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. 2017 Dec 6;18(12):2636. doi: 10.3390/ijms18122636

Table 1.

Pharmacokinetic parameters of cenerimod estimated following single-dose (Study 1), o.d. for 35 days (Study 2), and single-dose administration in fed or fasted conditions (Study 3).

Day 1 Day 35
Dose
(mg)
Cmax
(ng/mL)
tmax
(h)
AUC0–24
(ng·h/mL)
AUC0–∞
(ng·h/mL)
t1/2
(h)
Cmax
(ng/mL)
tmax
(h)
AUC0–24
(ng·h/mL)
AUC0–∞
(ng·h/mL)
t1/2
(h)
R
Cmax AUC0–24
Study 1 1 3.9 5.0 69.3 610 172 NC
(2.9–5.2) (4.0–8.0) (52.4–90.3) (504–735) (125–232)
3 13.1 6.0 232 2070 184
(10.1–16.8) (4.0–8.0) (181–292) (1470–2790) (153–220)
10 46.7 6.0 823 8030 199
(42.4–51.3) (6.0–8.0) (732–923) (6700–9550) (188–211)
25 122 6.2 2030 18,700 170
(89.5–161.0) (4.0–8.0) (1480–2700) (14,100–24,200) (134–213)
Study 2 0.5 2.4 5.0 41.1 NC NC 13.1 4.3 269 3390 283 5.5 6.6
(2.0–2.8) (4.0–6.0) (37.0–45.5) (9.8–17.6) (2.5–8.0) (198–366) (2050–5590) (210–381) (4.6–6.5) (5.3–8.1)
1 5.1 5.0 83.5 34.2 5.0 720 9750 436 6.7 8.6
(4.4–5.9) (4.0–6.0) (72.9–95.6) (26.8–43.7) (2.5–8.0) (560–926) (7270–13,100) (359–529) (5.5, 8.3) (7.3, 10.2)
2 7.7 6.0 134 43.9 6.0 925 11,900 415 5.7 6.9
(6.1–9.7) (4.0–8.0) (109–164) (35.9–53.8) (6.0–8.0) (767–1120) (8340–16,900) (358–481) (4.3, 7.5) (5.2, 9.3)
4 18.9 5.0 301 98.7 6.0 2100 31,900 539 5.2 7
(14.4–24.9) (4.0–6.0) (238–380) (68.0–143.0) (2.5–12.0) (1390–3170) (21,200–48,000) (492–591) (4.4, 6.3) (5.6, 8.7)
Study 3 1
fasted
4.73 6.0 83.7 649 200 NC
(4.1, 5.5) (6.0–8.0) (71.9, 97.4) (507, 832) (166, 239)
1
fed
4.35 7.0 75.5 630 191
(3.5, 5.4) (6.0–12.0) (62.0, 91.9) (498, 798) (157, 232)

The data are expressed as geometric mean (95% confidence interval), execpt tmax that is expressed as median (range). AUC0–∞: area under the curve from time zero to infinity, AUC0–24: area under the curve from time zero to 24 h, Cmax: maximum plasma concentration, NC: not calculated, R ratio Day35/Day1, t1/2: terminal half-life, tmax: time to maximum plasma concentration.