Imiquimod: In Vivo and In Vitro Characteristics and Toxicology

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Abstract
Mice Imiquimod (R-837, S-26308) (Figure 1) is a potent inducer of cytokines in a number of species including mice, rats, guinea pigs, monkeys, and humans (1-7). In mice, studies have demonstrated induction of interferon (IFN) in the serum as early as 1 hour after treatment. Concentrations of IFN generally peak 2 hours after dosing and at doses lower than 30 mg/kg return to background by 4 to 6 hours after administration. At doses higher than 30 mg/kg, peak concentrations of IFN are not any higher than those seen at the 30 mg/kg dose; however, IFN concentrations remain elevated for an extended time. Imiquimod not only induces IFN but also causes increases in tumor necrosis factor (TNF)-a and interleukin (IL)-6.

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