Quantification and identification of components in human urine and feces following intravenous administration of carbon 14-velsecorat
| % Matrix Content (% of dose) | |||
|---|---|---|---|
| Compound | Structure Modification | Urine | Feces |
| Velsecorat | Unchanged compound | ||
| M2 | O-dealkylation of the indazole ether | 30 (14.7) | |
| M1 | Sulfate conjugate of M2 | 84.9 (19.6) | 4.4 (2.2) |
| M22 | Glucuronide conjugate of M2 | 8.1 (1.9) | |
| M44 a | Ring deethylation of 1,4-benzodioxane | 25.4 (12.5) | |
| M46 a | Ring opening of 1,4-benzodioxane (diol) | ||
| M8 a | M46 + oxidation of 1 alcohol to acid | ||
| M23 a | M2 + hydrolysis of oxolane ring | 12.5 (6.2) | |
| M24 a | M23 + oxidation of 1 alcohol to acid | ||
| M32 a or M33 a | Hydrolysis of both the oxolane and 1,4-benzodioxane ring | 11.8 (5.8) | |
| M31 a | M32 + oxidation of 1 alcohol to acid in the opened 1,4-benzodioxane ring | ||
| M34 a | M32 + oxidation of 1 alcohol to acid in the hydrolyzed oxolane ring | ||
| M47 a | Hydrolysis of the oxolane ring | 3.2 (1.6) | |
| M9 a | M47 + oxidation of 1 alcohol to acid | ||
| M10 a | Monooxygenation of velsecorat | ||
| M11 a | Monooxygenation of velsecorat | ||
| M35 a | M47 + decarbonylation of the 1,4-benzodioxane ring | 2.8 (1.4) | |
Co-eluting peaks, percentages are presented as sum.
IV, intravenous
N = 5