TABLE 4
Structures of [14C]muraglitazar metabolites
Drug or Metabolite | Proposed Structurea | Source |
|---|---|---|
| Muraglitazar |
| Rat: Plasma, urine, feces, bile |
| Dog: Plasma, urine, feces | ||
| Monkey: Plasma, urine, feces, bile | ||
| Human: Plasma, urine, feces, bile | ||
| M1 |
| Rat: Plasma, urine, feces |
| (O-Dealkyl muraglitazar) | Dog: Plasma, urine, feces | |
| Monkey: Plasma, urine, feces, bile | ||
| Human: Plasma, urine, feces | ||
| M2 |
| Rat: Plasma, urine, feces, bile |
| (8-Hydroxy-O-demethyl muraglitazar) | Dog: N.D. | |
| Monkey: Plasma, urine, feces, bile | ||
| Human: Plasma, urine, feces, bile | ||
| M3 |
| Rat: Urine |
| (8,12-Dihydroxy muraglitazar) | Dog: N.D. | |
| Monkey: Feces, bile | ||
| Human: Plasma, urine, feces | ||
| M4 |
| Rat: N.D. |
| (9,12-Dihydroxy muraglitazar) | Dog: Feces | |
| Monkey: Feces, bile | ||
| Human: Plasma, urine, feces | ||
| M5 |
| Rat: Plasma, urine, feces, bile |
| (12-Hydroxy-O-demethyl muraglitazar) | Dog: Plasma, urine, feces | |
| Monkey: Plasma, urine, feces, bile | ||
| Human: Plasma, urine, feces, bile | ||
| M6 |
| Rat: Plasma, urine |
| (17-Hydroxy-O-demethyl muraglitazar) | Dog: Plasma, urine, feces | |
| Monkey: Plasma, urine, feces, bile | ||
| Human: Plasma, urine, feces | ||
| M7 |
| Rat: Feces, bile |
| (9-Hydroxy-O-demethyl muraglitazar) | Dog: Feces | |
| Monkey: Feces, bile | ||
| Human: Feces, bile | ||
| M8 |
| Rat: Plasma, bile |
| (12,17-Dihydroxy muraglitazar) | Dog: Feces | |
| Monkey: Plasma, urine, feces, bile | ||
| Human: Plasma, feces, bile | ||
| M8a |
| Rat: Plasma, urine, feces, bile |
| (8-Hydroxy muraglitazar) | Dog: Feces | |
| Monkey: Plasma, urine, bile | ||
| Human: Plasma, urine, feces, bile | ||
| M9 |
| Rat: Plasma, feces |
| (Imide derivative of muraglitazar) | Dog: Feces | |
| Monkey: Feces, bile | ||
| Human: Feces | ||
| M10 |
| Rat: Plasma, urine, feces, bile |
| (12-Hydroxy muraglitazar) | Dog: Feces | |
| Monkey: Plasma, urine, feces, bile | ||
| Human: Plasma, urine, feces, bile | ||
| M11 |
| Rat: Plasma, urine, feces, bile |
| (17-Hydroxy muraglitazar) | Dog: Feces | |
| Monkey: Plasma, urine, feces, bile | ||
| Human: Plasma, urine, feces | ||
| M12 |
| Rat: Plasma, urine, bile |
| (Muraglitazar 12-carboxylic acid) | Dog: Feces | |
| Monkey: Plasma, urine, feces, bile | ||
| Human: Plasma, feces, bile | ||
| M13 |
| Rat: Plasma, urine, bile |
| (Muraglitazar glucuronide) | Dog: Plasma | |
| Monkey: Plasma, urine, feces, bile | ||
| Human: Plasma, urine, bile | ||
| M14 |
| Rat: Urine, feces, bile |
| (9-Hydroxy muraglitazar) | Dog: Feces | |
| Monkey: Urine, feces, bile | ||
| Human: Feces, bile | ||
| M15 |
| Rat: Plasma, urine, feces, bile |
| (O-Demethyl muraglitazar) | Dog: Plasma, urine, feces | |
| Monkey: Plasma, urine, feces, bile | ||
| Human: Plasma, feces, bile | ||
| M16 |
| Rat: Plasma, feces |
| (Acetylimide derivative of muraglitazar) | Dog: Feces | |
| Monkey: Feces | ||
| Human: Plasma, feces | ||
| M17a |
| Rat: Bile |
| (Hydroxy-O-demethyl muraglitazar glucuronide) | Dog: N.D. | |
| Monkey: bile | ||
| Human: Bile | ||
| M17b |
| Rat: Urine, bile |
| (Hydroxy-O-demethyl muraglitazar glucuronide) | Dog: N.D. | |
| Monkey: Urine, bile | ||
| Human: Urine, bile | ||
| M17c |
| Rat: Bile |
| (Hydroxy-O-demethyl muraglitazar glucuronide) | Dog: N.D. | |
| Monkey: Bile | ||
| Human: Bile | ||
| M18a |
| Rat: Plasma, bile |
| (Hydroxy muraglitazar glucuronide) | Dog: N.D. | |
| Monkey: Bile | ||
| Human: Bile | ||
| M18b |
| Rat: Plasma, urine, bile |
| (Hydroxy muraglitazar glucuronide) | Dog: N.D. | |
| Monkey: Plasma, urine, bile | ||
| Human: Plasma, bile | ||
| M18c |
| Rat: Bile |
| (Hydroxy muraglitazar glucuronide) | Dog: N.D. | |
| Monkey: Bile | ||
| Human: Bile | ||
| M20 |
| Rat: Plasma, urine, bile |
| (O-Demethyl muraglitazar glucuronide) | Dog: Plasma, urine | |
| Monkey: Plasma, urine, bile | ||
| Human: Bile | ||
| M21 |
| Rat: Urine, feces |
| (O-Dealkyl-O-demethyl muraglitazar) | Dog: Urine | |
| Monkey: Plasma, urine, feces, bile | ||
| Human: Urine, feces | ||
| M22 |
| |
| (Di-oxygenated muraglitazar) | In incubations of hepatoctes from mice, rats, monkeys, and humans and in the control incubation without hepatocytes | |
| M23 |
| |
| (5-Methyl-2-phenyloxazoyl 4-acetic acid) |
| In incubations of hepatocytes from mice and monkeys |
-
N.D., not detected.
-
↵ a Structures were proposed based on MS data and comparison with synthetic metabolites.