Results from in vitro and in vivo studies evaluating the bioavailability, effects of food, and administration as crushed tablet suspension on vericiguat pharmacokinetics

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Table 4 Vericiguat bioavailability: point estimates (LS means) and two-sided 90% CIs of PK parameters after administration of vericiguat as intact tablets, PEG solution, and IV formulations

Comparison (test vs reference)	Parameter (unit)	n	CV (%)	Ratio (%)	90% CI
Relative bioavailability
5 mg intact tablet (fasted)/5 mg PEG solution (fasted)	AUC, µg*h/L	15	15.69	70.56	64.09–77.68
5 mg intact tablet (fasted)/5 mg PEG solution (fasted)	C_max, µg/L	15	27.68	59.94	50.69–70.88
1.25 mg intact tablet (fasted)/5 mg PEG solution (fasted)	AUC/D, h/L	15	15.69	92.38	83.91–101.70
1.25 mg intact tablet (fasted)/5 mg PEG solution (fasted)	C_max/D, /L	15	27.68	92.85	78.53–109.79
Absolute bioavailability study
10 mg intact tablets (fed)/20 µg IV infusion (fed)	AUC/D, h/L	10	4.23	93.03	89.86–96.31
10 mg intact tablets (fed)/20 µg IV infusion (fed)	C_max/D, /L	10	10.17	42.61	39.21–46.31

ANOVA Analysis of variance, AUC Area under curve, AUC/D Dose-normalized area under the curve, CI Confidence interval, C_max Maximum plasma concentration, C_max/D Dose-normalized maximum plasma concentration, CV Coefficient of variation, IV Intravenous, LS Least squares, PEG Polyethylene glycol
Ratio: LS means for the respective treatment ratio calculated by ANOVA