Inhibitor | Therapeutic Use and/or Drug Class | IC50 | Ki | Mode of Inhibition | Test System | Marker Reactiona | Imaxb | fub | I/Kic | Iu/Kic | References |
---|---|---|---|---|---|---|---|---|---|---|---|
µM (µg/ml) | µM (µg/ml) | µM | |||||||||
2-Oxo-clopidogrel | Drug metabolite | 33.9 | rCYP2C8 | DBF | Hagihara et al., 2008 | ||||||
4.1 | rCYP2C8 | Ceri-1 | Floyd et al., 2012 | ||||||||
4.2 | rCYP2C8 | Ceri-23 | Floyd et al., 2012 | ||||||||
32.0 | HLM | Amo | Tornio et al., 2014 | ||||||||
2,4-Dichloroaniline | Drug metabolite | 99.4 | HLM | Rosi-OH | Wu et al., 2014 | ||||||
4-Hydroxyospemifene | Drug metabolite | 27.7 | HLM | Amo | FDA, 2013i; Turpeinen et al., 2013 | ||||||
4’-Hydroxyospemifene | Drug metabolite | 7 | HLM | Amo | FDA, 2013i; Turpeinen et al., 2013 | ||||||
7-Epi-paclitaxel | Paclitaxel epimer | 2.1 | HLM | Pacli | Zhang et al., 2009b | ||||||
7-O-succinyl macrolactin A | Antibiotic | 20.5 | HLM | Rosi-OH | Bae et al., 2014 | ||||||
17β-Estradiol (estradiol) | Hormonal replacement therapy | 21.5 | rCYP2C8 | Amo | Walsky et al., 2005a | ||||||
6.6 | Competitive | HLM | Amo | VandenBrink et al., 2011 | |||||||
23.8 | Competitive | HLM | Monte | VandenBrink et al., 2011 | |||||||
17.7 | Competitive | HLM | Pacli | VandenBrink et al., 2011 | |||||||
8.9 | Competitive | HLM | Repa | VandenBrink et al., 2011 | |||||||
23.8 | Competitive | HLM | Rosi | VandenBrink et al., 2011 | |||||||
19 | HLM | Amo | Nirogi et al., 2014 | ||||||||
Abiraterone | Anticancer, CYP17A1 inhibitor | 1.6 | HLM | n/a | 0.65 | 0.002 | 0.81 | <0.01 | EMA, 2012a | ||
Abiraterone acetate | Anticancer, CYP17A1 inhibitor | 1.3 | HLM | n/a | EMA, 2012a | ||||||
Acotiamide (Z-338) | Antidyspeptic, acetylcholinesterase inhibitor | 121 | Competitive | HLM | DBF | Furuta et al., 2004, | |||||
Afatinib | Anticancer, PKI | 94.83 | HLM | Pacli | 0.078 | 0.428 | <0.01 | <0.01 | Wang et al., 2014a | ||
Alisertib (MLN8237) | Anticancer, PKI | 16.3 | n/a | n/a | Pusalkar et al., 2014 | ||||||
Alitretinoin (9-cis-retinoic acid) | Anticancer, retinoid | 17.6 | 20.2 | HLM | Taza | 0.28 | 0.01 | Attar et al., 2003 | |||
Amlodipine | Antihypertensive, CCB | 10.7 | rCYP2C8 | Amo | 0.0319 | 0.07 | <0.01 | <0.01 | Walsky et al., 2005a | ||
6.4 | rCYP2C8 | Ceri-1 | 0.01 | <0.01 | Floyd et al., 2012 | ||||||
4.0 | rCYP2C8 | Ceri-23 | 0.02 | <0.01 | Floyd et al., 2012 | ||||||
9.4 | HLM | Amo | <0.01 | <0.01 | Nirogi et al., 2014 | ||||||
Amodiaquine | Antimalarial | 11.7 | HLM | Monte | 0.047 | <0.01 | VandenBrink et al., 2011 | ||||
>100 | HLM | Pacli | <0.01 | VandenBrink et al., 2011 | |||||||
1.9 | HLM | Repa | 0.02 | VandenBrink et al., 2011 | |||||||
11.0 | HLM | Rosi | <0.01 | VandenBrink et al., 2011 | |||||||
Anastrozole | Anticancer, aromatase inhibitor | 48 | 10 | Competitive | HLM | Tolbu | 0.16 | 0.60 | 0.02 | 0.01 | Grimm and Dyroff, 1997 |
Anidulafungin | Antifungal | 12 | HLM | Amo | 3.07 | 0.16 | 0.51 | 0.08 | Damle et al., 2009 | ||
Apomorphine | Anti-Parkinson, dopamine agonist | 1–10 | rCYP2C8 | DBF | 4 | <0.01 | 8.00 | <0.08 | Salminen et al., 2011 | ||
Apremilast | Antipsoriatic, PDE4 inhibitor | 56.1 | HLM | Pacli | 0.764 | 0.32 | 0.03 | <0.01 | FDA, 2014e | ||
Atazanavir | Antiviral, protease inhibitor | 2.1 | n/a | n/a | 7.66 | 0.14 | 3.65 | 0.51 | FDA, 2015b | ||
Atorvastatin (acid, parent) | Antihyperlipidemic, HMG-CoA reductase inhibitor | 38.4 | 15.9 | Mixed | HLM | Pacli | 0.098 | 0.02 | <0.01 | <0.01 | Tornio et al., 2005 |
38.4 | HLM | Pacli | <0.01 | <0.01 | Sakaeda et al., 2006 | ||||||
21.9 | HLM | Amo | <0.01 | <0.01 | Jenkins et al., 2011 | ||||||
55.7 | rCYP2C8 | Fluo | <0.01 | <0.01 | Schelleman et al., 2014 | ||||||
Atorvastatin acyl-β-d glucuronide (G2) | Drug metabolite | 45 | HLM | Amo | Jenkins et al., 2011 | ||||||
Atorvastatin lactone | Antihyperlipidemic, HMG-CoA reductase inhibitor | 28.8 | HLM | Pacli | Sakaeda et al., 2006 | ||||||
Atrazine | Pesticide | 31.3 | HLM | Amo | Abass et al., 2009 | ||||||
Axitinib | Anticancer, PKI | 0.5 | HLM | Pacli | 0.16 | 0.01 | 0.32 | <0.01 | FDA, 2012f | ||
0.11 | HLM | Amo | 2.90 | 0.03 | Filppula et al., 2014 | ||||||
0.17 | HLM | Pacli | 0.94 | <0.01 | Wang et al., 2014a | ||||||
AZD2624 | Antipsychotic, neurokinin-3 receptor and tachykinin receptor 3 antagonist | 83.3 | HLM | Amo | 0.7 | 0.02 | Li et al., 2010 | ||||
Azilsartan medoxomil | Antihypertensive, prodrug | 3.5 | HLM | Pacli | FDA, 2011f | ||||||
Belinostat | Anticancer, histone deacetylase inhibitor | 100 | HLM | n/a | 100 | 0.071 | 2.00 | 0.14 | FDA, 2014c | ||
Belinostat 3-ASBA (M24) | Drug metabolite | 49.1 | HLM | n/a | FDA, 2014c | ||||||
Belinostat acid (M26) | Drug metabolite | 22.1 | HLM | n/a | FDA, 2014c | ||||||
Belinostat amide | Drug metabolite | 30.8 | HLM | n/a | FDA, 2014c | ||||||
Belinostat PX106507 | Drug metabolite | 13.8 | HLM | n/a | FDA, 2014c | ||||||
Benzbromarone | Antihyperuricemic, XO inhibitor | 0.055 | Competitive | HLM | Amo | VandenBrink et al., 2011 | |||||
0.38 | Competitive | HLM | Monte | VandenBrink et al., 2011 | |||||||
0.95 | Competitive | HLM | Pacli | VandenBrink et al., 2011 | |||||||
0.15 | Competitive | HLM | Repa | VandenBrink et al., 2011 | |||||||
0.36 | Competitive | HLM | Rosi | VandenBrink et al., 2011 | |||||||
(−)-N-3-benzyl-phenobarbital | Phenobarbital derivative | 34 | HLM | Pacli | Cai et al., 2004 | ||||||
Bezafibrate | Antihyperlipidemic, PPARα agonist | 74 | HLM | Pacli | 39.5 | 0.05 | 1.07 | 0.05 | Fujino et al., 2003a | ||
9.7 | Competitive | HLM | Pacli | 4.07 | 0.20 | Kajosaari et al., 2005a | |||||
Bisphenol A | Bisphenol | 97 | Noncompetitive | rCYP2C8 | Ami | Niwa et al., 2000 | |||||
BTFM gemfibrozil | Gemfibrozil analog | 13 | HLM | Amo | Jenkins et al., 2011 | ||||||
BTFM gemfibrozil acyl-β-d-glucuronide | Gemfibrozil acyl-β-d-glucuronide analog | 37 | HLM | Amo | Jenkins et al., 2011 | ||||||
Cabozantinib | Anticancer, PKI | 5.0 | rCYP2C8 | n/a | 3.27 | <0.003 | 1.31 | <0.01 | FDA, 2012c | ||
6.4 | 4.6 | Noncompetitive | HLM | Amo | 0.71 | <0.01 | FDA, 2012c | ||||
3.8 | 4.6 | Noncompetitive | HLM | Amo | 0.71 | <0.01 | Lacy et al., 2015; Nguyen et al., 2015 | ||||
Canagliflozin | Antidiabetic, SGLT2 inhibitor | 75 | n/a | n/a | 7.60 | 0.017 | 0.20 | <0.01 | FDA, 2013e | ||
Canagliflozin glucuronide (M7) | Drug metabolite | 64 | n/a | Amo | FDA, 2013e | ||||||
Candesartan | Antihypertensive, ARB | 36.2 | rCYP2C8 | Amo | 0.19 | 0.002 | 0.01 | <0.01 | Walsky et al., 2005a | ||
Candesartan cilexetil | Antihypertensive, prodrug | 0.496 | rCYP2C8 | Amo | 0.41 | <0.01 | 1.65 | 0.02 | Walsky et al., 2005a | ||
3.04 | HLM | Amo | 0.27 | <0.01 | Walsky et al., 2005a | ||||||
Carbaryl | Pesticide | 34.0 | HLM | Amo | Abass et al., 2009 | ||||||
Carvedilol | Antihypertensive | 16.6 | rCYP2C8 | Amo | 0.258 | 0.05 | 0.03 | <0.01 | Walsky et al., 2005a | ||
