Component | Cmax | tmax | AUC0–816 h | AUC0–∞ | t1/2 |
---|---|---|---|---|---|
pmol/ml (ng/ml) | h | nmol · h/ml (ng · h/ml) | nmol · h/ml (ng · h/ml) | h | |
M3 | 3.8 (1.1) | 12 | 0.776 (218) | 0.808 (227) | 170 |
M2 | 0.6 (0.2) | 12 | 0.140 (43) | 0.140 (43) | N.D. |
Fingolimoda | 9.2 (2.8) | 36 | 2.18 (669) | 2.25 (691) | 162 |
Fingolimod phosphate | 8.4 (3.3) | 12 | 0.965 (374) | 0.999 (387) | 166 |
M27b | 0.2 (0.1) | 216 | 0.072 (41) | 0.072 (41) | N.D. |
M28b | 0.5 (0.3) | 36 | 0.046 (25) | 0.046 (25) | N.D. |
M29 | 1.2 (0.7) | 36c | 0.834 (492) | 1.19 (704) | 404d |
M30 | 1.6 (0.9) | 72 | 0.684 (393) | 0.927 (532) | 410d |
Sum of additional metabolites detected | N.D. | N.D. | 2.78e | N.D. | N.D. |
Material lost during sample preparationf | N.D. | N.D. | 0.884 | N.D. | N.D. |
Total radioactivity | 33.3 | 36 | 9.35 | 12.7 | 382 |
tmax, time of maximum concentration; N.D., not determined.
↵a Differences from values in Table 1 are due to the different methods of analysis and different numbers of time points analyzed.
↵b Detected only at 2 time points.
↵c Concentrations showed a plateau between 36 and 480 h postdose.
↵d Estimated values, based on two time points (480 and 816 h).
↵e Numerous polar as well as nonpolar trace components, all less than 2.2% of AUC0–816 h of total radiolabeled components.
↵f No material lost during chromatography.