TABLE 1

Ki values obtained with four substrate probes, (S)-mephenytoin, (S)-omeprazole, (R)-omeprazole, and (S)-fluoxetine, using CYP2C19 Global S.E. for data fitting was <15% and r2 > 0.9 for each effector.

(S)-Mephenytoin
(S)-Omeprazole
(R)-Omeprazole
(S)-Fluoxetine
μM
Loratadine 0.006 0.035 0.022 0.025
Fluvoxamine 0.013 0.062 0.014 0.070
Ticlopidinea 0.020 0.115 0.061 0.067
(S)-(+)-(N)-(3)-Benzylnirvanol 0.027 0.156 0.225 0.046
Clotrimazole 0.055 0.172 0.736 0.080
(R)-Fluoxetinea 0.067 0.631 0.627 0.347
Sertraline 0.089 1.54 0.371 0.375
Oxybutynin 0.209 0.601 0.328 0.536
Ketoconazole 0.239 0.183 0.447 4.32
Raloxifene 0.266 0.795 0.289 0.167
Ethynylestradiol 0.289 1.54 2.14 3.20
Progesterone 0.376 0.995 2.07 29.1
(R)-Omeprazole 0.445 NA NA 2.99
Estradiol 0.524 2.03 3.93 7.82
(S)-Omeprazole 0.538 NA NA 2.59
Nifedipine 0.553 1.63 2.1 3.32
(S)-Fluoxetinea 0.813 9.69 3.93 NA
Amitriptyline 3.38 1.07 5.81 13.8
Ketoprofen 4.15 >100 >100 >100
Suprofen 5.52 35.1 >100 60.4
Docetaxel 12.28 47.9 >100 >100
Sulfaphenazole 43.7 >100 >100 >100
Verapamil 43.8 100 79.7 8.35
(S)-Mephenytoin
NA
29.9
15.27
>100

  • ↵ a Time-dependent inactivator of CYP2C19