Cefuroxime axetil | Antibiotic, prodrug | 11.1 | rCYP2C8 | Amo | 19.6 | 0.67 | 3.53 | 2.37 | Walsky et al., 2005a | ||
Celecoxib | Anti-inflammatory, NSAID | 15.9 | rCYP2C8 | Amo | 1.85 | 0.03 | 0.23 | <0.01 | Walsky et al., 2005a | ||
4.9 | Competitive | HLM | Amo | 0.38 | 0.01 | VandenBrink et al., 2011 | |||||
7.9 | Competitive | HLM | Monte | 0.23 | <0.01 | VandenBrink et al., 2011 | |||||
54.4 | Competitive | HLM | Pacli | 0.03 | <0.01 | VandenBrink et al., 2011 | |||||
3.1 | Competitive | HLM | Repa | 0.60 | 0.02 | VandenBrink et al., 2011 | |||||
5.1 | Competitive | HLM | Rosi | 0.36 | 0.01 | VandenBrink et al., 2011 | |||||
9.9 | rCYP2C8 | Ceri-1 | 0.37 | 0.01 | Floyd et al., 2012 | ||||||
5.4 | rCYP2C8 | Ceri-23 | 0.69 | 0.02 | Floyd et al., 2012 | ||||||
Ceritinib | Anticancer, PKI | 0.6d | 4.86d | HLM | Amo | 1.81 | 0.028 | 0.37 | 0.01 | FDA, 2014i | |
0.6d | HLM | Pacli | 6.03 | 0.17 | FDA, 2014i | ||||||
Cerivastatin (acid, parent) | Antihyperlipidemic, HMG-CoA reductase inhibitor | 34.4 | HLM | Pacli | 0.0085 | <0.01 | <0.01 | <0.01 | Fujino et al., 2004 | ||
30.0 | 31.7 | Mixed | HLM | Pacli | <0.01 | <0.01 | Tornio et al., 2005 | ||||
29.8 | HLM | Pacli | <0.01 | <0.01 | Sakaeda et al., 2006 | ||||||
4.2 | Competitive | HLM | Amo | <0.01 | <0.01 | VandenBrink et al., 2011 | |||||
4.6 | Competitive | HLM | Monte | <0.01 | <0.01 | VandenBrink et al., 2011 | |||||
77.4 | Competitive | HLM | Pacli | <0.01 | <0.01 | VandenBrink et al., 2011 | |||||
4.4 | Competitive | HLM | Repa | <0.01 | <0.01 | VandenBrink et al., 2011 | |||||
13.4 | Competitive | HLM | Rosi | <0.01 | <0.01 | VandenBrink et al., 2011 | |||||
Cerivastatin lactone | Antihyperlipidemic, HMG-CoA reductase inhibitor | 44.3 | HLM | Pacli | Sakaeda et al., 2006 | ||||||
Chlorpyrifos | Pesticide | 22.2 | HLM | Amo | Abass et al., 2009 | ||||||
Chlorpromazine | Antipsychotic | 20 | HLM | Amo | 0.470 | 0.05 | 0.05 | <0.01 | Nirogi et al., 2014 | ||
Cimetidine | Antiulcerative, H2RA | 250 | HLM | Pacli | 12 | 0.81 | 0.10 | 0.08 | Monsarrat et al., 1997 | ||
Ciprofibrate | Antihyperlipidemic, PPARα agonist | 441 | HLM | Pacli | 83.0 | 0.01 | 0.38 | <0.01 | Fujino et al., 2003a | ||
Clofazimine | Antilepric | 14.1 | HLM | Pacli | Shimokawa et al., 2015 | ||||||
Clopidogrel | Antithrombotic, platelet aggregation inhibitor | 10.2 | rCYP2C8 | Amo | 0.06 | 0.02 | 0.01 | <0.01 | Walsky et al., 2005a | ||
33.2 | rCYP2C8 | DBF | <0.01 | <0.01 | Hagihara et al., 2008 | ||||||
2.8 | rCYP2C8 | Ceri-1 | 0.04 | <0.01 | Floyd et al., 2012 | ||||||
3.4 | rCYP2C8 | Ceri-23 | 0.04 | <0.01 | Floyd et al., 2012 | ||||||
53.6 | HLM | Amo | <0.01 | <0.01 | Tornio et al., 2014 | ||||||
Clopidogrel carboxylic acid | Drug metabolite | >50.0 | rCYP2C8 | DBF | Hagihara et al., 2008 | ||||||
107 | rCYP2C8 | Ceri-1 | Floyd et al., 2012 | ||||||||
136 | rCYP2C8 | Ceri-23 | Floyd et al., 2012 | ||||||||
Clopidogrel active metabolite | Drug metabolite | >50.0 | rCYP2C8 | DBF | Hagihara et al., 2008 | ||||||
Clotrimazole | Antifungal | 2.5 | Noncompetitive | rCYP2C8 | Torse | 0.008 | <0.01 | Ong et al., 2000 | |||
0.725 | rCYP2C8 | Amo | 0.02 | Walsky et al., 2005a | |||||||
0.776 | HLM | Amo | 0.02 | Walsky et al., 2005a | |||||||
0.12 | Competitive | HLM | Amo | 0.07 | VandenBrink et al., 2011 | ||||||
0.27 | Competitive | HLM | Monte | 0.03 | VandenBrink et al., 2011 | ||||||
0.22 | Competitive | HLM | Pacli | 0.04 | VandenBrink et al., 2011 | ||||||
0.19 | Competitive | HLM | Repa | 0.04 | VandenBrink et al., 2011 | ||||||
1.9 | Competitive | HLM | Rosi | <0.01 | VandenBrink et al., 2011 | ||||||
0.803 | HLM | Pacli | 0.02 | Lee et al., 2012a | |||||||
Cobicistat | Antiviral, pharmacokinetic inhibitor | 30.1 | HLM | Pacli | 2.38 | 0.03 | 0.16 | <0.01 | FDA, 2012j | ||
CP-778875 | Antihyperlipidemic, PPARα agonist | 1.83 | HLM | Amo | Kalgutkar et al., 2013 | ||||||
Cyclosporine | Immunosuppressant, calcineurin inhibitor | 79 | rCYP2C8 | Pacli | 1.11 | 0.07 | 0.03 | <0.01 | Yoshida et al., 2012 | ||
CYP3cide (PF-04981517) | Pharmacokinetic inhibitor | 78 | HLM | Pacli | Walsky et al., 2012 | ||||||
Dabrafenib | Anticancer, PKI | 7.7–8.2 | HLM | Rosi | 2.85 | 0.003 | 0.74 | <0.01 | Lawrence et al., 2014 | ||
Dalcetrapib | Antihyperlipidemic, cholesterylester transfer protein inhibitor | 1.5 | HLM | Pacli | 9.70 | 12.93 | Derks et al., 2009 | ||||
Danazol | Hypoestrogenic, hyperandrogenic, ethisterone derivative | 1.95 | HLM | Pacli | 0.21 | 0.22 | Lee et al., 2012a | ||||
Dasabuvir (ABT-333) | Antiviral, NSB5 inhibitor | ∼17 | Competitive | n/a | n/a | 2.09 | 0.005 | ∼0.25 | <0.01 | FDA, 2014k | |
Dasatinib | Anticancer, PKI | 12 | 3.6 | HLM | Pacli | 0.13 | 0.04 | 0.04 | <0.01 | FDA, 2006a | |
38.6 | HLM | Pacli | <0.01 | <0.01 | Kim et al., 2013b | ||||||
6.31 | HLM | Pacli | 0.02 | <0.01 | Wang et al., 2014a | ||||||
N-debutyldronedarone (SR35021) | Drug metabolite | 24.4 | 36.6 | Noncompetitive | HLM | Pacli | FDA, 2009a | ||||
N-deethyl sunitinib (SU12662) | Drug metabolite | 52 | HLM | Pacli | FDA, 2006b | ||||||
N-demethylimatinib | Drug metabolite | 99 | HLM | Pacli | FDA, 2001 | ||||||
31.3 | 12.8 | Mixed | HLM | Amo | Filppula et al., 2012 | ||||||
N-demethyltoremifene | Drug metabolite | 2.1 | HLM | Pacli | Kim et al., 2011b | ||||||
Deferasirox | Antidote, iron chelating agent | 100 | HLM | Pacli | 0.46 | 0.01 | <0.01 | <0.01 | FDA, 2005a | ||
Deferasirox metabolite CGP82813A | Drug metabolite | 160 | HLM | Pacli | FDA, 2005a | ||||||
Dexamethasone | Anti-inflammatory, glucucorticoid | 12.0 | rCYP2C8 | Amo | 8.15 | 1.36 | Walsky et al., 2005a | ||||
Diclofenac | Anti-inflammatory, NSAID | 54 | HLM | Amo | 6.28 | <0.005 | 0.23 | <0.01 | Jenkins et al., 2011 | ||
Diclofenac acyl glucuronide | Drug metabolite | 14 | HLM | Amo | Jenkins et al., 2011 | ||||||
Diethyldithiocarbamate | Alcoholic detergent | 129.5 | rCYP2C8 | Dia | Sai et al., 2000 | ||||||
464.1 | rCYP2C8 | Phena | Sai et al., 2000 | ||||||||
Diethylstilbestrol | Synthetic estrogen | 8.0 | Competitive | HLM | Pacli | Qu et al., 2011 | |||||
Diltiazem | Antihypertensive, CCB | 25 | rCYP2C8 | Ceri-1 | 0.335 | 0.22 | 0.03 | <0.01 | Floyd et al., 2012 | ||
124 | rCYP2C8 | Ceri-23 | <0.01 | <0.01 | Floyd et al., 2012 | ||||||
Doxorubicin | Anticancer | 2 | HLM | Pacli | 1.63 | 0.24 | 1.63 | 0.39 | Monsarrat et al., 1997 | ||
64.8 | Competitive | HLM | Pacli | 0.03 | <0.01 | Bun et al., 2003 | |||||
90 | Noncompetitive | HLM | Luci | 0.02 | <0.01 | Masek et al., 2011 | |||||
Duloxetine | Antidepressant, SNRI | 180 | HLM | Pacli | 0.079 | 0.05 | <0.01 | <0.01 | FDA, 2008b | ||
60 | HLM | Amo | <0.01 | <0.01 | Paris et al., 2009 | ||||||
Efavirenz | Antiviral, NNRTI | 4.0 | rCYP2C8 | Amo | 12.6 | 0.005 | 6.30 | 0.03 | Parikh et al., 2007 | ||
6.05 | Competitive | rCYP2C8 | Amo | 2.08 | 0.01 | Xu and Desta, 2013 | |||||
4.78 | Competitive | HLM | Amo | 2.64 | 0.01 | Xu and Desta, 2013 | |||||
