Table 2.
Summary of Pharmacokinetic (PK) Parameters of Fevipiprant (PK Analysis Set) for the Single‐ and Multiple‐Dose Studies
| Dose | tmax a (h) | Cmax (ng/mL) | AUC0–24 (ng·h/mL) | AUC0–last (ng·h/mL) | t1/2 (h) |
|---|---|---|---|---|---|
| Fevipiprant Single‐Dose Study | |||||
| 10 mg | 1 (1–3) | 21 (8) | 133c (60) | 104 (58) | NC |
| 30 mg | 1 (0.5–3) | 105 (87) | 382 (120) | 445 (166) | NC |
| 100 mg | 2 (1–3) | 201 (68) | 1114 (342) | 1369 (408) | 19 (11) |
| 300 mg | 2 (1–6) | 803 (253) | 4857 (1219) | 6170 (1186) | 20 (6) |
| Dose | tmax a (h) | Cmax Day 7 (ng/mL) | AUCtau Day 7 (ng·h/mL) | Racb (AUCtau) | AG‐Metabolite/Fevipiprant AUCtau molar ratiod |
| Fevipiprant Multiple‐Dose Study | |||||
| 100 mg once daily | 2 (1–6) | 524 (217) | 2873 (783) | 1.3 (0.4) | 1.4 (0.1) |
| 300 mg once daily | 3 (1–6) | 1183 (404) | 6993 (2155) | 1.4 (0.5) | 1.3 (0.2) |
| 250 mg twice daily | 3 (2–6) | 978 (484) | 4569 (1797) | 1.8 (0.4) | 1.2 (0.1) |
Data are expressed as mean (SD) unless otherwise specified.
AUC, area under the plasma concentration–time curve; AUC0–24 h, AUC from 0 to 24 hours postdose; AUC0–last, AUC from 0 to last measurable plasma concentration; AUCtau, AUC in the dosing interval; Cmax, maximum plasma concentration; CLr, renal clearance; NC, not calculated (because of lack of sufficient data in the terminal phase); tmax, time to reach Cmax; t1/2, elimination half‐life.
atmax, expressed as median (min–max). bRac, accumulation ratio, AUCtau (day 7)/AUCtau (day 1). cThree subjects had concentrations below the limit of quantification (1 ng/mL) at 24 hours postdose. dAUCtau AG‐metabolite day 1 (μM·h)/AUCtau fevipiprant day 1 (μM·h).