Variability in the formation of paclitaxel metabolites Oxidation of paclitaxel was investigated in liver microsomes or in cDNA-expressed CYP3A4. Data are means ± S.D. (n = 3). Boldface indicates that this was the main metabolite described in this study.
Species | Paclitaxel Metabolites | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| di-OHP | C3′-OHP | C2-OHP | 6α-OHP | Unknown OHP | |||||
| pmol/min/mg microsomal protein | |||||||||
| Untreated rat | 1.0 ± 0.5 | 3.16 ± 1.5 | 0.5 ± 0.2 | * | 1.0 ± 0.2 | ||||
| Rat (PCN-induced) | 1.9 ± 0.1 | 81.5 ± 2.7 | 18.5 ± 0.3 | * | 14.4 ± 0.8 | ||||
| Minipig | * | 0.4 ± 0.2 | 0.3 ± 0.1 | * | 13.8 ± 2.5 | ||||
| Regular pig (females) | * | 0.3 ± 0.0 | * | * | 5.8 ± 0.1 | ||||
| Regular pig (males) | * | 0.5 ± 0.1 | * | * | 5.9 ± 1.2 | ||||
| Human | * | 15.0 ± 4.5 | 1.5 ± 0.9 | 81.8 ± 21.2 | * | ||||
| CYP3A4 |
*
|
1.38 ± 0.2
a
| 0.15 ± 0.1a |
*
|
*
| ||||