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. Author manuscript; available in PMC: 2019 Jul 15.
Published in final edited form as: J Enzyme Inhib Med Chem. 2016 Jul 17;31(SUP2):148–161. doi: 10.1080/14756366.2016.1193734

Table 4.

Cmax,u / IC50 values for inhibitors of tazarotenic acid sulfoxidation. Cmax and fu data compiled from literature references as noted in the Materials and Methods.


Cmax,u/IC50

Inhibitor Oral Dose Cmax (nM) fu,plasma Cmax, u (nM) CYP 26A1 CYP 26B1
Benzbromarone 100 mg 9236 0.010 92.4 0.147 0.012
Candesartan 16 mg QD 270 0.002 0.38 < 0.001 < 0.001
Clotrimazole 1% Topical 67300* 0.100 6730 337 135
17α-Ethynylestradiol 30 μg 0.5 0.002 0.00085 < 0.001 < 0.001
Fluconazole 200 mg BID 34606 0.890 30794 44.0 1.56
Itraconazole 200 mg QD 919 0.002 1.80 0.003 0.011
Mometasone 50 μg Inhaled 0.05 0.010 0.0005 < 0.001 < 0.001
Montelukast 10 mg 925 0.010 8.90 0.077 0.015
Pioglitazone 45 mg 4489 0.010 38.0 0.048 0.005
Quercetin 500 mg TID 50.9 0.009 0.45 < 0.001 < 0.001
Raloxifene 1 mg/kg 1.05 0.050 0.50 < 0.001 < 0.001
Repaglinide 4 mg 104 0.026 2.60 < 0.001 0.004
Ritonavir 600 mg BID 15258 0.010 150 0.040 0.060
Rosiglitazone 8 mg 1673 0.002 3.40 < 0.001 < 0.001
Tamoxifen 10 mg BID 323 0.020 6.40 < 0.001 < 0.001
Zafirlukast 20 mg BID 1125 0.010 3.00 0.188 0.016
*

Represents reported clotrimazole concentration in skin (stratum corneum) following topical administration of a 1% clotrimazole cream formulation.