Eltrombopag | Antihemorrhagic, c-mpl receptor agonist | 24.8 | HLM | Pacli | 29 | <0.01 | 2.34 | 0.02 | FDA, 2008c | ||
Enzalutamide | Anticancer, antiandrogen | 10 | 5.5 | Mixed | HLM | Amo | 35.7 | 0.02 | 6.50 | 0.13 | FDA, 2012k |
Enzalutamide M1 | Drug metabolite | 20 | HLM | Amo | FDA, 2012k | ||||||
Enzalutamide M2 | Drug metabolite | 28 | HLM | Amo | FDA, 2012k | ||||||
Erlotinib | Anticancer, PKI | 6.17 | 5.8 | Competitive | HLM | Pacli | 6.06 | 0.10 | 1.05 | 0.10 | Dong et al., 2011 |
9.5 | HLM | Pacli | 1.28 | 0.13 | Kim et al., 2013b | ||||||
4.02 | HLM | Pacli | 1.51 | 0.15 | Wang et al., 2014a | ||||||
Esomeprazole (S-omeprazole) | Antiulcerative, PPI | 31.0 | HLM | Amo | 4.5 | 0.05 | 0.29 | 0.02 | Zvyaga et al., 2012 | ||
Ethionamide | Antituberculosis | 110 | HLM | Pacli | 12.99 | 0.70 | 0.24 | 0.17 | Shimokawa et al., 2015 | ||
Etravirine | Antiviral, NNRTI | 19.6 | Noncompetitive | HLM | Pacli | 2.2 | 0.01 | 0.11 | <0.01 | FDA, 2008a | |
Exemestane | Anticancer, aromatase inhibitor | 13.5 | rCYP2C8 | Amo | 0.060 | 0.10 | <0.01 | <0.01 | Walsky et al., 2005a | ||
Febuxostat | Antihyperuricemic, XO inhibitor | 20 | n/a | n/a | 16.78 | 0.007 | 0.84 | <0.01 | Naik et al., 2012 | ||
Felodipine | Antihypertensive, CCB | 0.726 | rCYP2C8 | Amo | 0.0073 | 0.004 | 0.02 | <0.01 | Walsky et al., 2005a | ||
1.20 | HLM | Amo | 0.01 | <0.01 | Walsky et al., 2005a | ||||||
Fenitrothion | Pesticide | 4.3 | HLM | Amo | Abass et al., 2009 | ||||||
Fenofibrate | Antihyperlipidemic, PPARα agonist | 288 | HLM | Pacli | 23.83 | <0.01 | 0.17 | <0.01 | Fujino et al., 2003a | ||
92.6 | Competitive | HLM | Pacli | 0.26 | <0.01 | Kajosaari et al., 2005a | |||||
2.39 | rCYP2C8 | Amo | 19.94 | 0.20 | Walsky et al., 2005a | ||||||
4.8 | rCYP2C8 | Fluo | 9.93 | 0.10 | Schelleman et al., 2014 | ||||||
Fluoxymesterone | Androgenic, 3-oxoandrosten (4) derivative | 16 | rCYP2C8 | Ceri-1 | Floyd et al., 2012 | ||||||
16 | rCYP2C8 | Ceri-23 | Floyd et al., 2012 | ||||||||
Fluticasone | Anti-inflammatory, glucocorticoid | 0.58 | HLM | Pacli | 0.00023 | 0.01 | <0.01 | <0.01 | FDA, 2013c | ||
Fluticasone M10 metabolite | Drug metabolite | 80 | HLM | Pacli | FDA, 2013c | ||||||
Fluvastatin (acid, parent) | Antihyperlipidemic, HMG-CoA reductase inhibitor | 20 | HLM | Pacli | 0.461 | 0.01 | 0.05 | <0.01 | Fischer et al., 1999 | ||
36.7 | 18.9 | Mixed | HLM | Pacli | 0.02 | <0.01 | Tornio et al., 2005 | ||||
15.1 | rCYP2C8 | Amo | 0.06 | <0.01 | Walsky et al., 2005a | ||||||
70.2 | HLM | Pacli | 0.01 | <0.01 | Sakaeda et al., 2006 | ||||||
Fluvastatin lactone | Antihyperlipidemic, HMG-CoA reductase inhibitor | 55.4 | HLM | Pacli | Sakaeda et al., 2006 | ||||||
Gefitinib | Anticancer, PKI | 31.0 | HLM | Pacli | 0.8 | 0.10 | 0.05 | <0.01 | Kim et al., 2013b | ||
12.3 | HLM | Amo | 0.13 | 0.01 | Filppula et al., 2014 | ||||||
8.69 | HLM | Pacli | 0.09 | <0.01 | Wang et al., 2014a | ||||||
Gemfibrozil | Antihyperlipidemic, PPARα agonist | 49 | Hep | Ceri-23 | 100 | <0.03 | 4.08 | 0.12 | Prueksaritanont et al., 2002 | ||
87 | Competitive | HLM | Pacli | 1.15 | 0.03 | Prueksaritanont et al., 2002 | |||||
78 | rCYP2C8 | Ceri-1 | 2.56 | 0.08 | Wang et al., 2002 | ||||||
68 | rCYP2C8 | Ceri-23 | 2.94 | 0.09 | Wang et al., 2002 | ||||||
>250 | 273 | Competitive | HLM | Ceri-1 | <0.37 | <0.01 | Wang et al., 2002 | ||||
95 | 69 | Competitive | HLM | Ceri-23 | 1.45 | 0.04 | Wang et al., 2002 | ||||
91 | 75–76 | Competitive | HLM | Pacli | 1.33 | 0.04 | Wang et al., 2002 | ||||
48 | Mixed | HLM | Pacli | 4.17 | 0.13 | Fujino et al., 2003a | |||||
55.4 | Mixed | HLM | Pacli | 1.81 | 0.05 | Fujino et al., 2003b | |||||
36.8 | rCYP2C8 | Ceri-1 | 5.44 | 0.16 | Shitara et al., 2004 | ||||||
29.7 | rCYP2C8 | Ceri-23 | 6.73 | 0.20 | Shitara et al., 2004 | ||||||
119 | 69.0 | Noncompetitive | HLM | Rosi-OH | 1.45 | 0.04 | Hruska et al., 2005 | ||||
30.4 | Competitive | HLM | Pacli | 3.29 | 0.10 | Kajosaari et al., 2005a | |||||
75.6 | rCYP2C8 | Amo | 2.65 | 0.08 | Walsky et al., 2005a | ||||||
59 | HLM | Pio | 3.39 | 0.10 | Jaakkola et al., 2006c | ||||||
120 | HLM | Pacli | 1.67 | 0.05 | Ogilvie et al., 2006 | ||||||
107 | HLM | Monte | 1.87 | 0.06 | Karonen et al., 2010 | ||||||
63 | HLM | Monte-4 | 3.18 | 0.10 | Karonen et al., 2010 | ||||||
120 | HLM | Amo | 1.67 | 0.05 | Jenkins et al., 2011 | ||||||
10.2 | Competitive | HLM | Amo | 9.80 | 0.29 | VandenBrink et al., 2011 | |||||
13.5 | Competitive | HLM | Monte | 7.41 | 0.22 | VandenBrink et al., 2011 | |||||
>100 | Competitive | HLM | Pacli | 1.00 | 0.03 | VandenBrink et al., 2011 | |||||
9.3 | Competitive | HLM | Repa | 10.75 | 0.32 | VandenBrink et al., 2011 | |||||
36.1 | Competitive | HLM | Rosi | 2.77 | 0.08 | VandenBrink et al., 2011 | |||||
14 | rCYP2C8 | Ceri-23 | 7.14 | 0.21 | Floyd et al., 2012 | ||||||
Genistein | Anticancer, PKI | 2.5 | HLM | Pacli | Burnett et al., 2011 | ||||||
Glipizide | Antidiabetic, sulfonylurea | 338.2 | rCYP2C8 | Fluo | 1.04 | 0.016 | <0.01 | <0.01 | Schelleman et al., 2014 | ||
Glyburide (glibenclamide) | Antidiabetic, sulfonylurea | 10.8 | rCYP2C8 | Amo | 0.214 | 0.002 | 0.04 | <0.01 | Walsky et al., 2005a | ||
4.3 | rCYP2C8 | Ceri-1 | 0.10 | <0.01 | Floyd et al., 2012 | ||||||
6.7 | rCYP2C8 | Ceri-23 | 0.06 | <0.01 | Floyd et al., 2012 | ||||||
Glyphosate | Pesticide | 82.0 | HLM | Amo | Abass et al., 2009 | ||||||
Hydroxymethyl-ivacaftor (M1) | Drug metabolite | 17.7 | 0.39 | Competitive | HLM | Amo | FDA, 2012g | ||||
Ibrutinib | Anticancer, PKI | 12.03 | HLM | Pacli | 0.37 | 0.127 | 0.03 | <0.01 | FDA, 2013d | ||
Ibrutinib metabolite PCI-45227 | Drug metabolite | (7.84) | HLM | Pacli | FDA, 2013d | ||||||
Iclaprim | Antibiotic | (91.5) | rCYP2C8 | n/a | Hall et al., (2007) | ||||||
ID951551 | Acotiamide analog | 17 | HLM | DBF | Furuta et al., 2004 | ||||||
Idelalisib | Anticancer, PKI | 13 | HLM | Pacli | 4.6 | <0.16 | 0.71 | 0.11 | FDA, 2014h | ||
Idelalisib metabolite GS-563117 | Drug metabolite | 39.8 | HLM | Pacli | 9.4 | <0.12 | 0.47 | 0.06 | FDA, 2014h | ||
Imatinib | Anticancer, PKI | 15.7 | 8.4 | Mixed | HLM | Amo | 5.27 | 0.05 | 0.63 | 0.03 | Filppula et al., 2012 |
25.9 | HLM | Pacli | 0.41 | 0.02 | Kim et al., 2013b | ||||||
11.28 | HLM | Pacli | 0.47 | 0.02 | Wang et al., 2014a | ||||||
Indacaterol | Antiobstructive, LABA | 30 | HLM | Pacli | 0.00125 | 0.049 | <0.01 | <0.01 | FDA, 2011a | ||
Indiplon | Sedative, GABAA receptor modulator | 30 | 15 | HLM | Pacli | Madan et al., 2007 | |||||
Indomethacin | Anti-inflammatory, NSAID | 88 | HLM | Amo | 6.7 | 0.10 | 0.15 | 0.02 | Jenkins et al., 2011 | ||
Indomethacin acyl-β-D-glucuronide | Drug metabolite | 26 | HLM | Amo | Jenkins et al., 2011 | ||||||
Ipriflavone M1 | Drug metabolite | 9.9 | HLM | Pacli | Moon et al., 2007 | ||||||
Ipriflavone M2 | Drug metabolite | 10.2 | HLM | Pacli | Moon et al., 2007 | ||||||
