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Table 5 PR-104 and PR-104A plasma pharmacokinetic parameters for cycle 1 day 1

From: A phase I trial of PR-104, a pre-prodrug of the bioreductive prodrug PR-104A, given weekly to solid tumour patients

   

Cmax(μM)

AUC (μM.h)

t1/2(h)

Cl (L/h/m2)

Vdss(L/m2)

Dose-level (mg/m2)

 

n

PR-104

PR-104A

PR-104

PR-104A

PR-104

PR-104A

PR-104

PR-104

135

 

2

4.08

3.49

2.85

3.22

0.06

0.34

128

38.7

270

 

6

7.63 (3.13)

6.81 (2.15)

4.15 (1.69)

6.61 (2.88)

0.07 (0.05)

0.42 (0.16)

129 (49.4)

39.1 (9.83)

540

 

6

14.2 (6.51)

13.7 (2.94)

9.34 (4.17)

14.0 (2.70)

0.07 (0.03)

0.42 (0.16)

130 (119)

44.7 (38.5)

675

 

7

18.1 (9.9)

15.5 (6.1)

12.9 (7.0)

17.7 (5.6)

0.14 (0.10)

0.55 (0.11)

92.7 (52.2)

27.3 (14.4)

900

 

4

20.8 (5.71)

23.3 (4.64)

15.2 (4.97)

29.5 (8.44)

0.15 (0.10)

0.68 (0.14)

64.8 (22.9)

24.2 (10.5)

  1. Values are the mean (SD)