TABLE 3

Predicted change in AUCI/AUC for compounds exhibiting Ki < 1 μM for (S)-mephenytoin


Inhibitor

Predicted AUCI/AUC

Actual DDIa
(S)-Mephenytoin
(S)-Omeprazole
(R)-Omeprazole
Loratadine 1.8 1.2 1.2
Fluvoxamine 13.8 5.3 6.6 5.6b
Ticlopidinec 9.4 3.1 3.7 2.4d
Clotrimazole 1.0 1.0 1.0
(R)-Fluoxetinec 3.8 1.3 1.3
Sertraline 1.9 1.1 1.2
Oxybutynin 1.1 1.0 1.1
Ketoconazole 1.3 1.2 1.1
Raloxifene 1.4 1.2 1.3
Ethynylestradiol 1.0 1.0 1.0
(R)-Omeprazole 1.1 1.0 1.0
(S)-Omeprazole 1.4 1.1 1.1
Nifedipine 1.1 1.0 1.0
(S)-Fluoxetinec
1.3
1.0
1.1

  • a Omeprazole used as the in vivo substrate probe

  • b From Yasui-Furukori et al. (2004)

  • c Time-dependent inactivator of CYP2C19

  • d From Tateishi et al. (1999)