Table 3 Cmax, IC15, IC50 and percent reduction values obtained from intestinal toxicity assays.

From: Drug-induced gastrointestinal toxicity and barrier integrity: cytoskeleton-mediated impairment in a clinically relevant human intestinal epithelium model

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

  1. Cmax values (µM) were obtained from referenced sources. IC15, IC50 and percent reduction metrics were measured using TEER and ATP cell viability assays in hIEC and Caco-2 intestinal epithelial models. IC values reported as ‘>100 µM’ indicate right-censored data where no cytotoxicity or barrier disruption was detected at the highest tested concentration (100 µM). These cases were considered nontoxic within the assay range and were excluded from dose–response curve fitting.
  2. *IC15 and IC50 values reported as ‘>100 µM’ indicate right-censored data where no cytotoxicity or barrier disruption was detected at the highest tested concentration (100 µM). These cases were considered nontoxic within the assay range and were excluded from curve fitting.