Table 4 The main PK parameters of 116-N1 at day 1 and day 6 in multiple ascending-dose study.

From: Safety, tolerability, and pharmacokinetics of VV116, an oral nucleoside analog against SARS-CoV-2, in Chinese healthy subjects

Pharmacokinetic parameters

200 mg (n = 9)

400 mg (n = 9)

600 mg (n = 9)

Day 1

Day 6

Day 1

Day 6

Day 1

Day 6

AUC0-t (h·ng/mL)*

4610 (864)

9384 (1880)

10351 (2843)

20774 (8321)

12871 (3309)

25077 (7100)

AUC0-∞ (h·ng/mL)

5690 (981)

9664 (1809)

13071 (4244)

21195 (8611)

16581 (5175)

25448 (7329)

Cmax (ng/mL)

858 (186)

1131 (231)

1968 (670)

2304 (851)

2418 (708)

2842 (617)

Tmax (h)

1.50 (0.750, 1.50)

1.00 (0.750, 1.50)

1.50 (0.750, 1.50)

1.00 (0.330, 3.00)

1.50 (1.00, 6.00)

1.50 (1.00, 3.00)

t1/2 (h)

4.72 (1.02)

7.56 (1.59)

4.88 (0.718)

8.12 (0.903)

5.41 (0.808)

7.85 (0.692)

CL/F (L/h)

36.2 (6.84)

21.4 (4.28)

33.3 (9.91)

21.7 (8.20)

39.7 (13.9)

25.2 (6.83)

MRT (h)

7.42 (1.24)

9.91 (1.71)

7.56 (1.11)

10.6 (1.28)

8.20 (1.38)

10.1 (1.38)

AUC_TAU**

 

6959 (1148)

 

14745 (5419)

 

17966 (4205)

Rac_Cmax (%)

 

1.34 (0.206)

 

1.18 (0.219)

 

1.24 (0.336)

Rac_AUC (%)***

 

1.53 (0.235)

 

1.41 (0.239)

 

1.42 (0.175)

  1. AUC0-t area under the concentration–time curve from time zero to the time of the last measurable concentration, AUC0-∞ area under the concentration–time curve from time zero to infinity, Cmax maximum observed plasma concentration, Tmax time to maximum plasma concentration, t1/2 terminal elimination half-life, CL/F clearance rate, MRT mean retention time, AUC_TAU area under the concentration–time curve during a dosing interval, Rac accumulation ratio at steady state.
  2. Note: Data are expressed as mean (SD), except for Tmax, which is shown as median (min, max).
  3. *AUC0-t: the last timepoint was 12 h on day 1 and 48 h on day 6.
  4. **AUC_TAU: AUC from time 0 to 12 h.
  5. ***Rac_AUC was calculated based on AUC0-t on day 1 and AUC_TAU on day 6.
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