The metabolic profile of azimilide in man: in vivo and in vitro evaluations.

@article{Riley2005TheMP,
  title={The metabolic profile of azimilide in man: in vivo and in vitro evaluations.},
  author={Pamela Riley and P C Figary and John Entwisle and Amy L. Roe and Gary A. Thompson and Rikiya Ohashi and Noriko Ohashi and Thomas John Moorehead},
  journal={Journal of pharmaceutical sciences},
  year={2005},
  volume={94 9},
  pages={
          2084-95
        }
}
The metabolic fate of azimilide in man is unusual as it undergoes a cleavage in vivo resulting in the formation of two classes of structurally distinct metabolites. During a metabolite profiling study conducted in human volunteers to assess the contribution of all pathways to the clearance of (14)C-azimilide, greater than 82% of radioactivity was recovered in urine (49%-58%) and feces (33%). Urine, feces, and plasma were profiled for metabolites. A cleaved metabolite, 4-chloro-2-phenyl furoic… 
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This analysis suggests that fm is the major determinant of total drug M/P ratio for amine, alcohol, N- and S-oxide, and carboxylic acid metabolites and arenol metabolites show a more complex relationship with fm due largely to the new metabolic routes available to the metabolite compared with the parent drug molecule.
Which Metabolites Circulate ? s
TLDR
This analysis suggests that fm is the major determinant of total drug M/P ratio for amine, alcohol, Nand S-oxide, and carboxylic acid metabolites and arenol metabolites show amore complex relationship with fm due largely to the new metabolic routes available to the metabolite compared with the parent drug molecule.
Minireview Which Metabolites Circulate? s
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This analysis suggests that fm is the major determinant of total drug M/P ratio for amine, alcohol, N- and S-oxide, and carboxylic acid metabolites and arenol metabolites show a more complex relationship with fm due largely to the new metabolic routes available to the metabolite compared with the parent drug molecule.
DMD050278 933..951
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This analysis suggests that fm is the major determinant of total drug M/P ratio for amine, alcohol, Nand S-oxide, and carboxylic acid metabolites and arenol metabolites show amore complex relationship with fm due largely to the new metabolic routes available to the metabolite compared with the parent drug molecule.
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Results indicate that azimilide does not inhibit CYP2C19‐mediated metabolism, which had the lowest in vitro IC50 values for the cytochrome P450s most commonly involved with the metabolism of drugs.
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This Part presents some of the numerous hydrolases involved, their nomenclature, relevant biochemical properties, catalytic mechanisms, and the many reactions of hydrolysis they catalyze.
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