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. 2017 Mar 23;2(6):e91020. doi: 10.1172/jci.insight.91020

Figure 1. Unlike R848, the lipidated, locally acting TLR7/8 agonist 3M-052 demonstrates low serum distribution and little systemic cytokine induction.

Figure 1

(A) The structure of R848 (resiquimod) and 3M-052, a TLR7/8 activating imidazoquinoline bearing a C18 lipid moiety and designed for slow dissemination from the site of injection. (B and C) Rodent pharmacokinetic and pharmacodynamic studies. Serum drug levels were measured by LC-MS/MS at the indicated times before or after dose in rats following a single i.m. (into quadriceps) or s.c. (into scruff of neck) administration of 3M-052 or R848 formulated in oil-in-water (O/W) emulsion (vehicle). The results represent median serum drug levels and induced TNF at each time point for each dose (n = 5). (D) Evaluation of s.c. mouse serum cytokine kinetics after a single dose of 3M-052 or R848 (both 1 mg/kg, 20 μg/mouse) formulated in O/W emulsion (vehicle) (n = 3).