen et al. (2006), The small antitumoral immune response modifier imiquimod interacts with adenosine receptor signaling in a TLR7- and TLR8-independent fashion; J.Invest.Dermatol. 126 1338
4) Kan et al. (2012), Imiquimod Suppresses Propagation of Herpes Simplex Virus 1 by Upregulation of Cystatin A via the Adenosine Receptor A1 Pathway.; J. Virol. 86 10338
5) Urosevic et al. (2004), Imiquimod Treatment Induces Expression of Opioid Growth Factor Receptor; Clin. Cancer Res. 10 4959
6) Zagon et al. (2008), Imiquimod Upregulates the Opioid Growth Factor Receptor to Inhibit Cell Proliferation Independent of Immune Function.; Exp. Biol. Med.(Maywood) 233 968