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Table 3 Pharmacokinetic parameters of Canocapavir on days 1 and 28 in each treatment cohort (mean ± SD)

From: Safety, tolerability, pharmacokinetics, and antiviral activity of the novel core protein allosteric modulator ZM-H1505R (Canocapavir) in chronic hepatitis B patients: a randomized multiple-dose escalation trial

 

Day 1

Day 28

50 mg n = 8

100 mg n = 8

200 mg n = 8

50 mg n = 8

100 mg n = 8

200 mg n = 8

aTmax (h)

2.0 (2.0, 3.0)

3.0 (2.0, 4.0)

3.0 (2.0, 3.0)

2.5 (2.0, 3.0)

3.0 (2.0, 4.0)

3.0 (2.0, 4.0)

Cmax (ng/mL)

1344.1 ± 498.2

2770.1 ± 652.5

4389.8 ± 1950.4

1752.3 ± 815.2

3398.7 ± 611.3

5330.6 ± 1656.4

t1/2 (h)b

   

13.0 ± 1.9

12.1 ± 3.7

15.6 ± 2.3

AUC0-24 h (h·ng/mL)

11,732.9 ± 4933.2

28,447.1 ± 9350.9

50,875.4 ± 25,750.5

18,134.1 ± 9665.9

42,115.1 ± 9863.1

73,897.0 ± 29,108.4

AUC0-t (h·ng/mL)

11,701.1 ± 4915.6

28,356.5 ± 9307.9

50,671.4 ± 25,634.8

24,716.5 ± 15,157.2

57,807.0 ± 16,630.8

114,031.6 ± 51,939.3

AUC0-∞ (h·ng/mL)b

   

25,625.6 ± 15,804.7

59,399.0 ± 18,159.0

120,090.0 ± 57,318.9

CL/F (L/h)b

   

3.4 ± 1.5

2.5 ± 0.6

3.3 ± 2.0

Vz/F (L)b

   

61.4 ± 23.0

42.3 ± 10.9

73.6 ± 43.4

Ctrough (ng/mL)

   

289.8 ± 220.7

722.8 ± 256.6

1797.7 ± 933.9

degree of fluctuation (%)

  

203.5 ± 34.2

155.8 ± 21.9

121.8 ± 33.0

RACAUC0-24 h

   

1.65 ± 0.85

1.56 ± 0.45

1.99 ± 1.81

RACCmax

   

1.44 ± 0.85

1.26 ± 0.29

1.52 ± 1.12

  1. aMedian (min–max);
  2. b0–24 h blood samples were only collected on day 1. The values of CL/F, Vz/F, t1/2, and AUC0-∞ were not well estimated due to the short elimination phase