Table 3 Cmax, IC15, IC50 and percent reduction values obtained from intestinal toxicity assays.
Drug | Clinical Cmax (μM) | IC15 (μM) | IC50 (μM) | Reduction (%) | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
hIEC TEER | Caco-2 TEER | hIEC ATP | Caco-2 ATP | hIEC TEER | Caco-2 TEER | hIEC ATP | Caco-2 ATP | hIEC TEER | Caco-2 TEER | hIEC ATP | Caco-2 ATP | ||
Paclitaxel | 5.1 | 2.71 | 7.04 | 8.01 | 69.00 | 15.33 | 39.91 | 45.41 | 391.00 | 89.51 | 76.32 | 60.91 | 19.38 |
Docetaxel | 5.1 | 4.36 | 19.25 | 88.94 | 291.18 | 24.69 | 109.10 | 504.00 | 1650.00 | 91.28 | 50.38 | 10.69 | 1.71 |
Capecitabine | 13.7 | 5.74 | 10.27 | 62.59 | >100 μм | 32.52 | 58.21 | 354.70 | >100 μм | 79.92 | 70.45 | 18.49 | −10.35 |
Cyclophosphamide | 122.0 | 7.40 | 22.84 | 40.50 | >100 μм | 41.91 | 129.40 | 229.50 | >100 μм | 67.94 | 44.51 | 29.32 | −15.13 |
Cisplatin | 14.8 | 30.49 | 44.45 | 2.62 | 7.10 | 172.80 | 251.90 | 14.84 | 40.26 | 36.84 | 31.31 | 78.90 | 84.85 |
5-FU | 34.1 | 19.31 | 17.60 | 87.78 | 74.47 | 109.40 | 99.74 | 497.40 | 422.00 | 65.48 | 78.64 | 22.64 | 24.14 |
Doxorubicin | 7.6 | 1.99 | 3.08 | 0.28 | 7.42 | 11.28 | 17.48 | 1.61 | 42.04 | 95.35 | 94.75 | 76.28 | 58.92 |
Gefitinib | 0.5 | 3.80 | 2.41 | 5.81 | 2.24 | 21.51 | 13.68 | 32.95 | 12.72 | 90.44 | 98.16 | 75.25 | 82.42 |
Crizotinib | 1.0 | 4.81 | 4.64 | 5.70 | 3.78 | 27.25 | 26.31 | 32.32 | 21.41 | 88.04 | 98.27 | 82.94 | 86.50 |
Sunitinib | 0.3 | 3.68 | 7.70 | 2.25 | 6.24 | 20.87 | 43.61 | 12.77 | 35.35 | 96.79 | 91.17 | 80.96 | 80.57 |
Sorafenib | 6.5 | 3.36 | 3.77 | 3.26 | 19.82 | 19.05 | 21.38 | 19.32 | 112.30 | 87.72 | 93.32 | 75.98 | 43.81 |
Lapatinib | 4.2 | 5.44 | 2.98 | 3.48 | 3.64 | 30.82 | 16.89 | 19.73 | 20.63 | 80.26 | 93.56 | 79.81 | 79.31 |
Ibuprofen | 145.0 | >100 μм* | >100 μм | >100 μм | 59.49 | >100 μм | >100 μм | >100 μм | 337.10 | −8.14 | −23.28 | 1.75 | 24.28 |
Diclofenac | 5.0 | 43.52 | 1018.24 | >100 μм | 110.47 | 246.60 | 5,770.00 | >100 μм | 626.00 | 23.83 | 0.99 | 3.31 | 16.63 |
Naproxen | 313.0 | 7.90 | 37.01 | 177.71 | 42.25 | 44.75 | 209.70 | 1,007.00 | 239.40 | 47.84 | 54.68 | 14.01 | 34.81 |
Ketoprofen | 10.8 | 14.11 | 25.50 | 150.74 | 30.46 | 79.98 | 144.50 | 854.20 | 172.60 | 49.84 | 59.11 | 17.00 | 38.82 |
Ketorolac | 11.0 | 134.29 | 156.05 | 150.74 | 34.82 | 761.00 | 884.30 | 854.20 | 197.30 | 10.60 | 14.63 | 17.00 | 30.03 |