Ref. In vitro model Digoxin Detection Study Aim Results
[69] MDCK-MDR1 LSC Investigate IC50 (µmol/L) of test compounds Quinidine: 14.1±1.5
Quinine: 18.6±4.5
Ketoconazole: 3.71±1.26
Itraconazole: 1.25±0.46
Astemizole: 5.16±0.27
GF120918: 0.23±0.06
[131] MDCK-MDR1 LSC Investigate IC50 (µmol/L) of test compounds Quinidine: 14.9±9.0
Ketoconazole: 3.07±0.76
Vimblastina: 17.8±2.2
GF120918: 0.06±0.003
Verapamil: 10.7±4.1
Cyclosporin A: 1.6±0.3
[130] MDCK-MDR1 LSC Investigate P-gp modulators effect on digoxin Papp(B-A) Results in % of the alteration on digoxin Papp (B-A) after addition of:
Colchicine: 93.5-102.5
Cortisol: 97-114.9
Dexamethasone: 110.5-119.3
Etoposide: 94.6-104.1
Trimetroprim: 96.5-104.1
Probenecid: 92-106.5
[149] Caco-2 LSC Investigate IC50 (µmol/L) of test compounds Verapamil: 10
Cyclosporin A: 3
Ketoconazole: 4.6
Nicardipine: 8.0
Clarithromycin: 66
[150] Caco-2 LSC Investigate IC50 (µg/mL) of six clones of Rhodiola rosea IC50 between 16.7 and 51.7.
Rhodiola rosea might be a candidate for clinical DDI.
[151] Caco-2 LSC Investigate if Aloe vera inhibits P-gp Papp of digoxin is similar with and without inhibitor in both directions;
Aloe Vera juice is not P-gp inhibitor
Table 6: In vitro assays using digoxin as a probe substrate and their characteristics. DDI, drug-drug interactions; IC50 , concentration that inhibits 50%; LC, liquid chromatography; LSC, Liquid scintillation counter; MDCK, Madin-Darby canine kidney cell line; L-MDR1, porcine kidney tubular cell line transfected with human MDR1 gene; MDCK-MDR1, Madin-Darby canine kidney cell line transfected with human MDR1 gene; Papp (B-A), apparent permeability in efflux direction.
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