Ipriflavone M4 | Drug metabolite | 31.8 | HLM | Pacli | Moon et al., 2007 | ||||||
Ipriflavone M5 | Drug metabolite | 2.5 | HLM | Pacli | Moon et al., 2007 | ||||||
Irbesartan | Antihypertensive, ARB | 9.73 | rCYP2C8 | Amo | 3.0 | 0.10 | 0.62 | 0.06 | Walsky et al., 2005a | ||
18 | rCYP2C8 | Ceri-1 | 0.33 | 0.03 | Floyd et al., 2012 | ||||||
16 | rCYP2C8 | Ceri-23 | 0.38 | 0.04 | Floyd et al., 2012 | ||||||
Isotretinoin (13-cis-retinoic acid) | Antiacne, retinoid | 15.1 | 66.2 | HLM | Taza | 0.69 | <0.01 | 0.01 | <0.01 | Attar et al., 2003 | |
Isradipine | Antihypertensive, CCB | 5.00 | HLM | Pacli | 0.030 | 0.03 | 0.01 | <0.01 | Lee et al., 2012a | ||
Itraconazole | Antifungal | 31 | rCYP2C8 | Pacli | 0.9 | 0.002 | 0.06 | <0.01 | Yoshida et al., 2012 | ||
Ivacaftor | Antifibrotic | 3.8 | 3.4 | Mixed | HLM | Amo | 13.89 | <0.02 | 4.09 | 0.08 | FDA, 2012g |
Ivacaftor metabolite (M6) | Drug metabolite | 63.1 | HLM | Amo | FDA, 2012g | ||||||
Ketoconazole | Antifungal | 25 | HLM | Pacli | 3.2 | 0.01 | 0.26 | <0.01 | Monsarrat et al., 1997 | ||
2.5 | Noncompetitive | rCYP2C8 | Torse | 1.28 | 0.01 | Ong et al., 2000 | |||||
4.0 | rCYP2C8 | Dia | 1.60 | 0.02 | Sai et al., 2000 | ||||||
8.9 | rCYP2C8 | Phena | 0.72 | <0.01 | Sai et al., 2000 | ||||||
6-9 | HLM | Pacli | 1.07 | 0.01 | Dierks et al., 2001 | ||||||
11.8 | Noncompetitive | HLM | Pacli | 0.27 | <0.01 | Bun et al., 2003 | |||||
87.7 | HLM | Amo | 0.07 | <0.01 | Turpeinen et al., 2005 | ||||||
5.51 | rCYP2C8 | Amo | 1.16 | 0.01 | Walsky et al., 2005a | ||||||
4 | rCYP2C8 | Amo | 1.60 | 0.02 | O'Donnell et al., 2007 | ||||||
2.45 | HLM | Pacli | 2.61 | 0.03 | Lee et al., 2012a | ||||||
1.7 | HLM | Amo | 3.77 | 0.04 | Nirogi et al., 2015 | ||||||
Ketoprofen acyl-β-d-glucuronide | Drug metabolite | 26 | HLM | Amo | Jenkins et al., 2011 | ||||||
KR-32570 | Antiarrhythmic | 30 | HLM | Pacli | Kim et al., 2006 | ||||||
KR-60436 | Antiulcerative, PPI | 30 | HLM | Pacli | Ji et al., 2005 | ||||||
Lansoprazole | Antiulcerative, PPI | 55 | rCYP2C8 | Ceri-1 | 0.671 | 0.03 | 0.02 | <0.01 | Floyd et al., 2012 | ||
19 | rCYP2C8 | Ceri-23 | 0.07 | <0.01 | Floyd et al., 2012 | ||||||
5.75 | HLM | Pacli | 0.23 | <0.01 | Lee et al., 2012a | ||||||
Lapatinib | Anticancer, PKI | 0.60 | Competitive | HLM | Pacli | 4.2 | <0.01 | 7.00 | <0.07 | FDA, 2007e | |
1.43 | HLM | Pacli | 2.94 | <0.03 | Wang et al., 2014a | ||||||
Laropiprant | Antiasthmatic, PGD2 receptor antagonist | 6.5 | n/a | n/a | Schwartz et al., 2009 | ||||||
Laromustine (VNP40101M) | Anticancer, alkylating agent | >750 | Noncompetitive | HLM | Amo | Nassar et al., 2009 | |||||
Lasofoxifene | Antiosteoporotic, SERM | 8.1 | HLM | Amo | 0.0050 | <0.01 | Moller et al., 2006 | ||||
Lenvatinib | Anticancer, PKI | 10.1 | 10.1 | HLM | Pacli | 1.546 | 0.02 | 0.15 | <0.01 | FDA, 2015a | |
Lestaurtinib (CEP-701) | Anticancer, PKI | 9.5 | HLM | Amo | Filppula et al., 2014 | ||||||
Levothyroxine | Hormonal replacement therapy | 3.30 | rCYP2C8 | Amo | Walsky et al., 2005a | ||||||
5.4 | rCYP2C8 | Ceri-1 | Floyd et al., 2012 | ||||||||
4.6 | rCYP2C8 | Ceri-23 | Floyd et al., 2012 | ||||||||
Loperamide | Antidiarrheal, opioid | 24 | HLM | Amo | 0.0042 | <0.01 | Nirogi et al., 2014 | ||||
Lopinavir | Antiviral, protease inhibitor | 4.1 | rCYP2C8 | Amo | 15.6 | 0.02 | 7.61 | 0.15 | Parikh et al., 2007 | ||
Loratadine | Antihistamine | 3.36 | rCYP2C8 | Amo | 0.0088 | 0.03 | <0.01 | <0.01 | Walsky et al., 2005a | ||
2.95 | HLM | Pacli | <0.01 | <0.01 | Lee et al., 2012a | ||||||
Lorcaserin | Antiobesity, 5-HT2C receptor agonist | >200 | HLM | Pacli | 0.434 | 0.30 | <0.01 | <0.01 | FDA, 2012b | ||
Lorcaserin sulfamate (M1) | Drug metabolite | >200 | HLM | Pacli | FDA, 2012b | ||||||
Losartan | Antihypertensive, ARB | 12.9 | rCYP2C8 | Amo | 0.64 | 0.013 | 0.10 | <0.01 | Walsky et al., 2005a | ||
40.7 | Competitive | rCYP2C8 | Pacli | 0.02 | <0.01 | Mukai et al., 2014 | |||||
Lovastatin (lactone, parent) | Antihyperlipidemic, HMG-CoA reductase inhibitor | 14.7 | 8.4 | Mixed | HLM | Pacli | 0.100 | 0.05 | 0.01 | <0.01 | Tornio et al., 2005 |
9.10 | rCYP2C8 | Amo | 0.02 | <0.01 | Walsky et al., 2005a | ||||||
79.9 | HLM | Pacli | <0.01 | <0.01 | Sakaeda et al., 2006 | ||||||
5.6 | Competitive | HLM | Amo | 0.02 | <0.01 | VandenBrink et al., 2011 | |||||
9.3 | Competitive | HLM | Monte | 0.01 | <0.01 | VandenBrink et al., 2011 | |||||
18.8 | Competitive | HLM | Pacli | <0.01 | <0.01 | VandenBrink et al., 2011 | |||||
2.8 | Competitive | HLM | Repa | 0.04 | <0.01 | VandenBrink et al., 2011 | |||||
4.2 | Competitive | HLM | Rosi | 0.02 | <0.01 | VandenBrink et al., 2011 | |||||
27.5 | rCYP2C8 | Fluo | <0.01 | <0.01 | Schelleman et al., 2014 | ||||||
Lovastatin acid | Antihyperlipidemic, HMG-CoA reductase inhibitor | 54.9 | 48.9 | Mixed | HLM | Pacli | 0.011 | 0.05 | <0.01 | <0.01 | Tornio et al., 2005 |
74.6 | HLM | Pacli | <0.01 | <0.01 | Sakaeda et al., 2006 | ||||||
Macitentan | Antihypertensive, ERA | 21 | HLM | Pacli | 0.29 | <0.01 | 0.03 | <0.01 | FDA, 2013k | ||
Macitentan metabolite M6 (ACT-132577) | Drug metabolite | 23 | HLM | Pacli | FDA, 2013k | ||||||
Macrolactin A | Antibiotic | 26.4 | HLM | Rosi-OH | Bae et al., 2014 | ||||||
Malathion | Pesticide | 31.0 | HLM | Amo | Abass et al., 2009 | ||||||
Medroxyprogesterone | Progestin | 4.79 | rCYP2C8 | Amo | 0.123 | 0.14 | 0.05 | <0.01 | Walsky et al., 2005a | ||
0.76 | Competitive | HLM | Amo | 0.16 | 0.02 | VandenBrink et al., 2011 | |||||
7.5 | Competitive | HLM | Monte | 0.02 | <0.01 | VandenBrink et al., 2011 | |||||
8.2 | Competitive | HLM | Pacli | 0.02 | <0.01 | VandenBrink et al., 2011 | |||||
1.9 | Competitive | HLM | Repa | 0.07 | <0.01 | VandenBrink et al., 2011 | |||||
6.6 | Competitive | HLM | Rosi | 0.02 | <0.01 | VandenBrink et al., 2011 | |||||
Mefenamic acid | Anti-inflammatory, NSAID | 14.9 | HLM | Amo | 41.44 | <0.10 | 5.56 | 0.56 | Jenkins et al., 2011 | ||
Mefenamic acyl-β-d-glucuronide | Drug metabolite | 8.5 | HLM | Amo | Jenkins et al., 2011 | ||||||
Mertansine (DM1) | Antibody-drug linker | 11 | Competitive | HLM | Pacli | Davis et al., 2012 | |||||
Methoxsalen (8-methoxypsoralen) | Antipsoriatic | ∼10 | HLM | Pacli | 2.36 | ∼0.47 | Dierks et al., 2001 | ||||
Methyl belinostat | Drug metabolite | 13.8 | HLM | n/a | FDA, 2014c | ||||||
Methylprednisolone | Anti-inflammatory, glucucorticoid | 25.4 | rCYP2C8 | Amo | 0.475 | 0.22 | 0.04 | <0.01 | Walsky et al., 2005a | ||
Midazolam | Sedative, benzodiazepine | 18 | Noncompetitive | rCYP2C8 | Torse | 0.34 | 0.02 | 0.02 | <0.01 | Ong et al., 2000 | |
12.4 | rCYP2C8 | Amo | 0.06 | <0.01 | Walsky et al., 2005a | ||||||
MMB4 DMS | Antidote, cholinergic agonist | 82.9 | 126 | Noncompetitive | rCYP2C8 | Luci | Hong et al., 2013 | ||||
Mometasone furoate | Anti-inflammatory, glucucorticoid | 0.813 | rCYP2C8 | Amo | 0.00012 | 0.02 | <0.01 | <0.01 | Walsky et al., 2005a | ||
