Pharmacokinetic parameters of total radiolabeled components (radioactivity) and fingolimod in blood
Data are means ± S.D. or median (range) from healthy male subjects treated with a single oral dose of 4.5 mg of [14C]fingolimod; n = 4. Radioactivity and fingolimod were determined by liquid scintillation counting and LC-MS/MS, respectively.
| Radioactivity | Fingolimod | |
|---|---|---|
| Cmax (pmol/ml) | 33.3 ± 1.1 (32.1–34.3) | 9.5 ± 1.6 (7.5–11.1) |
| Cmax (ng/ml) | 2.9 ± 0.5 (2.3–3.4) | |
| tmax (h) | 36 (36–36) | 24 (8–36) |
| AUC0–∞ (nmol · h/ml) | 12.7 ± 2.5 (9.5–15.4) | 1.85 ± 0.59 (1.01–2.39) |
| AUC0–∞ (ng · h/ml) | 568 ± 181 (312–734) | |
| CL/F (l/h)a | 8.7 ± 3.7 (6.3–14.1) | |
| Vz/F (liters)a | 1509 ± 225 (1290–1790) | |
| t1/2 (h) | 382 ± 43 (319–411) | 137 ± 55 (63–196) |
tmax, time of maximum concentration.
↵a Clearance (CL) and terminal volume of distribution (Vz), divided by absolute bioavailability (F; not determined).