Table 2 The pharmacokinetic profile of bisthianostat in mice.

From: Pharmacodynamic, pharmacokinetic, and phase 1a study of bisthianostat, a novel histone deacetylase inhibitor, for the treatment of relapsed or refractory multiple myeloma

Dose

Gender

tmax

Cmax

S.E. for Cmax

AUC0–t

S.E. for AUC0–t

AUC0–∞

MRT0–∞

t1/2

CL

Vss

(mg/kg)

(h)

(μg/mL)

(μg/mL)

(h × μg/mL)

(h × μg/mL)

(h × μg/mL)

(h)

(h)

(L·h-1·kg-1)

(L/kg)

50

Male

0.25

8.34

0.48

12.1

0.68

12.8

1.35

0.96

/

/

(p.o.)

Female

0.25

7.97

0.51

14.1

0.60

14.1

1.86

1.10

/

/

 

Meana

0.25 (0.25–0.25)

8.15 (3.13%)

/

13.0 (10.9%)

/

13.4 (7.1%)

1.61 (22.4%)

1.03 (9.6%)

/

/

100

Male

0.50

8.68

1.54

15.8

1.18

16.0

1.96

0.77

/

/

(p.o.)

Female

0.50

8.65

1.12

25.9

2.12

26.0

3.45

1.13

/

/

 

Meana

0.50 (0.50–0.50)

8.66 (0.24%)

/

20.2 (35.9%)

/

20.4 (35.5%)

2.71 (38.8%)

0.95 (26.6%)

/

/

200

Male

0.50

8.88

0.68

23.3

2.28

23.8

2.52

1.82

/

/

(p.o.)

Female

0.25

10.8

2.05

26.4

2.37

26.5

2.85

1.46

/

/

 

Meana

0.38 (0.25–0.50)

9.80 (14.1%)

/

24.8 (8.9%)

/

25.1 (7.7%)

2.68 (8.1%)

1.63 (15.5%)

/

/

10

Male

/

/

/

6.80

0.18

6.81

0.22

0.26

1.47

0.33

(i.v.)

Female

/

/

/

7.88

0.39

7.90

0.24

0.29

1.27

0.30

 

Meana

/

/

/

7.32 (10.5%)

/

7.34 (10.6%)

0.23 (3.4%)

0.27 (7.1%)

1.37 (10.5%)

0.31 (7.1%)

  1. The parameters for male and female mice are calculated based on the mean concentration–time profiles and the standard error (SE) for Cmax and AUC0–t is provided additionally. / denotes not available.
  2. aThe tmax is presented by median (range), Cmax and AUC are presented by geometric mean (CV%), and others are presented by mean (CV%).
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