0.327 | HLM | Amo | <0.01 | <0.01 | Walsky et al., 2005a | ||||||
Montelukast | Antiasthmatic, LTRA | 0.00922 | rCYP2C8 | Amo | 0.89 | <0.01 | 193.06 | 1.93 | Walsky et al., 2005a | ||
0.0196 | HLM | Amo | 90.82 | 0.91 | Walsky et al., 2005a | ||||||
0.0092 | Competitive | rCYP2C8 | Amo | 96.74 | 0.97 | Walsky et al., 2005b | |||||
0.019 | Competitive | rCYP2C8 | Rosi | 46.84 | 0.47 | Walsky et al., 2005b | |||||
0.020–2.0 | 0.014 | Competitive | HLM | Amo | 63.57 | 0.64 | Walsky et al., 2005b | ||||
0.15 | Competitive | HLM | Pacli | 5.93 | 0.06 | Walsky et al., 2005b | |||||
0.11 | Competitive | HLM | Rosi | 8.09 | 0.08 | Walsky et al., 2005b | |||||
0.18 | HLM | Pio | 9.89 | 0.10 | Jaakkola et al., 2006c | ||||||
0.009–0.01 | rCYP2C8 | Amo | 197.78 | 1.98 | O'Donnell et al., 2007 | ||||||
0.022 | 0.013 | HLM | Amo | 68.46 | 0.69 | Perloff et al., 2009 | |||||
0.0081 | Competitive | HLM | Amo | 109.88 | 1.10 | VandenBrink et al., 2011 | |||||
0.026 | Competitive | HLM | Pacli | 34.23 | 0.34 | VandenBrink et al., 2011 | |||||
0.016 | Competitive | HLM | Repa | 55.63 | 0.56 | VandenBrink et al., 2011 | |||||
0.21 | Competitive | HLM | Rosi | 4.24 | 0.04 | VandenBrink et al., 2011 | |||||
1.2 | rCYP2C8 | Ceri-1 | 1.48 | 0.02 | Floyd et al., 2012 | ||||||
0.02 | rCYP2C8 | Ceri-23 | 89.00 | 0.89 | Floyd et al., 2012 | ||||||
0.05–0.10 | HLM | Amo | 35.60 | 0.36 | Kozakai et al., 2012 | ||||||
0.14 | Competitive | HLM | Pacli | 6.36 | 0.06 | Kim et al., 2013b | |||||
0.16 | Competitive | HLM | Amo | 5.56 | 0.06 | Kim et al., 2013b | |||||
2.67 | HLM | Pacli | 0.67 | <0.01 | Zheng et al., 2013 | ||||||
0.27 | n/a | n/a | 6.59 | 0.07 | Korzekwa, 2014 | ||||||
159 | Hep | Amo | 0.01 | <0.01 | Kosugi et al., 2014 | ||||||
2.9 | HLM | Rosi-OH | 0.61 | <0.01 | Zheng et al., 2014 | ||||||
0.101 | HLM | Pacli | 17.62 | 0.18 | FDA, 2014j | ||||||
0.14 | HLM | Amo | 12.71 | 0.13 | FDA, 2014j | ||||||
0.010–0.75 | HLM | Amo | 178.00 | 1.78 | Nirogi et al., 2015 | ||||||
Nebivolol | Antihypertensive, β1 receptor blocker | 55 | Noncompetitive | HLM | Pacli | 3.65 | 0.0887 | 0.07 | <0.01 | FDA, 2007a | |
Nefazodone | Antidepressant | 23.2 | rCYP2C8 | Amo | 4.70 | <0.01 | 0.41 | <0.01 | Walsky et al., 2005a | ||
Netupitant | Antiemetic | 50.43 | HLM | Pacli | 0.75 | 0.005 | 0.03 | <0.01 | FDA, 2014b | ||
Netupitant hydroxylation metabolite M3 | Drug metabolite | 26.95 | HLM | Pacli | FDA, 2014b | ||||||
Netupitant N-demethylation metabolite M1 | Drug metabolite | 4.74 | HLM | Pacli | FDA, 2014b | ||||||
Nicardipine | Antihypertensive, CCB | 7.1 | HLM | Pacli | 0.17 | 0.02 | 0.02 | <0.01 | Nakamura et al., 2005 | ||
1.56 | HLM | Pacli | 0.22 | <0.01 | Lee et al., 2012a | ||||||
Nifedipine | Antihypertensive, CCB | 9.66 | rCYP2C8 | Amo | 0.14 | 0.04 | 0.03 | <0.01 | Walsky et al., 2005a | ||
20-23 | rCYP2C8 | Amo | 0.01 | <0.01 | O'Donnell et al., 2007 | ||||||
13.53 | rCYP2C8 | Pacli | 0.02 | <0.01 | Gao et al., 2010 | ||||||
2.4 | Competitive | HLM | Amo | 0.06 | <0.01 | VandenBrink et al., 2011 | |||||
6.3 | Competitive | HLM | Monte | 0.02 | <0.01 | VandenBrink et al., 2011 | |||||
9.5 | Competitive | HLM | Pacli | 0.02 | <0.01 | VandenBrink et al., 2011 | |||||
1.5 | Competitive | HLM | Repa | 0.09 | <0.01 | VandenBrink et al., 2011 | |||||
5.8 | Competitive | HLM | Rosi | 0.02 | <0.01 | VandenBrink et al., 2011 | |||||
3.5 | HLM | Amo | 0.08 | <0.01 | Nirogi et al., 2014 | ||||||
Nilotinib | Anticancer, PKI | <1 | 0.236 | Competitive | HLM | Pacli | 4.3 | 0.02 | 18.22 | 0.36 | FDA, 2007c |
0.61 | Competitive | rCYP2C8 | Amo | 7.04 | 0.14 | Kim et al., 2013b | |||||
0.10 | Competitive | rCYP2C8 | Pacli | 43.00 | 0.86 | Kim et al., 2013b | |||||
0.7 | 0.15 | Competitive | HLM | Amo | 28.67 | 0.53 | Kim et al., 2013b | ||||
0.4 | 0.9 | Competitive | HLM | Pacli | 4.78 | 0.10 | Kim et al., 2013b | ||||
7.5 | HLM | Rosi-OH | 1.15 | 0.02 | Kim et al., 2013b | ||||||
0.10 | HLM | Pacli | 43.00 | 0.86 | Wang et al., 2014a | ||||||
Nintedanib | Anticancer, PKI | >50 | HLM | Pacli | 0.028 | 0.022 | <0.01 | <0.01 | FDA, 2014d | ||
Nystatin | Antifungal | 12.7 | rCYP2C8 | Amo | Walsky et al., 2005a | ||||||
Ombitasvir (ABT-267) | Antiviral, NS5A inhibitor | 7.4 | n/a | n/a | 0.070 | <0.01 | 0.02 | <0.01 | FDA, 2014k | ||
Orphenadrine | Muscle relaxant | 278.8 | rCYP2C8 | Dia | Sai et al., 2000 | ||||||
249.1 | rCYP2C8 | Phena | Sai et al., 2000 | ||||||||
265 | HLM | Amo | Nirogi et al., 2015 | ||||||||
Orteronel (TAK-700) | Anticancer, antiandrogen | 27.7 | HLM | n/a | Lu et al., 2012 | ||||||
Ospemifene | Antidyspareunia, SERM | 36.4 | HLM | Amo | 3.16 | <0.01 | 0.17 | <0.01 | FDA, 2013i; Turpeinen et al., 2013 | ||
Oxybutynin | Anticholinergic | 4.50 | rCYP2C8 | Amo | 0.031 | <0.01 | 0.01 | <0.01 | Walsky et al., 2005a | ||
Paclitaxel (taxol) | Anticancer, taxane | 14.9 | 30.0 | Competitive | HLM | Taza | 0.85 | 0.12 | 0.03 | <0.01 | Attar et al., 2003 |
13.3 | rCYP2C8 | Amo | 0.13 | 0.02 | Walsky et al., 2005a | ||||||
23–24 | rCYP2C8 | Amo | 0.07 | <0.01 | O'Donnell et al., 2007 | ||||||
5.4 | Competitive | HLM | Amo | 0.16 | 0.02 | VandenBrink et al., 2011 | |||||
89.8 | Competitive | HLM | Monte | <0.01 | <0.01 | VandenBrink et al., 2011 | |||||
6.5 | Competitive | HLM | Repa | 0.13 | 0.016 | VandenBrink et al., 2011 | |||||
12.0 | Competitive | HLM | Rosi | 0.07 | <0.01 | VandenBrink et al., 2011 | |||||
Pasireotide | Hormonal therapy, somastatin analog | ∼50 | HLM | Pacli | 0.015 | 0.12 | <0.01 | <0.01 | FDA, 2012h | ||
Pazopanib | Anticancer, PKI | 10 | HLM | Pacli | 132 | <0.01 | 26.40 | 0.26 | FDA, 2009d | ||
3.72 | HLM | Pacli | 35.48 | 0.36 | Wang et al., 2014a | ||||||
PF-562,271 | Anticancer, PKI | 23 | HLM | n/a | Rong et al., 2008 | ||||||
Phenthoate | Pesticide | 10.3 | HLM | Amo | Abass et al., 2009 | ||||||
Pioglitazone | Antidiabetic, PPAR-γ agonist | 9.38 | 1.69 | Competitive | HLM | Pacli | 3.8 | <0.01 | 2.25 | 0.02 | Sahi et al., 2003 |
11.7 | rCYP2C8 | Amo | 0.65 | <0.01 | Walsky et al., 2005a | ||||||
6.6 | Competitive | HLM | Amo | 0.58 | <0.01 | VandenBrink et al., 2011 | |||||
7.1 | Competitive | HLM | Monte | 0.54 | <0.01 | VandenBrink et al., 2011 | |||||
37.6 | Competitive | HLM | Pacli | 0.10 | <0.01 | VandenBrink et al., 2011 | |||||
3.8 | Competitive | HLM | Repa | 1.00 | 0.01 | VandenBrink et al., 2011 | |||||
6.1 | Competitive | HLM | Rosi | 0.62 | <0.01 | VandenBrink et al., 2011 | |||||
14 | rCYP2C8 | Ceri-1 | 0.54 | <0.01 | Floyd et al., 2012 | ||||||
16 | rCYP2C8 | Ceri-23 | 0.48 | <0.01 | Floyd et al., 2012 | ||||||
Pitavastatin (acid, parent) | Antihyperlipidemic, HMG-CoA reductase inhibitor | 57.0 | HLM | Pacli | 0.0296 | 0.005 | <0.01 | <0.01 | Sakaeda et al., 2006 | ||
Pitavastatin lactone | Antihyperlipidemic, HMG-CoA reductase inhibitor | 50.5 | HLM | Pacli | 0.0190 | 0.005 | <0.01 | <0.01 | Sakaeda et al., 2006 | ||
Ponatinib | Anticancer, PKI | 6.1 | 3.05 | n/a | n/a | 0.161 | 0.0008 | 0.05 | <0.01 | FDA, 2012e | |
