TABLE 5

Variability in the formation of docetaxel metabolites by liver microsomes from different species Docetaxel concentration was 10 μM. Results are means ± S.D. of at least two determinations from 30-min incubations. In PCN microsomes, 10-min incubations that already metabolized docetaxel completely were used. Values are the rates of formation of docetaxel metabolites in different liver microsomes.


Species

Hydroxydocetaxel

Hydroxyoxazolidinone `A'

Hydroxyoxazolidinone `B'
pmol of metabolite/min/mg protein
Untreated rat 32 ± 1 0.9 ± 0.02 *
Rat (PCN induced) * 213.3 ± 8.2 258.7 ± 13.6
Minipig 21 ± 4 * *
Regular pig (females) 10 * *
Regular pig (males) 12 ± 2 * *
Human sample H6
3.5 ± 1.5
0.7 ± 0.6
0.7 ± 0.1
  • * , metabolite was not detected