Table 3 Plasma pharmacokinetic parameters of ZSP1601 and M3–5

From: ZSP1601, a novel pan-phosphodiesterase inhibitor for the treatment of NAFLD, A randomized, placebo-controlled phase Ib/IIa trial

Treatment

Day 1

Day 14

t1/2 (h)

Tmax (h)

Cmax (μg/mL)

AUC0-12h (h μg/mL)

Tmax (h)

Cmax (μg/mL)

AUCss (h μg/mL)

RCmax

RAUC

ZSP1601

50 mg QD (n = 9)

9.20 (2.56)

2.50 (1.50–4.00)

1.00 (0.208)

7.59 (1.44)

2.00 (0.750–3.00)

1.32 (0.217)

14.7 (3.48)

1.33 (0.169)

1.36 (0.0848)

50 mg BID (n = 9)

–

2.50 (0.250–4.00)

1.11 (0.234)

7.59 (0.948)

2.00 (0.500–3.00)

1.83 (0.330)

14.7 (2.34)

1.71 (0.457)

1.95 (0.306)

100 mg BID (n = 9)

–

2.00 (0.750–3.00)

2.33 (0.371)

15.9 (1.56)

1.00 (0.500–3.00)

3.60 (0.469)

27.8 (5.25)

1.58 (0.327)

1.75 (0.322)

M3–5

50 mg QD (n = 9)

–

6.00 (6.00–12.0)

0.266 (0.0415)

2.43 (0.451)

6.00 (2.50–8.00)

0.403 (0.0599)

7.05 (1.41)

1.53 (0.180)

1.57 (0.166)

50 mg BID (n = 9)

–

8.00 (6.00−11.5)

0.232 (0.0430)

2.14 (0.508)

4.00 (2.00–8.00)

0.630 (0.101)

6.53 (1.09)

2.77 (0.507)

3.15 (0.618)

100 mg BID (n = 9)

–

6.00 (4.00−11.8)

0.553 (0.114)

5.24 (1.19)

3.00 (1.00–6.00)

1.33 (0.116)

13.7 (1.55)

2.50 (0.581)

2.77 (0.874)

  1. Results were expressed as the arithmetic mean (standard deviation), except for Tmax which was presented as median (range). t1/2, elimination half-life; Cmax, maximum concentration in the plasma; Tmax, the time of peak plasma concentration or the time needed to reach Cmax; AUC0–12h, the area under the plasma concentration-time curve from 0 to 12 h; AUCss, the area under the plasma concentration–time curve at steady state; RCmax, accumulation ratio Cmax.
Back to article page