Prasugrel | Antithrombotic, platelet aggregation inhibitor | >45.2 | rCYP2C8 | DBF | 1.37 | <0.061 | Hagihara et al., 2008 | ||||
Prasugrel active metabolite (R–138727) | Drug metabolite | >45.2 | rCYP2C8 | DBF | Hagihara et al., 2008 | ||||||
Prasugrel thiolactone (R–95913) | Drug metabolite | >50.0 | rCYP2C8 | DBF | Hagihara et al., 2008 | ||||||
Pravastatin (acid, parent) | Antihyperlipidemic, HMG-CoA reductase inhibitor | >100 | >50 | Mixed | HLM | Pacli | 0.085 | 0.57 | <0.01 | <0.01 | Tornio et al., 2005 |
>100 | HLM | Pacli | <0.01 | <0.01 | Sakaeda et al., 2006 | ||||||
Pravastatin lactone | Antihyperlipidemic, HMG-CoA reductase inhibitor | 99.3 | HLM | Pacli | Sakaeda et al., 2006 | ||||||
Profenofos | Pesticide | 84.0 | HLM | Amo | Abass et al., 2009 | ||||||
Promethazine | Sedative, antihistamine | 23 | HLM | Amo | 0.07 | 0.07 | <0.01 | <0.01 | Nirogi et al., 2014 | ||
Propoxyphene | Analgesic, opioid | 32 | rCYP2C8 | Ceri-1 | Floyd et al., 2012 | ||||||
18 | rCYP2C8 | Ceri-23 | Floyd et al., 2012 | ||||||||
Prothionamide | Antituberculosis | 57.6 | HLM | Pacli | Shimokawa et al., 2015 | ||||||
Pyrimethamine | Antimalarial | 45.1 | rCYP2C8 | Amo | 4.74 | 0.13 | 0.21 | 0.027 | Parikh et al., 2007 | ||
Quetiapine | Antipsychotic | 20 | HLM | Amo | 0.314 | 0.17 | 0.03 | <0.01 | Nirogi et al., 2014 | ||
Quinidine | Antiarrhythmic | 98.5 | rCYP2C8 | Dia | 4 | 0.13 | 0.08 | 0.01 | Sai et al., 2000 | ||
135.4 | rCYP2C8 | Phena | 0.06 | <0.01 | Sai et al., 2000 | ||||||
50 | HLM | Pacli | 0.16 | 0.02 | Dierks et al., 2001 | ||||||
Quinine | Antimalarial | 11 | Competitive | rCYP2C8 | Torse | 29 | 0.15 | 2.64 | 0.40 | Ong et al., 2000 | |
R483 | Antidiabetic, PPAR-γ agonist | 5 | HLM | Pacli | Weber et al., 2005 | ||||||
Rabeprazole | Antiulcerative, PPI | 12.0 | rCYP2C8 | Amo | 0.9 | 0.037 | 0.15 | <0.01 | Walsky et al., 2005a | ||
Ranitidine | Antiulcerative, H2RA | 10,000 | HLM | Pacli | 1.31 | 0.85 | <0.01 | <0.01 | Monsarrat et al., 1997 | ||
3.1 | HLM | Amo | 0.85 | 0.72 | Nirogi et al., 2014 | ||||||
Regorafenib | Anticancer, PKI | 1.7 | 0.6 | n/a | n/a | 8.1 | 0.005 | 13.50 | 0.04 | FDA, 2012i | |
Regorafenib M2 | Drug metabolite | 1.0 | n/a | n/a | FDA, 2012i | ||||||
Regorafenib M5 | Drug metabolite | 1.3 | n/a | n/a | FDA, 2012i | ||||||
Repaglinide | Antidiabetic, meglitinide analog | 27.1 | Competitive | HLM | Amo | 0.104 | 0.026 | <0.01 | <0.01 | VandenBrink et al., 2011 | |
11.1 | Competitive | HLM | Monte | <0.01 | <0.01 | VandenBrink et al., 2011 | |||||
>100 | Competitive | HLM | Pacli | <0.01 | <0.01 | VandenBrink et al., 2011 | |||||
23.0 | Competitive | HLM | Rosi | <0.01 | <0.01 | VandenBrink et al., 2011 | |||||
Retinoic acid, all-trans (tretinoin) | Antiacne, retinoid | 27.0 | Competitive | HLM | Pacli | 1.15 | <0.05 | 0.04 | <0.01 | Rahman et al., 1994 | |
Rifampin (rifampicin) | Antibiotic | 30.2 | Competitive | HLM | Pacli | 8 | 0.40 | 0.27 | 0.11 | Kajosaari et al., 2005a | |
Rifapentine | Antituberculosis | 115 | HLM | Pacli | 34.21 | 0.02 | 0.59 | 0.01 | Shimokawa et al., 2015 | ||
Rilpivirine | Antiviral, NNRTI | 13.2–19.1 | 10.0 | HLM | Pacli | 0.5 | <0.01 | 0.05 | <0.01 | FDA, 2011d | |
Ritonavir | Antiviral, protease inhibitor | 3.03 | rCYP2C8 | Amo | 15 | 0.02 | 9.90 | 0.20 | Walsky et al., 2005a | ||
1–2 | rCYP2C8 | Amo | 30.00 | 0.60 | O'Donnell et al., 2007 | ||||||
5.5 | HLM | Pacli | 5.46 | 0.11 | FDA, 2012j | ||||||
Rofecoxib | Anti-inflammatory, NSAID | 95 | rCYP2C8 | Ceri-1 | 1.02 | 0.13 | 0.02 | <0.01 | Floyd et al., 2012 | ||
14 | rCYP2C8 | Ceri-23 | 0.15 | 0.02 | Floyd et al., 2012 | ||||||
Rose bengal | Xanthene dye | 53 | Hep | Amo | Kazmi et al., 2014 | ||||||
Rosiglitazone | Antidiabetic, PPAR-γ agonist | 18 | HLM | Pacli | 1.7 | 0.002 | 0.19 | <0.01 | Baldwin et al., 1999 | ||
9.58 | 5.59 | Competitive | HLM | Pacli | 0.30 | <0.01 | Sahi et al., 2003 | ||||
24.1–26.3 | HLM | Pacli | 0.13 | <0.01 | Kim et al., 2005b | ||||||
10.8 | rCYP2C8 | Amo | 0.13 | <0.01 | Walsky et al., 2005a | ||||||
5.2 | Competitive | HLM | Amo | 0.33 | <0.01 | VandenBrink et al., 2011 | |||||
4.1 | Competitive | HLM | Monte | 0.42 | <0.01 | VandenBrink et al., 2011 | |||||
28.6 | Competitive | HLM | Pacli | 0.06 | <0.01 | VandenBrink et al., 2011 | |||||
1.4 | Competitive | HLM | Repa | 1.21 | <0.01 | VandenBrink et al., 2011 | |||||
3.0 | rCYP2C8 | Ceri-1 | 1.13 | <0.01 | Floyd et al., 2012 | ||||||
2.7 | rCYP2C8 | Ceri-23 | 1.26 | <0.01 | Floyd et al., 2012 | ||||||
Rosuvastatin (acid, parent) | Antihyperlipidemic, HMG-CoA reductase inhibitor | >100 | >50 | Mixed | HLM | Pacli | 0.0046 | 0.12 | <0.01 | <0.01 | Tornio et al., 2005 |
>100 | HLM | Pacli | <0.01 | <0.01 | Sakaeda et al., 2006 | ||||||
Rosuvastatin lactone | Antihyperlipidemic, HMG-CoA reductase inhibitor | 9.8 | HLM | Pacli | Fujino et al., 2004 | ||||||
32.5 | HLM | Pacli | Sakaeda et al., 2006 | ||||||||
Salmeterol | Antiasthmatic, β-2- agonist | 1.87 | rCYP2C8 | Amo | 0.0040 | <0.01 | Walsky et al., 2005a | ||||
Sanguinarine | Anticancer | 10.2 | 8.9 | Noncompetitive | HLM | Pacli | Qi et al., 2013 | ||||
Saquinavir | Antiviral, protease inhibitor | 1.8 | rCYP2C8 | Amo | 1.41 | 0.02 | 1.57 | 0.031 | Parikh et al., 2007 | ||
Saracatinib | Anticancer, PKI | 201.8 | HLM | Amo | Filppula et al., 2014 | ||||||
Sarizotan | Antipsychotic | 18.2d | Competitive | HLM | Pacli | 0.91 | 0.05 | Gallemann et al., 2010 | |||
Satraplatin (JM-216) | Anticancer | 1–3 | 0.9 | Noncompetitive | HLM | Pacli | Ando et al., 1998 | ||||
Seliciclib (R-roscovitine) | Anticancer, PKI | 119 | rCYP2C8 | DBF | 10 | 0.10 | 0.17 | 0.02 | McClue and Stuart, 2008 | ||
Sertraline | Antidepressant, SSRI | 25.5 | rCYP2C8 | Amo | 0.484 | 0.02 | 0.04 | <0.01 | Walsky et al., 2005a | ||
350 | HLM | Pacli | <0.01 | <0.01 | FDA, 2008b | ||||||
>100 | Competitive | HLM | Amo | <0.01 | <0.01 | VandenBrink et al., 2011 | |||||
9.0 | Competitive | HLM | Monte | 0.05 | <0.01 | VandenBrink et al., 2011 | |||||
>100 | Competitive | HLM | Pacli | <0.01 | <0.01 | VandenBrink et al., 2011 | |||||
7.8 | Competitive | HLM | Repa | 0.06 | <0.01 | VandenBrink et al., 2011 | |||||
8.1 | Competitive | HLM | Rosi | 0.06 | <0.01 | VandenBrink et al., 2011 | |||||
29.7 | HLM | Pacli | 0.03 | <0.01 | Erve et al., 2013 | ||||||
15 | HLM | Amo | 0.06 | <0.01 | Nirogi et al., 2014 | ||||||
Simeprevir (TMC435) | Antiviral, protease inhibitor | (36.8) | HLM | n/a | 14.5 | <0.001 | 0.79 | <0.01 | FDA, 2013h | ||
Simvastatin (lactone, parent) | Antihyperlipidemic, HMG-CoA reductase inhibitor | 9.6 | 7.1 | HLM | Pacli | 0.096 | 0.06 | 0.01 | <0.01 | Tornio et al., 2005 | |
5.39 | rCYP2C8 | Amo | 0.04 | <0.01 | Walsky et al., 2005a | ||||||
44.1 | HLM | Pacli | <0.01 | <0.01 | Sakaeda et al., 2006 | ||||||
8.3 | HLM | Amo | 0.02 | <0.01 | Jenkins et al., 2011 | ||||||
