c.421C>A polymorphism affects only intestinal BCRP (assumption 1) |
CLint,bile,cc (Liters/h) | 15.4 | 18.3 | 26.6 | 39.9 ± 28.2 | 36.4 ± 31.6 | 22.4 ± 31.8 |
PBCRP,cc (10−5 cm/s) | 4.73 | 4.72 | 4.72 | 14.2 ± 2.2 | 14.2 ± 2.2 | 14.2 ± 2.4 |
Fraction of BCRP activityc | fca | 0.753 | 0.755 | 0.759 | 0.749 ± 0.088 | 0.752 ± 0.088 | 0.754 ± 0.087 |
faa | 0.174 | 0.181 | 0.194 | 0.373 ± 0.051 | 0.376 ± 0.051 | 0.377 ± 0.054 |
Fraction of absorbedd | FaFg,cc | 0.413 | 0.414 | 0.414 | 0.209 ± 0.024e | 0.209 ± 0.024e | 0.209 ± 0.026e |
FaFg,ca | 0.468 | 0.468 | 0.467 | 0.257 ± 0.034e | 0.257 ± 0.034e | 0.256 ± 0.036e |
FaFg,aa | 0.673 | 0.670 | 0.664 | 0.391 ± 0.041e | 0.389 ± 0.041e | 0.388 ± 0.044e |
c.421C>A polymorphism affects only hepatic BCRP (assumption 2) |
CLint,bile,cc (Liters/h) | 16.4 | 19.7 | 29.0 | 42.5 ± 17.7 | 51.0 ± 24.8 | 75.1 ± 45.3 |
PBCRP,cc (10−5 cm/s) | 4.37 | 4.37 | 4.37 | 9.10 ± 1.33 | 9.44 ± 1.26 | 10.2 ± 1.2 |
Fraction of BCRP activityc | fca | 0.797 | 0.773 | 0.715 | 0.751 ± 0.094 | 0.713 ± 0.096 | 0.624 ± 0.100 |
faa | 0.286 | 0.259 | 0.208 | 0.284 ± 0.048 | 0.250 ± 0.042 | 0.186 ± 0.033 |
Fraction of absorbedd | FaFg,cc | 0.429 | 0.429 | 0.429 | 0.286 ± 0.027e | 0.279 ± 0.025e | 0.265 ± 0.021e |
FaFg,ca | 0.429 | 0.429 | 0.429 | 0.286 ± 0.027e | 0.279 ± 0.025e | 0.265 ± 0.021e |
FaFg,aa | 0.429 | 0.429 | 0.429 | 0.286 ± 0.027e | 0.279 ± 0.025e | 0.265 ± 0.021e |
c.421C>A polymorphism affects both of intestinal and hepatic BCRP (assumption 3) |
CLint,bile,cc (Liters/h) | 16.0 | 19.0 | 27.6 | 41.4 ± 18.8 | 39.2 ± 21.0 | 25.7 ± 21.5 |
PBCRP,cc (10−5 cm/s) | 4.55 | 4.55 | 4.54 | 12.2 ± 1.5 | 12.5 ± 1.5 | 13.0 ± 1.7 |
Fraction of BCRP activityc | fca | 0.882 | 0.875 | 0.860 | 0.848 ± 0.050 | 0.839 ± 0.051 | 0.818 ± 0.055 |
faa | 0.529 | 0.513 | 0.479 | 0.539 ± 0.036 | 0.522 ± 0.036 | 0.478 ± 0.041 |
Fraction of absorbedd | FaFg,cc | 0.421 | 0.421 | 0.421 | 0.234 ± 0.021e | 0.230 ± 0.020e | 0.223 ± 0.021e |
FaFg,ca | 0.446 | 0.447 | 0.451 | 0.262 ± 0.025e | 0.260 ± 0.024e | 0.257 ± 0.026e |
FaFg,aa | 0.539 | 0.544 | 0.555 | 0.348 ± 0.028e | 0.350 ± 0.028e | 0.358 ± 0.031e |