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Table 3 Pharmacokinetics parameters after a repeat (7-day) rising dose in healthy volunteers.

From: Pharmacokinetics, Safety and Inducible Cytokine Responses during a Phase 1 Trial of the Oral Histone Deacetylase Inhibitor ITF2357 (Givinostat)

Dose

 

50 mg every day

100 mg every day

200 mg every day

100 mg twice a day

Day 1

 

Day 7

Day 1

Day 7

Day 1

Day 7

Day 1a

Day 7a

Cmax

(ng/mL)

56 ± 5

67 ± 5

124 ± 9

135 ± 10

322 ± 26

283 ± 16

116 ± 15

182b ± 17

Cmin

(ng/mL)

2.4 ± 0.2

3.5 ± 0.2

4.1 ± 0.3

5.5 ± 0.3

10.2 ± 1.3

12.0 ± 1.4

17.7 ± 1.6

30.9 ± 2.6

max

(h)

2.5 ± 0.5

2.1 ± 0.4

2.6 ± 0.4

2.8 ± 0.34

2.4 ± 0.4

2.6 ± 0.4

2.8 ± 0.4

3.1 ± 0.6

AUC0-†

(ng · h/mL)

369 ± 23

452 ± 20

771 ± 27

891 ± 32

1875 ± 102

1,907 ± 130

1,326 ± 148

1,084 ± 84

Half-life

(h)

7.31 ± 0.16

6.47 ± 0.22

6.54 ± 0.16

  1. aFirst daily dose.
  2. bStatistically significant difference (P> 0.05) from day 1 Cmax.