Article Figures & Data
Figures
- Fig. 1.
In vitro consumption of EPA (5 μM) by individual recombinant human UGTs (0.5 mg/ml) over 1 hour.
- Fig. 2.
Formation of M11 from EPA (10 μM) and benzamidine from benzamidoxime (10 μM) by human liver mitochondria, microsomes, homogenate, S9 fraction and cytosol (2 mg/ml protein) over 30 minutes. Incubations were conducted in potassium phosphate buffer (pH 6.0) with NADH (2 mM).
- Fig. 3.
Representative extracted ion chromatograms showing ex vivo formation of M11 from EPA in human feces homogenate (a) and decrease in M11 formation from EPA in human feces homogenate by commonly prescribed antibiotics (b).
- Fig. 4.
Formation of M12 from M11 (10 μM) by human tissue microsomes (2 mg/ml protein) and S9 fractions (3 mg/ml protein) and recombinant cytochrome P450s (0.3 nmol/ml).
- Fig. 5.
Proposed major metabolic pathways of EPA in humans.
Tables
- TABLE 1
Area under the curve (AUC0–12h) ratios of major EPA metabolites relative to EPA in humans following a single oral dose and at steady state.
Dose Day EPA M9 M11 M12 50 mg BID 1 1 8.2 NC NC 10 1 8.1 0.3 0.8 NC, Not calculable because most plasma concentrations were below the lower limit of quantitation.
- TABLE 2
In vivo formation of M11 and M12 in mice given EPA with and without antibiotic or ABT pretreatment.
Dose Group AUC0-6h Ratio Relative to EPA EPA M11 M12 Control 1.000 0.260 0.107 Ciprofloxacin pretreatment 1.000 0.119 0.044 ABT pretreatment 1.000 0.372 0.017 AUC0-6h ratio relative to M11 Control 1.000 0.411 Ciprofloxacin pretreatment 1.000 0.372 ABT pretreatment 1.000 0.045
In this issue
Metabolism of Epacadostat in Humans
