Table 3

Correlation between rates of saquinavir metabolite formation in human small-intestinal microsomes

Correlation (r2)*
M-1M-2M-3M-4M-5M-6M-7
M-1 0.880.780.880.800.700.85
M-2 0.900.990.970.910.99
M-3 0.870.880.920.86
M-4 0.980.860.96
M-5 0.890.94
M-6 0.91
  • The rates of saquinavir metabolite formation were assessed with small-intestinal microsomes from 17 individual donors. Human small-intestinal microsomes were diluted with reaction buffer to give a final protein concentration of ∼0.05 mg/ml. Microsomes were warmed at 37°C in the presence of a NADPH-generating system for 3 min, and reactions were initiated by the addition of 10 μl of a 0.5 mM saquinavir solution in 1:1 acetonitrile:water to 0.99 ml reaction mixture. Reactions were terminated after 15 min by the addition of 1 ml of acetonitrile.

  • * Correlations between saquinavir metabolites were statistically significant, p < 0.001.