Compound | M01 | M02 | M11 | MT35 | MT38 | MT43 | HLMs |
---|---|---|---|---|---|---|---|
500 pmol/mla | 1 mg/mla | ||||||
Alprazolam | <5b | <5b | <5b | 10 | <5b | <5b | <5b |
Amitriptyline | 36 | 34 | 74 | 96 | 84 | 25 | 18 |
Aprepitant | 10 | <5b | 10 | <5b | 9 | 17 | 45 |
Aripiprazole | 99 | 99 | 99 | 93 | 99 | 99 | 93 |
Astemizole | 95 | 8 | 94 | 68 | <5b | 10 | 22 |
Buspirone | 46 | 75 | 83 | 67 | 9 | 29 | 17 |
Carbamazepine | <5b | <5b | <5c | 11 | <5b | 10 | <5b |
Carvedilol | 86 | 9 | 78 | 66 | 51 | 32 | 8 |
Cilostazol | <5b | 25 | 17 | 37 | 82 | 93 | 38 |
Cinacalcet | 96 | 89 | 97 | 87 | 67 | 96 | 46 |
Citalopram | 29 | 7 | 56 | 78 | 27 | 10 | <5b |
Dextromethorphan | 68 | 23 | 95 | 97 | 80 | 50 | 27 |
Diclofenac | 18 | <5b | 13 | 50 | <5b | 7 | 45 |
Diltiazem | 6 | <5b | <5b | 55 | 11 | 10 | 28 |
Duloxetine | 18 | <5b | 39 | 51 | 53 | 20 | <5b |
Glipizide | <5b | <5b | 7 | 35 | <5b | 9 | 44 |
Imatinib | 51 | 80 | 77 | 30 | 13 | <5b | <5b |
Indomethacin | <5c | <5c | <5c | <5c | <5c | <5c | <5b |
Irbesartan | 12 | <5b | 7 | 80 | 23 | 6 | <5b |
Lacosamide | <5b | <5b | <5b | <5b | 7 | <5b | <5b |
Meloxicam | <5c | <5c | <5c | <5c | <5c | <5c | <5b |
Midazolam | <5c | <5c | <5c | 40 | <5c | <5c | 36 |
Minaprine | 11 | 6 | <5b | 19 | 7 | 9 | <5b |
Nelfinavir | 7 | <5b | <5b | <5b | 24 | 37 | <5b |
Nicotine | 36 | 8 | <5b | 43 | 37 | 21 | 48 |
Nifedipine | 63 | 32 | <5b | <5b | 58 | 67 | <5b |
Nilotinib | 9 | 23 | <5b | 21 | 10 | 10 | 24 |
Ondansetron | 30 | 6 | 11 | 9 | 18 | 30 | 6 |
Paroxetine | 10 | 6 | 41 | 17 | 17 | 6 | <5b |
Phenacetine | <5b | <5b | <5b | <5b | <5b | 6 | 9 |
Pimozide | 16 | 38 | <5b | 26 | 37 | 11 | <5b |
Propafenone | 10 | <5b | 21 | 23 | 22 | 21 | <5b |
Quinidine | <5b | 17 | 9 | 23 | <5b | <5b | <5b |
Repaglinide | <5b | <5b | 13 | 55 | <5b | <5b | 33 |
Rosiglitazone | 99 | 99 | 95 | 82 | 76 | 99 | <5b |
R-warfarin | 6 | <5b | <5b | <5b | <5b | <5b | <5b |
Saquinavir | <5b | <5b | <5b | 35 | <5b | 8 | 52 |
Sorafenib | <5c | <5b | 36 | <5b | 38 | 36 | 71 |
Tamoxifen | 62 | 68 | 36 | 28 | 63 | 73 | 8 |
Terfenadine | 10 | 21 | 7 | 7 | 62 | 54 | <5b |
Thioridazine | 99 | 91 | 96 | 97 | 97 | 83 | 7 |
Tipranavir | 23 | <5c | <5b | 63 | 63 | 69 | 58 |
Verapamil | <5b | <5b | <5b | 27 | <5b | <5b | 30 |
a The substrate depletion is calculated by using the average peak area of the parent at 90 min and at time zero. Values are expressed in percentages of the average peak area of the parent at time zero. Measurements were performed in duplicate.
b The calculated substrate depletion was below the overall precision (CV) of the screening assay but minor amounts of P450-mediated metabolites were detected by LC-MS.
c The calculated substrate depletion was below the overall precision (CV) of the screening assay and no P450-mediated metabolites could be detected by LC-MS.