7.5 | Competitive | HLM | Amo | 0.01 | <0.01 | VandenBrink et al., 2011 | |||||
5.7 | Competitive | HLM | Monte | 0.02 | <0.01 | VandenBrink et al., 2011 | |||||
12.3 | Competitive | HLM | Pacli | <0.01 | <0.01 | VandenBrink et al., 2011 | |||||
1.1 | Competitive | HLM | Repa | 0.09 | <0.01 | VandenBrink et al., 2011 | |||||
3.3 | Competitive | HLM | Rosi | 0.03 | <0.01 | VandenBrink et al., 2011 | |||||
3.70 | HLM | Pacli | 0.05 | <0.01 | Lee et al., 2012a | ||||||
28 | rCYP2C8 | Fluo | <0.01 | <0.01 | Schelleman et al., 2014 | ||||||
Simvastatin acid | Antihyperlipidemic, HMG-CoA reductase inhibitor | 66.5 | 41.1 | Mixed | HLM | Pacli | Tornio et al., 2005 | ||||
51.5 | HLM | Pacli | Sakaeda et al., 2006 | ||||||||
76.5 | rCYP2C8 | Fluo | Schelleman et al., 2014 | ||||||||
Simvastatin acyl-β-d-glucuronide | Drug metabolite | 3.8 | HLM | Amo | Jenkins et al., 2011 | ||||||
SIPI5357 | Antidepressant, Serotonin-norepinephrine-dopamine reuptake inhibitor | 89.23 | HLM | Pacli | Fan et al., 2015 | ||||||
Sitaxentan | Antihypertensive, ERA | 1.58 | HLM | Pacli | 22.42 | 28.38 | Erve et al., 2013 | ||||
Sorafenib | Anticancer, PKI | 1-2 | rCYP2C8 | Amo | 21.5 | 0.01 | 21.50 | 0.22 | FDA, 2005b | ||
2.4 | n/a | n/a | 8.96 | 0.09 | Flaherty et al., 2011 | ||||||
1.59 | HLM | Pacli | 13.52 | 0.14 | Wang et al., 2014a | ||||||
Spironolactone | Diuretic | 6.99 | rCYP2C8 | Amo | 0.444 | <0.10 | 0.13 | 0.01 | Walsky et al., 2005a | ||
Stiripentol | Antiepileptic | 37.1 | 35 | Noncompetitive | rCYP2C8 | Carba | 28.17 | 0.76 | Cazali et al., 2003 | ||
Sulfaphenazole | Antimicrobial | 63 | Competitive | rCYP2C8 | DTP | Mancy et al., 1996 | |||||
0.42 | rCYP2C8 | R-ibu-2 | Hamman et al., 1997 | ||||||||
0.55 | rCYP2C8 | R-ibu-3 | Hamman et al., 1997 | ||||||||
0.36 | rCYP2C8 | S-ibu-2 | Hamman et al., 1997 | ||||||||
0.38 | rCYP2C8 | S-ibu-3 | Hamman et al., 1997 | ||||||||
505 | rCYP2C8 | Torse | Miners et al., 2000 | ||||||||
172.0 | rCYP2C8 | Dia | Sai et al., 2000 | ||||||||
>50 | HLM | Pacli | Dierks et al., 2001 | ||||||||
Sunitinib | Anticancer, PKI | 28 | HLM | Pacli | 0.21 | 0.05 | <0.01 | <0.01 | FDA, 2006b | ||
91.51 | HLM | Pacli | <0.01 | <0.01 | Wang et al., 2014a | ||||||
Sunitinib metabolite Su012662 | Drug metabolite | 52 | HLM | Pacli | FDA, 2006b | ||||||
Suvorexant | Sedative, orexin receptor antagonist | 15 | HLM | Pacli | 0.96 | <0.01 | 0.13 | <0.01 | FDA, 2014j | ||
Suvorexant M9 (L-002015883) | Drug metabolite | 37 | HLM | Amo | FDA, 2014j | ||||||
Tamoxifen | Anticancer, SERM | 3.34 | rCYP2C8 | Amo | 0.323 | <0.02 | 0.19 | <0.01 | Walsky et al., 2005a | ||
3–10 | rCYP2C8 | Amo | 0.22 | <0.01 | O'Donnell et al., 2007 | ||||||
3.1 | Competitive | HLM | Amo | 0.10 | <0.01 | VandenBrink et al., 2011 | |||||
2.1 | Competitive | HLM | Monte | 0.15 | <0.01 | VandenBrink et al., 2011 | |||||
12.2 | Competitive | HLM | Pacli | 0.03 | <0.01 | VandenBrink et al., 2011 | |||||
10.1 | Competitive | HLM | Repa | 0.03 | <0.01 | VandenBrink et al., 2011 | |||||
2.6 | Competitive | HLM | Rosi | 0.12 | <0.01 | VandenBrink et al., 2011 | |||||
14.3 | HLM | Pacli | 0.06 | <0.01 | Lee et al., 2012a | ||||||
2.3 | HLM | Amo | 0.28 | <0.01 | Nirogi et al., 2014 | ||||||
Tanespimycin | Anticancer | 29 | HLM | Pacli | 17.34 | <0.10 | 1.20 | 0.12 | Gan et al., 2012 | ||
Tasimelteon | Circadian regulator | >100 | HLM | Amo | 0.80 | ∼0.10 | 0.02 | <0.01 | FDA, 2014m | ||
Tasimelteon M12 | Drug metabolite | >100 | HLM | Amo | FDA, 2014m | ||||||
Tegaserod | Gastroprokinetic, 5-HT4 receptor agonist | ∼130 | HLM | Pacli | 0.0065 | 0.02 | <0.01 | <0.01 | Vickers et al., 2001 | ||
Telithromycin | Antibiotic | 87 | rCYP2C8 | Pacli | 2.7 | 0.30 | 0.06 | 0.02 | Yoshida et al., 2012 | ||
Temsirolimus | Anticancer, PKI | 27 | HLM | Pacli | 0.57 | 0.02 | FDA, 2007d | ||||
Terbinafine | Antifungal | ∼150 | HLM | Pacli | 3 | <0.01 | Vickers et al., 1999 | ||||
Terfenadine | Antihistamine | 5 | Noncompetitive | rCYP2C8 | Torse | 0.0033 | 0.03 | <0.01 | <0.01 | Ong et al., 2000 | |
11.5 | rCYP2C8 | Amo | <0.01 | <0.01 | Walsky et al., 2005a | ||||||
19.1 | HLM | Pacli | <0.01 | <0.01 | Erve et al., 2013 | ||||||
Teriflunomide | Immunosuppressant, drug metabolite | 0.174–0.219 | 0.100-0.150 | Competitive, mixed | HLM | Pacli | 0.11 | 0.05 | 1.1 | 0.06 | FDA, 2012l |
Ticagrelor | Antithrombotic, platelet aggregation inhibitor | >50 | HLM | Pacli | 1.3 | <0.02 | Zhou et al., 2011; FDA, 2011b | ||||
Ticagrelor metabolite AR-C124910XX | Drug metabolite | 43 | HLM | Pacli | FDA, 2011b | ||||||
Ticlopidine | Antithrombotic, platelet aggregation inhibitor | 100 | rCYP2C8 | 2-TPE | 3 | 0.02 | 0.06 | <0.01 | Ha-Duong et al., 2001 | ||
43.9 | rCYP2C8 | DBF | 0.14 | <0.01 | Hagihara et al., 2008 | ||||||
29 | HLM | Amo | 0.21 | <0.01 | Nirogi et al., 2015 | ||||||
Tipranavir | Antiviral, protease inhibitor | 2.1 | rCYP2C8 | Amo | 94.8 | <0.01 | 90.29 | <0.90 | Parikh et al., 2007 | ||
Tolbutamide | Antidiabetic, sulfonylurea | 2,370 | Mixed | HLM | Pacli | 196 | 0.09 | 0.08 | <0.01 | Rahman et al., 1994 | |
Trametinib | Anticancer, PKI | 0.34 | HLM | Rosi | 0.032 | 0.038 | 0.19 | 0.01 | FDA, 2013f | ||
Tranylcypromine | Antidepressant, MAOI | 26–35 | HLM | Pacli | 0.42 | 0.03 | Dierks et al., 2001 | ||||
12.1 | rCYP2C8 | Amo | 0.07 | Walsky et al., 2005a | |||||||
103–113 | rCYP2C8 | Amo | <0.01 | O'Donnell et al., 2007 | |||||||
11.24 | rCYP2C8 | Pacli | 0.07 | Gao et al., 2010 | |||||||
22.5 | HLM | Amo | 0.04 | Nirogi et al., 2015 | |||||||
Triamcinolone | Anti-inflammatory, glucocorticoid | 19.3 | rCYP2C8 | Amo | Walsky et al., 2005a | ||||||
32.5 | Competitive | HLM | Amo | VandenBrink et al., 2011 | |||||||
53.1 | Competitive | HLM | Monte | VandenBrink et al., 2011 | |||||||
>100 | Competitive | HLM | Pacli | VandenBrink et al., 2011 | |||||||
42.5 | Competitive | HLM | Repa | VandenBrink et al., 2011 | |||||||
20.4 | Competitive | HLM | Rosi | VandenBrink et al., 2011 | |||||||
Triazolam | Sedative, benzodiazepine | 25 | Noncompetitive | rCYP2C8 | Torse | 0.013 | 0.099 | <0.01 | <0.01 | Ong et al., 2000 | |
Trimethoprim | Antimicrobial, dihydrofolate reductase inhibitor | 75 | rCYP2C8 | Pacli | 4 | 0.63 | 0.05 | 0.03 | Wen et al., 2002 | ||
54 | 32 | Competitive | HLM | Pacli | 0.13 | 0.08 | Wen et al., 2002 | ||||
51.5 | 29.0 | Competitive | HLM | Rosi-OH | 0.14 | 0.09 | Hruska et al., 2005 | ||||
71 | HLM | Pio | 0.11 | 0.07 | Jaakkola et al., 2006c | ||||||
40.6 | rCYP2C8 | Amo | 0.20 | 0.12 | Parikh et al., 2007 | ||||||
34.1 | Competitive | rCYP2C8 | Pio | 0.12 | 0.07 | Tornio et al., 2008b | |||||
38.2 | Competitive | HLM | Pio | 0.10 | 0.07 | Tornio et al., 2008b | |||||
9.2 | Competitive | HLM | Amo | 0.43 | 0.27 | VandenBrink et al., 2011 | |||||
>100 | Competitive | HLM | Monte | <0.04 | <0.03 | VandenBrink et al., 2011 | |||||
>100 | Competitive | HLM | Pacli | <0.04 | <0.03 | VandenBrink et al., 2011 | |||||
