Fig. 1
From: Pharmacokinetics of ivermectin metabolites and their activity against Anopheles stephensi mosquitoes
Ivermectin metabolism. Chemical structure of ivermectin and putative structure of the metabolites (M1–M9): M1: Desmethyl-H2B1a, M2: Hydroxy-H2B1a, M3: Hydroxy-H2B1a, M4: Desmethyl, hydroxy-H2B1a, M5: Hydroxy-H2B1a monosaccharide, M6: Desmethyl, hydroxy-H2B1a, M7: Hydroxy-H2B1a monosaccharide, M8: Dihydroxy-H2B1a, M9: Hydroxy-H2B1a. Ivermectin (10 µM) was incubated for 60 min in the presence of CYP3A4 (blue) or CYP3A5 (red) enzymes (supersomes). Incubations were performed in the presence (empty circle) or absence (filled circle) of ketoconazole (1 µM), a potent 3A inhibitor. Formation of the ivermectin metabolites is shown as mean peak area ratio (analyte peak area: ivermectin-d2 area). The error bars correspond to the standard error of the mean. A representative chromatogram recorded 60 min post-incubation is depict for each metabolite transition. Ivermectin-d2 (IVM-d2) was added as point of comparison into each chromatogram