MKI | Dose | Fa | fu | Cmax,u(portal) | R[ka 0.03]a | R[ka 0.1] | R[ka 0.03] | R[ka 0.1] | |
---|---|---|---|---|---|---|---|---|---|
ka 0.03 | ka 0.1 | eq. 3 | eq. 3 | eq. 4 | eq. 4 | ||||
mg | µM | ||||||||
OATP1A2 | |||||||||
Cediranib | 30 | 1 | 0.03 | 0.037 | 0.130 | 2.23 | 5.43 | 2.12 | 4.94 |
Erlotinib | 150 | 0.60 | 0.07 | 0.620 | 1.32 | 1.56 | 2.20 | ||
OATP1B3 | |||||||||
Erlotinib | 1.52 | 2.11 | |||||||
OATP2B1 | |||||||||
Erlotinib | 21.7 | 45.0 | 16.1 | 33.2 | |||||
Gefitinib | 250 | 0.59 | 0.09 | 0.818 | 2.52 | 2.26 | 4.88 | ||
OAT3 | |||||||||
Nilotinib | 300 | 0.31 | 0.02 | 0.117 | 0.270 | 1.29 | 1.66 |
Fa, reported oral bioavailability of the MKI.
↵a rB = 1, except for gefitinib (0.76; Li et al., 2006).