8.5 | Competitive | HLM | Repa | 0.47 | 0.30 | VandenBrink et al., 2011 | |||||
13.2 | Competitive | HLM | Rosi | 0.30 | 0.19 | VandenBrink et al., 2011 | |||||
4.5–17 | HLM | Amo | 1.78 | 1.12 | Dinger et al., 2014 | ||||||
122 | Hep | Amo | 0.07 | 0.04 | Kosugi et al., 2014 | ||||||
17.41–20.38 | HLM | Pacli | 0.46 | 0.29 | Peng et al., 2015 | ||||||
Troglitazone | Antidiabetic, PPAR-γ agonist | 1–5 | 0.3 | Competitive | rCYP2C8 | Pacli | 3 | <0.01 | 10.00 | <0.10 | Yamazaki et al., 2000 |
15–20 | HLM | Pacli | 0.30 | <0.01 | Yamazaki et al., 2000 | ||||||
2.33 | 2.59 | Competitive | HLM | Pacli | 1.16 | 0.01 | Sahi et al., 2003 | ||||
9.78 | rCYP2C8 | Pacli | 0.61 | <0.01 | Gao et al., 2010 | ||||||
Troglitazone M1 | Drug metabolite | 9–41 | rCYP2C8 | Pacli | Yamazaki et al., 2000 | ||||||
Troglitazone M3 | Drug metabolite | 6-26 | 3.0 | Competitive | rCYP2C8 | Pacli | Yamazaki et al., 2000 | ||||
39–>50 | HLM | Pacli | Yamazaki et al., 2000 | ||||||||
Troleandomycin | Antibiotic | 953.0 | rCYP2C8 | Phena | 3 | <0.01 | Sai et al., 2000 | ||||
TSAHC | Anticancer | 1.0 | 0.81 | Noncompetitive | HLM | Amo | Im et al., 2012 | ||||
Ulipristal | Contraceptive, progesterone receptor modulator | 2.6 | HLM | Pacli | 0.037 | <0.06 | 0.03 | <0.01 | FDA, 2010b | ||
UTL-5g | Chemoprotective, TNF-α inhibitor | 61.2 | HLM | Rosi-OH | Wu et al., 2014 | ||||||
Valdecoxib | Anti-inflammatory, NSAID | 15.0 | rCYP2C8 | Amo | 0.512 | 0.02 | 0.07 | <0.01 | Walsky et al., 2005a | ||
Vemurafenib | Anticancer, PKI | 12 | HLM | n/a | 125 | <0.01 | 20.9 | 0.21 | EMA, 2012d | ||
Vidupiprant (AMG 853) | Antiasthmatic, PGD2 receptor antagonist | 1.8 | Biphasic | HLM | Monte | Foti et al., 2012 | |||||
5.4 | 1.1 | Competitive | HLM | Pacli | Foti et al., 2012 | ||||||
6.0 | Competitive | HLM | Rosi | Foti et al., 2012 | |||||||
Vidupiprant acyl glucuronide (M1) | Drug metabolite | 7.3 | Biphasic | HLM | Monte | Foti et al., 2012 | |||||
2.7 | Mixed | HLM | Pacli | Foti et al., 2012 | |||||||
6.9 | Mixed | HLM | Rosi | Foti et al., 2012 | |||||||
Vilazodone | Antidepressant, SSRI | 1.8 | 0.46 | Competitive | HLM | Pacli | 0.33 | 0.04 | 0.72 | 0.03 | FDA, 2011g |
Vinblastine | Anticancer | 100 | HLM | Pacli | Monsarrat et al., 1997 | ||||||
Vincristine | Anticancer | 8 | HLM | Pacli | 0.43 | 0.11 | Monsarrat et al., 1997 | ||||
Vismodegib (GDC-0449) | Anticancer, SMO Antagonist | 6.0 | Noncompetitive | HLM | Pacli | 16.4 | 0.01 | 2.73 | 0.03 | Wong et al., 2009; LoRusso et al., 2013 | |
Vorapaxar | Antithrombotic, platelet aggregation inhibitor | 1.5 | 0.86 | Mixed | HLM | n/a | 0.0527 | 0.002 | 0.06 | <0.01 | Chen et al., 2014, FDA, 2014l |
Vortioxetine | Antidepressant, SMS | 9.34 | HLM | n/a | 0.04724 | 0.02 | <0.01 | <0.01 | FDA, 2013j | ||
Vortioxetine metabolite Lu AA34443 | Drug metabolite | 4.24 | HLM | n/a | FDA, 2013j | ||||||
Zafirlukast | Antiasthmatic, LTRA | 0.644 | rCYP2C8 | Amo | 0.295 | <0.01 | 0.92 | <0.01 | Walsky et al., 2005a | ||
0.388 | HLM | Amo | 1.52 | 0.02 | Walsky et al., 2005a | ||||||
0.78 | HLM | Pio | 0.76 | Jaakkola et al., 2006c | |||||||
>100 | Hep | Amo | <0.01 | <0.01 | Kosugi et al., 2014 | ||||||
0.014 | HLM | Amo | 42.14 | 0.42 | Nirogi et al., 2014 |
3-ASBA, 3-(anilinosulfonyl)-benzenecarboxylic acid; 5-HT, 5-hydroxytryptamine (serotonin); 5-MeO-DIPT, 5-methoxy-N,N-diisopropyltryptamine; ARB, angiotensin II receptor blocker; BTFM gemfibrozil, 5-(2,5-bis(trifluoromethyl)phenoxy)-2,2-dimethylpentanoic acid; CCB, calcium channel blocker; CP-778875; 5-(N-(4-((4-ethylbenzyl)thio)phenyl)sulfamoyl)-2-methyl benzoic acid; ERA, endothelin receptor antagonist; fu, fraction unbound in plasma; GABA, γ-aminobutyric acid; H2RA, H-2 receptor antagonist; HLM, human liver microsomes; HMG-CoA, 3-hydroxy-3-methylglutaryl-coenzyme A; IC50, inhibitor concentration supporting half of the maximal inhibition; Imax, peak inhibitor concentration in plasma; Ki, reversible inhibition constant; LABA, long-acting β-adrenoceptor agonist; LTRA, leukotriene receptor antagonist; MAO, monoamine oxidase; MMB4 DMS, 1,1′-methylenebis [4-[(hydroxyimino)methyl]-pyridinium] dimethanesulfonate; c-mpl, myeloproliferative leukemia; n/a, not available; NNRTI, nonnucleoside reverse transcriptase inhibitor; NS, nonstructural protein; NSAID, nonsteroidal anti-inflammatory drug; PDE, phosphodiesterase; PGD2, prostaglandin D2; PKI, protein kinase inhibitor; PPAR, peroxisome proliferator-activated receptor; PPI, proton pump inhibitor; rCYP2C8, recombinant CYP2C8; SERM, selective estrogen receptor modulator; SGLT, sodium-glucose linked transporter; SMO, smoothened receptor; SMS, serotonin modulator and stimulator; SNRI, serotonin-norepinephrine reuptake inhibitor; SSRI, selective serotonin reuptake inhibitor; TNF, tumor necrosis factor; TSAHC, 4-(p-toluenesulfonylamido)-4-hydroxychalcone; XO, xanthine oxidase; UTL-5g, N-(2,4-dichlorophenyl)-5-methyl-1,2-oxazole-3-carboxamide.
↵a 2-TPE, 2-aroylthiophen 5-hydyroxylation; Ami, aminopyrine N-demethylation; Amo, amodiaquine N-deethylation; Carba, carbamazepine 10,11-epoxidation; Ceri-1, cerivastatin demethylation (M-1); Ceri-23, cerivastatin 6-hydroxylation (M-23); DBF, dibenzylfluorescein (fluorescent reaction); Dia, diazepam N-demethylation; DTP, 2,3-dichloro-4(2-thenoyl) phenol 5-hydroxylation; Fluo, fluorometric reaction; R-ibu-2, R-ibuprofen 2-hydroxylation; R-ibu-3, R-ibuprofen 3-hydroxylation; S-ibu-2, S-ibuprofen 2-hydroxylation; S-ibu-3, S-ibuprofen 3-hydroxylation; Luci, luciferin-6 methyl ether demethylation (luminogenic reaction); Monte, montelukast 36-hydroxylation; Monte-4, formation of montelukast metabolite 4; Pacli, paclitaxel 6α-hydroxylation; Phena, phenanthrene hydroxylation; Pio, pioglitazone hydroxylation (M-IV); Repa, repaglinide 3′-hydroxylation; Rosi, rosiglitazone N-demethylation; Rosi-OH, rosiglitazone p-hydroxylation; Taza, tazarotenic acid sulfoxidation; Tolbu, tolbutamide methyl hydroxylation; Torse, torsemide methylhydroxylation.
↵b This information is primarily based on information from the UW Metabolism and Transport Drug Interaction Database (DIDB), Copyright University of Washington 1999-2015 (DIDB accessed May-September, 2015), and secondarily on information from Martindale: The Complete Drug Reference. London: Pharmaceutical Press (electronic version), Truven Health Analytics (Healthcare), Greenwood Village, Colorado. Available at: http://www.micromedexsolutions.com/ (Martindale accessed June-September, 2015). In case several values were reported for Imax and fu, the highest values were selected.
↵c When experimentally determined Ki was not available, Ki was calculated as IC50/2. An I/Ki > 1.0 indicates that a clinically relevant inhibition is likely, I/Ki = 0.1–1 indicates that a clinically relevant inhibition is possible, I/Ki < 0.1 indicates that a clinically relevant inhibition is unlikely.
↵d Unbound value.