Table 1

Summary of pharmacokinetic parameters for fevipiprant and AG metabolite by treatment

Data are arithmetic mean ± S.D. (CV%) [n]. CV% = sqrt(exp(variance for log-transformed data)−1) × 100.

Parameter (Unit)Fevipiprant 150 mg OralProbenecid + Fevipiprant 150 mg OralAG Metabolite (after Dosing with Fevipiprant 150 mg Oral)AG Metabolite (after Dosing with Probenecid and Fevipiprant 150 mg Oral)
Cmax (ng/ml)812 ± 386 (47.5) [n = 16]1350 ± 682 (50.6) [n = 15]1070 ± 380 (35.7) [n = 16]1410 ± 703 (49.9) [n = 15]
AUClast (ng*h/ml)3530 ± 945 (26.8) [n = 16]9320 ± 4180 (44.9) [n = 15]6910 ± 2280 (33.0) [n = 16]12600 ± 7560 (60.1) [n = 15]
AUCinf (ng*h/ml)3680 ± 1010 (27.4) [n = 15]9980 ± 4520 (45.3) [n = 15]7220 ± 2340 (32.5) [n = 16]14400 ± 9270 (64.4) [n = 12]
Tmax (h)a1.50 (1.00–6.00) [n = 16]2.00 (1.00–6.00) [n = 15]2.50 (2.00–6.00) [n = 16]2.02 (1.50–6.00) [n = 15)
CL/F (l/h)43.7 ± 11.7 (26.8) [n = 15]17.8 ± 7.12 (40.0) [n = 15]
Vz/F (l)1470 ± 926 (63.2) [n = 15]600 ± 299 (49.8) [n = 15]
t1/2 (h)23.5 ± 14.6 (62.0) [n = 15]24.9 ± 11.2 (45.0) [n = 15]24.7 ± 14.5 (58.8) [n = 16]35.2 ± 18.9 (53.8) [n = 15]
MR Cmax1.05 ± 0.382 (36.3) [n = 16]0.802 ± 0.329 (41.0) [n = 15]
MR AUCinf1.41 ± 0.362 (25.7) [n = 15]1.06 ± 0.363 (34.4) [n = 12]
MR AUClast1.41 ± 0.342 (24.1) [n = 16]0.977 ± 0.354 (36.3) [n = 15]
Ae0–last (mg)27.7 ± 8.57 [n = 16]7.08 ± 2.15 [n = 15]36.5 ± 9.62 [n = 16]13.0 ± 5.80 [n = 15]
CLr (l/h)9.87 ± 1.85 (18.7) [n = 16]1.21 ± 0.378 (31.2) [n = 15]7.14 ± 1.79 (25.0) [n = 16]1.66 ± 0.350 (21.1) [n = 15]
  • exp, exponent; max, maximum value; min, minimum value; sqrt, square root; Tmax, time of maximal observed plasma concentration.

  • a For Tmax, data are median (min–max) [n].