Study overview
| Study | Description | Dosing Regimen | Route | Blood Sample Collection | Measured |
|---|---|---|---|---|---|
| Rat | |||||
| 1 | Single-dose PKPD study in Lewis rat | Single intravenous fingolimod dose: 1 mg/kg or single oral fingolimod dose: 0.1, 0.3, 1, or 3 mg/kg (n = 3 per group) | iv and oral | i.v.: 0, 0.25, 0.5, 1, 2, 6, 24, and 48 hours after dose; oral: 0, 1, 2, 6, 24, 48, 96, 168, 216, 264, and 336 hours after dose | fingolimod and fingolimod-P |
| 2 | Pharmacokinetics of fingolimod and fingolimod-P in male Sprague-Dawley rats after single intravenous administration of fingolimod or fingolimod-P | Single intravenous fingolimod dose: 1 mg/kg or single intravenous fingolimod-P dose: 0.1 mg/kg (n = 3 per group) | iv | 0.0083, 0.0167, 0.025, 0.033, 0.0833, 0.1667, 0.5, and 1 hour after dose | fingolimod and fingolimod-P |
| Human | |||||
| 2105 | Randomized, double-blind, placebo-controlled, multiple-dose study in healthy subjects | Once daily dosing of 0.5 mg fingolimod (n = 12), 1.25 mg fingolimod (n = 12), or placebo (n = 12) for 14 days | oral | Day 1: predose, 1, 2, 6, 8, 12, 16, 20 and 24 hours after dose. Days 3 and 7: predose (trough). Days 28 and 42: any time | fingolimod and fingolimod-P |
| 2213 | Randomized, double-blind, placebo-controlled, multiple-dose study in healthy subjects (Kovarik, 2004) | Once-daily dosing of 1.25 mg fingolimod (n = 20), 5 mg fingolimod (n = 20), or placebo (n = 20) for 7 days | oral | Days 1 and 7: predose, 1, 2, 6, 8, 12, 16, 20, and 24 hours after dose. Days 2 to 6: before (trough) and 6-8 h (peak) after the daily dose | fingolimod |
| 2215 | Randomized, single-blind, placebo-controlled, time-lagged, ascending single dose study in healthy subjects | Single dose of 5, 7.5, 10, 15, 25, or 40 mg fingolimod (n = 6, per group) or placebo (n = 2 per group) | oral | Predose, 0.25, 0.5 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 36 48, 72, 96, (120), 168, 264, 600, and 936 hours after the first dose | fingolimod and fingolimod-P |